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Integrative Structural and Computational Biology

Patrick Griffin, PhD

Scientific Director
Department of Molecular Medicine
Florida Campus
Laboratory Website
(561) 228-2200

Scripps Research Joint Appointments

Director, Translational Research Institute
Department of Integrative Structural and Computational Biology
Faculty, Graduate Program

Research Focus

Group Members: Ruben D. Garcia-Ordonez, Scott Novick, and Mi Ra Chang.  Current Students: Valentine Courouble and Kuang-Ting Kuo. Former members of the lab: Tim Strutzenberg, Jie Zheng, Anthony Ciesla, Bruce Pascal, Vinh Lam, Venkat Dharmarajan, Tanya Khan, Dana Kuruvilla, Elizabeth Miguet, A. Corzo, D. Goswami, D. Marciano, Y. Mari, G. West, M.J. Chalmers, N. Kumar, J. Lauer, S.A. Busby, R. Landgraf, S. Willis, M. Istrate, D. Policastro, C. Griffin, E. Tracy, J. Zhang, X. Zhang, S. Dai, S. Prasad, R. Leon.

My scientific career has focused on the study of protein structure and approaches to modulating protein function via synthetic small molecules with a focus on nuclear receptors. I have a broad background in drug discovery and development that spans the last 25+ years. I received a Ph.D. in Chemistry from the University of Virginia under the direction of Professor Donald F. Hunt where I was involved in methodology development in the field of Biological Mass Spectrometry. After graduating from UVa, I was a Postdoctoral Fellow for Professor Leroy Hood at Caltech where I was involved in the application of mass spectrometry to systems biology.

Prior to Scripps, I was Chief Science Officer of ExSAR Corporation, NJ, a biotech company focused the use of HDX mass spectrometry (HDX-MS) to aid in the development of chemical chaperones for protein misfolding disorders. Prior to ExSAR, I was Senior Director, Chemistry, at Merck Research Laboratories where he spent over 11 years applying biological mass spectrometry and proteomics to a wide range of therapeutic areas including metabolic disorders, cardiovascular disease, and infectious diseases. At Merck, I headed the discovery DMPK operation within the Chemistry Department and the Molecular Profiling Proteomics group. My team made significant contributions to over 35 safety assessment programs. Most significant were my team’s contributions towards the discovery and development of MK-0431, a DPP4 inhibitor now in clinical use (Januvia), and towards clinical development of DMP-777, an elastase inhibitor for treatment of cystic fibrosis that progressed to phase IIb trials.

In 2004, I joined The Scripps Research Institute (TSRI) Scripps Florida as Professor and in 2007 was named Professor and founding Chair of the Department of Molecular Therapeutics. As PI, Co-PI, and co-investigator on several NIH-funded grants, my research continues to focus on protein structure and function, particularly on mutational- and ligand-mediated alterations in protein structural plasticity, as well as quantitative SAR to facilitate lead optimization of molecules targeting therapeutic proteins. Using mutagenesis, HDX-MS, crystallography, proteomics and genomics my research is focused on structure-function of nuclear receptors, enzymes, and G protein coupled receptors (GPCRs). My research program has a major focus on understanding nuclear receptor (NR) signaling using structural, chemical and biological approaches. We have made significant contributions to understanding the mechanism of ligand activation of NRs such as PPARs, RORs, REV-ERBs, LRH1, VDR, ER, GR, and PR. We have also made significant contributions dissecting domain-domain interactions in control of positive and negative allostery. Our chemical biology program is focused on the RORs, PPARs, VDR and LRH1. In each of these programs we are developing functionally selective and promoter-specific modulators targeting disease such as cancer, autoimmune, obesity, and diabetes. My lab is well known for the development and application of biophysical methods including our HDX and XL-MS platform for the analysis of protein plasticity with a focus on NRs, enzymes, and GPCRs.

For the first half of my career I was in industry where there was less of an emphasis on publications. However, over the last 16 years as an academic I have published >240 peer-reviewed manuscripts.  According to Google Scholar I have an h-index of 83 (58 since 2016) and an i10-index of 223.  Below is a URL for My Bibliography of Patrick R. Griffin; some papers are under Griffin P

Contributions to Science

As a graduate student at the University of Virginia, I worked in Don Hunt’s lab alongside John Yates and together we performed ground-breaking studies in the use of mass spectrometry to determine the primary structure of proteins. I am first author on a paper describing the complete sequence of a protein using tandem mass spectrometry. Prior, only a few small proteins for which their amino sequence was known had been sequenced by tandem mass spectrometry. This work helped validate that it was possible to sequence proteins using tandem mass spectrometry. I am first author on one of the first papers describing the using low nano-LC coupled with ESI. I contributed to many other publications demonstrating the use of mass spectrometry for structural analysis of proteins.

While at Merck Research Laboratories, my lab made significant contributions to a wide range of projects including key contributions to the development of the DPP4 program which led to the approval and marketing of Januiva. The range of contributions to drug discovery and development are exemplified in manuscripts listed below. My efforts in drug discovery have continued in the academic setting.

In 2002 I became interested in the application of hydrogen/deuterium exchange mass spectrometry. My lab focused on the development of a fully automated system, advanced software to facilitate robust high precision analysis, and applications of HDX in protein-ligand interactions with an emphasis on nuclear receptors, enzymes, and GPCRs. The publications listed below include an extensive list of key contributions to the HDX field.

In addition to the advancement of structural proteomics, my research has focused on chemical biology approaches to better understand nuclear receptor signaling. Our group described the first synthetic ligand for the orphan nuclear receptor NR1F subfamily (ROR)s and subsequently showed the utility of advanced compounds as anti-inflammatory and anti-obesity agents as well as RORG agonists for enhancing protective immunity in the context of cancer therapy. Our lab has also contributed to a fundamentally new understanding of the mechanism by which the nuclear receptor PPARG impacts insulin sensitivity.

Highlights on grant funding related to drug development programs

• I was consortium PI of the “The Comprehensive Center for Chemical Probe Discovery and Optimization at Scripps,” I had both a leadership role and a scientific role on this large multi-center 6-year U54 MLPCN Roadmap initiative.

• I was consortium PI of a RC4 program in collaboration with Bruce Spiegelman at the Dana Faber, I was involved in the discovery and development of novel molecules for the treatment of obesity and diabetes. Work from our labs in this area led us to co-found Ember, a private biotech funded by Third Rock Ventures.

• I was Co-PI on a NIDA funded U19 NCDDDG focused on the discovery and development of novel positive allosteric modulators of GABAB receptor for treatment of nicotine addiction.

• I served on the Scripps-Pfizer collaboration Steering Committee for its 5 year term coordinating collaborative drug discovery programs.

• I am PI of a 13-year long collaboration between my lab and Eli Lilly. • I am PI on a collaborative grant with the private Biotech Synkine Therapeutics.

• I am Co-PI on a NIH Blueprint UH3 titled, “Developing nonmuscle myosin II inhibitors for substance use relapse.” Co-founder of Myosin Therapeutics. The Myosin Therapeutics’ clinical candidate emerged from the NIH Blueprint program.


B.S., Chemistry, Syracuse University, 1985
Ph.D., Chemistry, University of Virginia, 1989

Professional Experience

Co-Chair, Molecular Medicine, TSRI, CA and FL, 01/17-present
Member, Board of Trustees, TSRI, CA and FL, 02/15 to 06/16
Member, Strategic Planning Committee, TSRI, CA and FL, 06/16 to 6/18
Member, Academic Planning Committee, TSRI, CA and FL, 09/15 to 06/16
Professor, Molecular Therapeutics, 03/07 to 01/17
Chair, Molecular Therapeutics, 03/07 to 09/15
Director, Translational Research Institute, 06/06 to present
Co-founder, Ember Therapeutics, 08/10
Member of Scripps Florida Steering Committee, 01/07 to 01/11
Member of Pfizer/TSRI Joint Steering Committee, 01/07 to 12/11
Member, Board of Directors, Centre for Drug Research and Development, 08/09 to 8/15
Professor Biochemistry, Scripps Florida, 05/04 - 3/07
Chief Scientific Officer, ExSAR Corporation, 07/02 - 05/04
Senior Director, Basic Chemistry and Molecular Profiling Proteomics, Merck, 09/01 - 06/02
Director, Basic Chemistry and Molecular Profiling Proteomics, Merck, 05/99 – 09/01
Senior Research Fellow, Molecular Design and Diversity, Merck, 04/96 – 05/99
Research Fellow, Inflammation Research, Merck, 12/91-04/96
Post-Doctoral Fellow, California Institute of Technology 5/90 - 12/91
Associate Scientist, Genentech, Inc. 4/89 - 4/90

Awards & Professional Activities

Dupont Chemistry Fellow, University of Virginia
Dean's Fellow, University of Virginia

Selected References

Radnai L, Surman M, Hafenbreidel M, Young EJ, Stremel RF, Lin L, Bdiri B, Pasetto P, Jin X, Geedy M, Partridge JR, Patel A, Conlon M, Sellers JR, Cameron MD, Rumbaugh G, Griffin PR, Kamenecka TM, Miller CA. Discovery of Selective Inhibitors for In Vitro and In Vivo Interrogation of Skeletal Myosin II.  ACS Chem Biol. 2021 Sep 24. doi: 10.1021/acschembio.1c00067.

Strutzenberg TS, Zhu Y, Novick SJ, Garcia-Ordonez RD, Doebelin C, He Y, Ra Chang M, Kamenecka TM, Edwards DP, Griffin PR.  Conformational Changes of RORy During Response Element Recognition and Coregulator Engagement. J Mol Biol. 2021 Sep 18:167258. doi: 10.1016/j.jmb.2021.167258.

Zhang S, Ren Q, Novick SJ, Strutzenberg TS, Griffin PR, Bao H. One-step construction of circularized nanodiscs using SpyCatcher-SpyTag.  Nat Commun. 2021 Sep 14;12(1):5451. doi: 10.1038/s41467-021-25737-7.

Min J, Nwachukwu JC, Min CK, Njeri JW, Srinivasan S, Rangarajan ES, Nettles CC, Sanabria Guillen V, Ziegler Y, Yan S, Carlson KE, Hou Y, Kim SH, Novick S, Pascal BD, Houtman R, Griffin PR, Izard T, Katzenellenbogen BS, Katzenellenbogen JA, Nettles KW.  Dual-mechanism estrogen receptor inhibitors.  Proc Natl Acad Sci U S A. 2021 Aug 31;118(35):e2101657118. doi: 10.1073/pnas.2101657118.

Yan Y, Mukherjee S, Harikumar KG, Strutzenberg TS, Zhou XE, Suino-Powell K, Xu TH, Sheldon RD, Lamp J, Brunzelle JS, Radziwon K, Ellis A, Novick SJ, Vega IE, Jones RG, Miller LJ, Xu HE, Griffin PR, Kossiakoff AA, Melcher K. Structure of an AMPK complex in an inactive, ATP-bound state.  Science. 2021 Jul 23;373(6553):413-419. doi: 10.1126/science.abe7565; PMCID: PMC8428800.

Li K, Zheng J, Wirawan M, Trinh NM, Fedorova O, Griffin PR, Pyle AM, Luo D.  Insights into the structure and RNA-binding specificity of Caenorhabditis elegans Dicer-related helicase 3 (DRH-3)  Nucleic Acids Res. 2021 Sep 27;49(17):9978-9991. doi: 10.1093/nar/gkab712; PMCID: PMC8464030.

Shirey RJ, Hart JR, Sridharan B, Novick SJ, Turner LD, Zhou B, Nielsen AL, Eubanks LM, Ueno L, Hixon MS, Lairson LL, Spicer TP, Scampavia LD, Griffin PR, Vogt PK, Janda KD.Bioorg. Synthetic fluorescent MYC probe: Inhibitor binding site elucidation ad development of a high-throughput screening assay.  Med Chem. 2021 Jul 15;42:116246. doi: 10.1016/j.bmc.2021.116246. Epub 2021 Jun 6; PMCID: PMC8279689.

Courouble VV, Dey SK, Yadav R, Timm J, Harrison JJEK, Ruiz FX, Arnold E, Griffin PR. Revealing the Structural Plasticity of SARS-CoV-2 nsp7 and nsp8 Using Structural Peoteomics.  J Am Soc Mass Spectrom. 2021 Jul 7;32(7):1618-1630. doi: 10.1021/jasms.1c00086. Epub 2021 Jun 14; PMCID: PMC8231661.

Shin M, Watson ER, Song AS, Mindrebo JT, Novick SJ, Griffin PR, Wiseman RL, Lander GC.  Structures of the human LONP1 protease reveal regulatory steps involved in protease activation.  Nat Commun. 2021 May 28;12(1):3239.  PMCID: PMC8163871.

Sun L, Wei N, Kuhle B, Blocquel D, Novick S, Matuszek Z, Zhou H, He W, Zhang J, Weber T, Horvath R, Latour P, Pan T, Schimmel P, Griffin PR, Yang XL. CMT2N-causing aminoacylation domain mutants enable Nrp1 interaction with AlaRS. Proc Natl Acad Sci U S A. 2021 Mar 30;118(13):e2012898118. PMCID: PMC8020758.

Baroi S, Czernik PJ, Chougule A, Griffin PR, Lecka-Czernik B. PPARG in osteocytes controls sclerostin expression, bone mass, marrow adiposity and mediates TZD-induced bone loss. Bone. 2021 Jun;147:115913. Epub 2021 Mar 16. PMCID: PMC8076091.

Courouble VV, Dey SK, Yadav R, Timm J, Harrison JJEK, Ruiz FX, Arnold E, Griffin PR. Resolving the Dynamic Motions of SARS-CoV-2 nsp7 and nsp8 Proteins Using Structural Proteomics. bioRxiv. 2021 Mar 6:2021.03.06.434214. Preprint. PMCID: PMC7941636.

Mosure SA, Strutzenberg TS, Shang J, Munoz-Tello P, Solt LA, Griffin PR, Kojetin DJ Structural basis for heme-dependent NCoR binding to the transcriptional repressor REV-ERBβ. Sci Adv. 2021 Jan 27;7(5):eabc6479. Print 2021 Jan. PMCID: PMC7840129.

Lam AT, Zhang XN, Courouble VV, Strutzenberg TS, Pei H, Stiles BL, Louie SG, Griffin PR, Zhang Y. A Bifunctional NAD+ for Profiling Poly-ADP-Ribosylation-Dependent Interacting Proteins. ACS Chem Biol. 2021 Feb 19;16(2):389-396. Epub 2021 Feb 1. PMCID: PMC7909001.

Lin H, Sharabi K, Lin L, Ruiz C, Zhu D, Cameron MD, Novick SJ, Griffin PR, Puigserver P, Kamenecka TM Structure-Activity Relationship and Biological Investigation of SR18292 (16), a Suppressor of Glucagon-Induced Glucose Production. J Med Chem. 2021 Jan 28;64(2):980-990. Epub 2021 Jan 12. PMCID: PMC7869975.

Radnai L, Stremel RF, Vaissiere T, Lin L, Cameron M, Martin WH, Rumbaugh G, Kamenecka TM, Griffin PR, Miller CA. A simple and robust cell-based assay for the discovery of novel cytokinesis inhibitors. J Biol Methods. 2020 Sep 17;7(3):e136.  eCollection 2020. PMCID: PMC7666332.

Liu WH, Zheng J, Feldman JL, Klein MA, Kuznetsov VI, Peterson CL, Griffin PR, Denu JM. Multivalent interactions drive nucleosome binding and efficient chromatin deacetylation by SIRT6. Nat Commun. 2020 Oct 16;11(1):5244. PMCID: PMC7568541.

Bester SM, Wei G, Zhao H, Adu-Ampratwum D, Iqbal N, Courouble VV, Francis AC, Annamalai AS, Singh PK, Shkriabai N, Van Blerkom P, Morrison J, Poeschla EM, Engelman AN, Melikyan GB, Griffin PR, Fuchs JR, Asturias FJ, Kvaratskhelia M. Structural and mechanistic bases for a potent HIV-1 capsid inhibitor. Science. 2020 Oct 16;370(6514):360-364. PMCID: PMC7831379.

Smith E, Davis-Gardner ME, Garcia-Ordonez RD, Nguyen TT, Hull M, Chen E, Baillargeon P, Scampavia L, Strutzenberg T, Griffin PR, Farzan M, Spicer TP. High-Throughput Screening for Drugs That Inhibit Papain-Like Protease in SARS-CoV-2. SLAS Discov. 2020 Dec;25(10):1152-1161. Epub 2020 Oct 10. PMCID: PMC7550789.

Zheng J, Strutzenberg TS, Reich A, Dharmarajan V, Pascal BD, Crynen GC, Novick SJ, Garcia-Ordonez RD, Griffin PR. Comparative Analysis of Cleavage Specificities of Immobilized Porcine Pepsin and Nepenthesin II under Hydrogen/Deuterium Exchange Conditions. Anal Chem. 2020 Aug 18;92(16):11018-11028. Epub 2020 Jul 30. PMID: 32658454.

Khan AK, Jagielnicki M, McIntire WE, Purdy MD, Dharmarajan V, Griffin PR, Yeager M. A Steric "Ball-and-Chain" Mechanism for pH-Mediated Regulation of Gap Junction Channels. Cell Rep. 2020 Apr 21;31(3):107482. PMID: 32320665.

Shang J, Mosure SA, Zheng J, Brust R, Bass J, Nichols A, Solt LA, Griffin PR, Kojetin DJ. A molecular switch regulating transcriptional repression and activation of PPARγ. Nat Commun. 2020 Feb 19;11(1):956. PMCID: PMC7031403.

Nguyen PDM, Zheng J, Gremminger TJ, Qiu L, Zhang D, Tuske S, Lange MJ, Griffin PR, Arnold E, Chen SJ, Zou X, Heng X, Burke DH. Binding interface and impact on protease cleavage for an RNA aptamer to HIV-1 reverse transcriptase. Nucleic Acids Res. 2020 Mar 18;48(5):2709-2722. PMCID: PMC7049723.

Tuske S, Zheng J, Olson ED, Ruiz FX, Pascal BD, Hoang A, Bauman JD, Das K, DeStefano JJ, Musier-Forsyth K, Griffin PR, Arnold E. Integrative structural biology studies of HIV-1 reverse transcriptase binding to a high-affinity DNA aptamer. Curr Res Struct Biol. 2020;2:116-129. Epub 2020 Jun 30. PMCID: PMC8052095.

Heidari Z, Chrisman IM, Nemetchek MD, Novick SJ, Blayo AL, Patton T, Mendes DE, Diaz P, Kamenecka TM, Griffin PR, Hughes TS. Definition of functionally and structurally distinct repressive states in the nuclear receptor PPARγ. Nat Commun. 2019 Dec 20;10(1):5825. PMCID: PMC6925260.

Berman HM, Adams PD, Bonvin AA, Burley SK, Carragher B, Chiu W, DiMaio F, Ferrin TE, Gabanyi MJ, Goddard TD, Griffin PR, Haas J, Hanke CA, Hoch JC, Hummer G, Kurisu G, Lawson CL, Leitner A, Markley JL, Meiler J, Montelione GT, Phillips GN Jr, Prisner T, Rappsilber J, Schriemer DC, Schwede T, Seidel CAM, Strutzenberg TS, Svergun DI, Tajkhorshid E, Trewhella J, Vallat B, Velankar S, Vuister GW, Webb B, Westbrook JD, White KL, Sali Federating Structural Models and Data: Outcomes from A Workshop on Archiving Integrative Structures. A.Structure. 2019 Dec 3;27(12):1745-1759. Epub 2019 Nov 25. PMCID: PMC7108332.

Espada A, Haro R, Castañon J, Sayago C, Perez-Cozar F, Cano L, Redero P, Molina-Martin M, Broughton H, Stites RE, Pascal BD, Griffin PR, Dodge JA, Chalmers MJ. A Decoupled Automation Platform for Hydrogen/Deuterium Exchange Mass Spectrometry Experiments. J Am Soc Mass Spectrom. 2019 Dec;30(12):2580-2583. Epub 2019 Nov 13. PMID: 31724102.

Sanulli S, Trnka MJ, Dharmarajan V, Tibble RW, Pascal BD, Burlingame AL, Griffin PR, Gross JD, Narlikar GJ. HP1 reshapes nucleosome core to promote phase separation of heterochromatin. Nature. 2019 Nov;575(7782):390-394. Epub 2019 Oct 16. PMCID: PMC7039410.

Shang J, Brust R, Griffin PR, Kamenecka TM, Kojetin DJ.  Quantitative structural assessment of graded receptor agonism  Proc Natl Acad Sci U S A. 2019 Oct 29;116(44):22179-22188. Epub 2019 Oct 14.  PMCID: PMC6825269.

Zheng J, Strutzenberg T, Pascal BD, Griffin PR. Protein dynamics and conformational changes explored by hydrogen/deuterium exchange mass spectrometry. Curr Opin Struct Biol. 2019 Oct;58:305-313. PMID: 31351767.

Yong HY, Zheng J, Ho VCY, Nguyen MT, Fink K, Griffin PR, Luo D. Structure-guided design of immunomodulatory RNAs specifically targeting the cytoplasmic viral RNA sensor RIG-I. FEBS Lett. 2019 Nov;593(21):3003-3014. Epub 2019 Aug 19. PMID: 31369683..

Kim H, Wrann CD, Jedrychowski M, Vidoni S, Kitase Y, Nagano K, Zhou C, Chou J, Parkman VA, Novick SJ, Strutzenberg TS, Pascal BD, Le PT, Brooks DJ, Roche AM, Gerber KK, Mattheis L, Chen W, Tu H, Bouxsein ML, Griffin PR, Baron R, Rosen CJ, Bonewald LF, Spiegelman BM. Irisin Mediates Effects on Bone and Fat via αV Integrin Receptors. Cell. 2019 Jul 11;178(2):507-508. PMCID: PMC6298040.

Masson GR, Burke JE, Ahn NG, Anand GS, Borchers C, Brier S, Bou-Assaf GM, Engen JR, Englander SW, Faber J, Garlish R, Griffin PR, Gross ML, Guttman M, Hamuro Y, Heck AJR, Houde D, Iacob RE, Jørgensen TJD, Kaltashov IA, Klinman JP, Konermann L, Man P, Mayne L, Pascal BD, Reichmann D, Skehel M, Snijder J, Strutzenberg TS, Underbakke ES, Wagner C, Wales TE, Walters BT, Weis DD, Wilson DJ, Wintrode PL, Zhang Z, Zheng J, Schriemer DC, Rand KD. Recommendations for performing, interpreting and reporting hydrogen deuterium exchange mass spectrometry (HDX-MS) experiments. Nat Methods. 2019 Jul;16(7):595-602. PMCID: PMC6614034.

Strutzenberg TS, Garcia-Ordonez RD, Novick SJ, Park H, Chang MR, Doebellin C, He Y, Patouret R, Kamenecka TM, Griffin PR. HDX-MS reveals structural determinants for RORγ hyperactivation by synthetic agonists.  Elife. 2019 Jun 7;8; PMCID PMC6579513

Law YS, Utt A, Tan YB, Zheng J, Wang S, Chen MW, Griffin PR, Merits A, Luo D.  Structural insights into RNA recognition by the Chikungunya virus nsP2 helicase.  Proc Natl Acad Sci U S A. 2019 May 7;116(19):9558-9567. PMCID: PMC6511008.

Chang MR, Ciesla A, Strutzenberg TS, Novick SJ, He Y, Garcia-Ordonez R, Frkic RL, Bruning JB, Kamenecka TM, Griffin PR.  A unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem Biol. 2019 Apr 5 [Epub ahead of print].

Doebelin C, He Y, Campbell S, Nuhant P, Kumar N, Koenig M, Garcia-Ordonez R, Chang MR, Roush WR, Lin L, Kahn S, Cameron MD, Griffin PR, Solt LA, Kamenecka TM.  Discovery and optimization of a series of sulfonamide inverse agonists for the retinoic acid receptor-related receptor-α.  Med Chem. 2019 Feb 22 [Epub ahead of print].

Baillargeon P, Fernandez-Vega V, Sridharan BP, Brown S, Griffin PR, Rosen H, Cravatt B, Scampavia L, Spicer TP.  The Scripps Molecular Screening Center and Translational Research Institute. SLAS Discov. 2019 Mar;24(3):386-397.

Mosure SA, Shang J, Eberhardt J, Brust R, Zheng J, Griffin PR, Forli S, Kojetin DJ.  Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPARγ Drug Pioglitazone.  J Med Chem. 2019 Feb 28;62(4):2008-2023.

Longbotham JE, Chio CM, Dharmarajan V, Trnka MJ, Torres IO, Goswami D, Ruiz K, Burlingame AL, Griffin PR, Fujimori DG.  Histone H3 binding to the PHD1 domain of histone demethylase KDM5A enables active site remodeling.  Nat Commun. 2019 Jan 9;10(1):94.

Zheng J, Wang C, Chang MR, Devarkar SC, Schweibenz B, Crynen GC, Garcia-Ordonez RD, Pascal BD, Novick SJ, Patel SS, Marcotrigiano J, Griffin PR. HDX-MS reveals dysregulated checkpoints that compromise discrimination against self RNA during RIG-I mediated autoimmunity. Nature Commun. 2018 Dec 18;9(1):5366.

Fanning SW, Jeselsohn R, Dharmarajan V, Mayne CG, Karimi M, Buchwalter G, Houtman R, Toy W, Fowler CE, Han R, Lainé M, Carlson KE, Martin TA, Nowak J, Nwachukwu JC, Hosfield DJ, Chandarlapaty S, Tajkhorshid E, Nettles KW, Griffin PR, Shen Y, Katzenellenbogen JA, Brown M, Greene GL. The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells.   Elife. 2018 Nov 29;7.

Patil DN, Rangarajan ES, Novick SJ, Pascal BD, Kojetin DJ, Griffin PR, Izard T, Martemyanov KA. Structural organization of a major neuronal G protein regulator, the RGS7-Gβ5-R7BP complex.   Elife. 2018 Dec 12;7.

Kim H, Wrann CD, Jedrychowski M, Vidoni S, Kitase Y, Nagano K, Zhou C, Chou J, Parkman VA, Novick SJ, Strutzenberg TS, Pascal BD, Le PT, Brooks DJ, Roche AM, Gerber KK, Mattheis L, Chen W, Tu H, Bouxsein ML, Griffin PR, Baron R, Rosen CJ, Bonewald LF, Spiegelman BM.  Irisin Mediates Effects on Bone and Fat via αV Integrin Receptors.  Cell. 2018 Dec 13;175(7):1756-1768.e17.

Yan Y, Zhou XE, Novick SJ, Shaw SJ, Li Y, Brunzelle JS, Hitoshi Y, Griffin PR, Xu HE, Melcher K. Structures of AMP-activated protein kinase bound to novel pharmacological activators in phosphorylated, non-phosphorylated, and nucleotide-free states.   J Biol Chem. 2018 Nov 26. pii: jbc.RA118.004883.

de Vera IMS, Munoz-Tello P, Zheng J, Dharmarajan V, Marciano DP, Matta-Camacho E, Giri PK, Shang J, Hughes TS, Rance M, Griffin PR, Kojetin DJ.Defining a Canonical Ligand-Binding Pocket in the Orphan Nuclear Receptor Nurr1.   Structure. 2018 Oct 25.

Brust R, Shang J, Fuhrmann J, Mosure SA, Bass J, Cano A, Heidari Z, Chrisman IM, Nemetchek MD, Blayo AL, Griffin PR, Kamenecka TM, Hughes TS, Kojetin DJ. A structural mechanism for directing corepressor-selective inverse agonism of PPARγ.   Nat Commun. 2018 Nov 8;9(1):4687.

Zheng J, Corzo C, Chang MR, Shang J, Lam VQ, Brust R, Blayo AL, Bruning JB, Kamenecka TM, Kojetin DJ, Griffin PR. Chemical Crosslinking Mass Spectrometry Reveals the Conformational Landscape of the Activation Helix of PPARγ; a Model for Ligand-Dependent Antagonism.  Structure. 2018, S0969-2126(18)30253-3.

Zhang C, Konermann S, Brideau NJ, Lotfy P, Wu X, Novick SJ, Strutzenberg T, Griffin PR, Hsu PD, Lyumkis D. Structural Basis for the RNA-Guided Ribonuclease Activity of CRISPR-Cas13d.  Cell. 2018, 175(1):212-223.e17.

Evans PR, Gerber KJ, Dammer EB, Duong DM, Goswami D, Lustberg DJ, Zou J, Yang JJ, Dudek SM, Griffin PR, Seyfried NT, Hepler JR. Interactome Analysis Reveals Regulator of G Protein Signaling 14 (RGS14) is a Novel Calcium/Calmodulin (Ca2+/CaM) and CaM Kinase II (CaMKII) Binding Partner.   J Proteome Res. 2018 Apr 6;17(4):1700-1711.

Lin H, Long JZ, Roche AM, Svensson KJ, Dou FY, Chang MR, Strutzenberg T, Ruiz C, Cameron MD, Novick SJ, Berdan CA, Louie SM, Nomura DK, Spiegelman BM, Griffin PR, Kamenecka TM. Discovery of Hydrolysis-Resistant Isoindoline N-Acyl Amino Acid Analogues that Stimulate Mitochondrial Respiration.   J Med Chem. 2018, 61(7):3224-3230.

Patouret R, Doebelin C, Garcia-Ordonez RD, Chang MR, Ruiz C, Cameron MD, Griffin PR, Kamenecka TM. Identification of an aminothiazole series of RORβ modulators.   Bioorg Med Chem Lett. 2018, 28:1178-1181.

Lin H, Doebelin C, Patouret R, Garcia-Ordonez RD, Chang MR, Dharmarajan V, Bayona CR, Cameron MD, Griffin PR, Kamenecka TM.  Design, synthesis, and evaluation of simple phenol amides as ERRγ agonists.  Bioorg Med Chem Lett. 2018, 28:1313-1319.

Schleussner N, Merkel O, Costanza M, Liang HC, Hummel F, Romagnani C, Durek P, Anagnostopoulos I, Hummel M, Jöhrens K, Niedobitek A, Griffin PR, Piva R, Sczakiel HL, Woessmann W, Damm-Welk C, Hinze C, Stoiber D, Gillissen B, Turner SD, Kaergel E, von Hoff L, Grau M, Lenz G, Dörken B, Scheidereit C, Kenner L, Janz M, Mathas S. The AP-1-BATF and -BATF3 module is essential for growth, survival and TH17/ILC3 skewing of anaplastic large cell lymphoma.   Leukemia. 2018, 32:1994-2007.

Cherian MT, Chai SC, Wright WC, Singh A, Alexandra Casal M, Zheng J, Wu J, Lee RE, Griffin PR, Chen T. CINPA1 binds directly to constitutive androstane receptor and inhibits its activity.   Biochem Pharmacol. 2018,152:211-223.

Chinthalapudi K, Mandati V, Zheng J, Sharff AJ, Bricogne G, Griffin PR, Kissil J, Izard T.  Lipid binding promotes the open conformation and tumor-suppressive activity of neurofibromin 2.  Nat Commun. 2018, 6;9(1):1338.

Chrisman IM, Nemetchek MD, de Vera IMS, Shang J, Heidari Z, Long Y, Reyes-Caballero H, Galindo-Murillo R, Cheatham TE 3rd, Blayo AL, Shin Y, Fuhrmann J, Griffin PR, Kamenecka TM, Kojetin DJ, Hughes TS.Defining a conformational ensemble that directs activation of PPARγ.    Nat Commun. 2018, 9:1794.

Long JZ, Roche AM, Berdan CA, Louie SM, Roberts AJ, Svensson KJ, Dou FY, Bateman LA, Mina AI, Deng Z, Jedrychowski MP, Lin H, Kamenecka TM, Asara JM, Griffin PR, Banks AS, Nomura DK, Spiegelman BM.Ablation of PM20D1 reveals N-acyl amino acid control of metabolism and nociception.    Proc Natl Acad Sci U S A. 2018, 115:E6937-E6945.

Bandyopadhyay A, Van Eps N, Eger BT, Rauscher S, Yedidi RS, Moroni T, West GM, Robinson KA, Griffin PR, Mitchell J, Ernst OP.   A Novel Polar Core and Weakly Fixed C-Tail in Squid Arrestin Provide New Insight into Interaction with Rhodopsin. J Mol Biol. 2018, 430:4102-4118.

Frkic RL, Marshall AC, Blayo AL, Pukala TL, Kamenecka TM, Griffin PR, Bruning JB.  PPARγ in Complex with an Antagonist and Inverse Agonist: a Tumble and Trap Mechanism of the Activation Helix.   iScience. 2018, 5:69-79.

Spicer TP, Gardiner DL, Schoenen FJ, Roy S, Griffin PR, Chase P, Scampavia L, Hodder P, Trenholme KR. Identification of Antimalarial Inhibitors Using Late-Stage Gametocytes in a Phenotypic Live/Dead Assay.   SLAS Discov. 2018, Aug 24:2472555218796410.

Doebelin C, Patouret R, Garcia-Ordonez RD, Chang MR, Dharmarajan V, Novick S, Ciesla A, Campbell S, Solt LA, Griffin PR, Kamenecka TM.  Identification of potent RORβ modulators: Scaffold variation.   Bioorg Med Chem Lett. 2018, 28:3210-3215.

Kurumbail RG, West GM, Dharmarajan V, Borzilleri KA, Withka JM, Ward J, Reyes AR, Rajamohan F, Griffin PR, Calabrese MF. Biophysical Interactions of Direct AMPK Activators.  Methods Mol Biol. 2018; 1732:29-55.

Khandekar MJ, Banks AS, Laznik-Bogoslavski D, White JP, Choi JH, Kazak L, Lo JC, Cohen P, Wong KK, Kamenecka TM, Griffin PR, Spiegelman BM. Noncanonical agonist PPARγ ligands modulate the response to DNA damage and sensitize cancer cells to cytotoxic chemotherapy.   Proc Natl Acad Sci U S A. 2018, 115(3):561-566.

Pettersson-Klein AT, Izadi M, Ferreira DMS, Cervenka I, Correia JC, Martinez-Redondo V, Southern M, Cameron M, Kamenecka T, Agudelo LZ, Porsmyr-Palmertz M, Martens U, Lundgren B, Otrocka M, Jenmalm-Jensen A, Griffin PR, Ruas JL. Small molecule PGC-1α1 protein stabilizers induce adipocyte Ucp1 expression and uncoupled mitochondrial respiration.   Mol Metab. 2018, 9:28-42.

Francis JW, Goswami D, Novick SJ, Pascal BD, Weikum ER, Ortlund EA, Griffin PR, Kahn RA.Nucleotide binding to ARL2 in the TBCD∙ARL2∙β-tubulin complex drives conformational changes in β-tubulin.    J Mol Biol. 2017, 429(23):3696-3716.

Lam V, Zheng J, Griffin PR. Unique interactome network signatures for PPARγ Modulation by functional selective ligands.  Mol Cell Proteomics. 2017, 16, 2098-2110.

Zheng J, Chang MR, Stites RE, Wang Y, Bruning JB, Pascal BD, Novick SJ, Garcia-Ordonez RD, Stayrook KR, Chalmers MJ, Dodge JA, Griffin PR, HDX reveals the conformational dynamics of DNA sequence specific VDR co-activator interactions.  Nat Commun. 2017, 8:923.

Lin W, Wang YM, Chai SC, Lv L, Zheng J, Wu J, Zhang Q, Wang YD, Griffin PR, Chen T. SPA70 is a potent antagonist of human pregnane X receptor.   Nat Commun. 2017 8:741.

deVera IMS, Zheng J, Novick S, Shang J, Hughes TS, Brust R, Munoz-Tello P, Gardner WJ Jr, Marciano DP, Kong X, Griffin PR, Kojetin DJ.  Synergistic Regulation of Coregulator/Nuclear Receptor Interaction by Ligand and DNA.   Structure 2017 Aug 23. Pii: S0969-2126(17)30253-8.

Zhou XE, He Y, deWaal PW, Gao X, Kang Y, Van Eps N, Yin Y, Pal K, Goswami D, White TA, Barty A, Latorraca NR, Chapman HN, Hubbell WL, Dror RO, Stevens RC, Cherezov V, Gurevich VV, Griffin PR, Ernst OP, Melcher K, Xu HE.  Identification of Phosphorylation Codes for Arrestin Recruitment by G. Protein-Coupled Receptors.  Cell 2017 Jul 27;170(3):457-469.

Frkic RL, He Y, Rodriguez BB, Chang MR, Kuruvilla D, Ciesla A, Abell AD, Kamenecka TM, Griffin PR, Bruning JB. Structure-Activity Relationship of 2,4-Dichloro-N-(3,5-dichloro-4-(quinolin-3-yloxy)phenyl)benzenesulfonamide (INT131) Analogs for PPARγ-Targeted Antidiabetics.   J Med Chem., 2017, 60, 4584-4593.

Zhang X, Zhao F, Wu Y, Yang J, Han GW, Zhao S, Ishchenko A, Ye L, Lin X, Ding K, Dharmarajan V, Griffin PR, Gati C, Nelson G, Hunter MS, Hanson MA, Cherezov V, Stevens RC, Tan W, Tao H, Xu F. Crystal structure of a multi-domain human smoothened receptor in complex with a super stabilizing ligand.  Nat Commun. 2017 May 17;8:15383.

Zhang H, Qiao A, Yang D, Yang L, Dai A, de Graaf C, Reedtz-Runge S, Dharmarajan V, Zhang H, Han GW, Grant TD, Sierra RG, Weierstall U, Nelson G, Liu W, Wu Y, Ma L, Cai X, Lin G, Wu X, Geng Z, Dong Y, Song G, Griffin PR, Lau J, Cherezov V, Yang H, Hanson MA, Stevens RC, Zhao Q, Jiang H, Wang MW, Wu B. Structure of the full-length glucagon class B G-protein-coupled receptor.  Nature. 2017, 546, 259-264.

Pal K, Bandyopadhyay A, Zhou XE, Xu Q, Marciano DP, Brunzelle JS, Yerrum S, Griffin PR, Vande Woude G, Melcher K, Xu HE. Structural Basis of TPR-Mediated Oligomerization and Activation of Oncogenic Fusion Kinases.  Structure. 2017, 25, 867-877.

Gu X, Yan Y, Novick SJ, Kovich A, Goswami D, Ke J, Tan MHE, Wang L, Li X, de Waal P, Webb MR, Griffin PR, Xu HE, Melcher K. Deconvoluting AMP-dependent kinase (AMPK) adenine nucleotide binding and sensing.  J Biol Chem. 2017 Jun 14. pii: jbc.M117.793018.

Mays SG, Okafor CD, Tuntland ML, Whitby RJ, Dharmarajan V, Stec J, Griffin PR, Ortlund EA. Structure and Dynamics of the Liver Receptor Homolog 1-PGC1α Complex.  Mol Pharmacol. 2017 Mar 31. pii: mol.117.108514

Sturchler E, Li X, de Lourdes Ladino M, Kaczanowska K, Cameron M, Griffin PR, Finn MG, Markou A, McDonald P.GABAB receptor allosteric modulators exhibit pathway-dependent and species-selective activity.   Pharmacol Res Perspect. 2017 Mar 24;5(2):e00288.

Sharabi K, Lin H, Tavares CD, Dominy JE, Camporez JP, Perry RJ, Schilling R, Rines AK, Lee J, Hickey M, Bennion M, Palmer M, Nag PP, Bittker JA, Perez J, Jedrychowski MP, Ozcan U, Gygi SP, Kamenecka TM, Shulman GI, Schreiber SL, Griffin PR, Puigserver P.  Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes. Cell. 2017, 169, 148-160.

Darrah E, Kim A, Zhang X, Boronina T, Cole RN, Fava A, Giles JT, Iii CO, Chalmers MJ, Griffin PR, Sadegh-Nasseri S, Rosen A. Proteolysis by Granzyme B Enhances Presentation of Autoantigenic Peptidylarginine Deiminase 4 Epitopes in Rheumatoid Arthritis.  J Proteome Res. 2017, 16, 355-365.

Srinivasan S, Nwachukwu JC, Bruno NE, Dharmarajan V, Goswami D, Kastrati I, Novick S, Nowak J, Cavett V, Zhou HB, Boonmuen N, Zhao Y, Min J, Frasor J, Katzenellenbogen BS, Griffin PR, Katzenellenbogen JA, Nettles KW. Full antagonism of the estrogen receptor without a prototypical ligand side chain.   Nat Chem Biol. 2017 Jan;13(1):111-118.

Jin Z, Lin H, Srinivasan S, Nwachukwu JC, Bruno N, Griffin PR, Nettles KW, Kamenecka TM.Synthesis of novel steroidal agonists, partial agonists, and antagonists for the glucocorticoid receptor  Bioorg Med Chem Lett. 2017 Jan 15;27(2):347-353.

Mays SG, Okafor CD, Whitby RJ, Goswami D, Stec J, Flynn AR, Dugan MC, Jui NT, Griffin PR, Ortlund EA. Crystal Structures of the Nuclear Receptor, Liver Receptor Homolog 1, Bound to Synthetic Agonists.  J Biol Chem. 2016, 291, 25281-25291.

Doebelin C, Patouret R, Garcia-Ordonez RD, Chang MR, Dharmarajan V, Kuruvilla DS, Novick SJ, Lin L, Cameron MD, Griffin PR, Kamenecka TM. N-Arylsulfonyl Indolines as Retinoic Acid Receptor-Related Orphan Receptor γ (RORγ) Agonists. ChemMedChem. 2016 Dec 6;11(23):2607-2620.

Saltzberg DJ, Broughton HB, Pellarin R, Chalmers MJ, Espada A, Dodge JA, Pascal BD, Griffin PR, Humblet C, Sali A. A Residue Resolved Bayesian Approach to Quantitative Interpretation of Hydrogen Deuterium Exchange from Mass Spectrometry: Application to Characterizing Protein-Ligand Interactions. J Phys Chem B. 2016 Nov 3.

Long JZ, Svensson KJ, Bateman LA, Lin H, Kamenecka T, Lokurkar IA, Lou J, Rao RR, Chang MR, Jedrychowski MP, Paulo JA, Gygi SP, Griffin PR, Nomura DK, Spiegelman BM. The Secreted Enzyme PM20D1 Regulates Lipidated Amino Acid Uncouplers of Mitochondria. Cell. 2016 Jul 14;166(2):424-35.

Mo Z, Zhang Q, Liu Z, Lauer J, Shi Y, Sun L, Griffin PR, Yang XL. Neddylation requires glycyl-tRNA synthetase to protect activated E2.  Nat Struct Mol Biol. 2016 Aug;23(8):730-737. doi: 10.1038/nsmb.3250. Epub 2016 Jun 27. PMID: 27348078.

Cummins DJ, Espada A, Novick SJ, Molina-Martin M, Stites RE, Espinosa JF, Broughton H, Goswami D, Pascal BD, Dodge JA, Chalmers MJ, Griffin PR. Two-Site Evaluation of the Repeatability and Precision of an Automated Dual-Column Hydrogen/Deuterium Exchange Mass Spectrometry Platform.  Anal Chem. 2016 Jun 21;88(12):6607-14. PMID: 27224086.

Tavares CD, Sharabi K, Dominy JE, Lee Y, Isasa M, Orozco JM, Jedrychowski MP, Kamenecka TM, Griffin PR, Gygi SP, Puigserver P. The Methionine Transamination Pathway Controls Hepatic Glucose Metabolism through Regulation of the GCN5 Acetyltransferase and the PGC-1α Transcriptional Coactivator.  J Biol Chem. 2016 May 13;291(20):10635-45. PMCID: PMC4865912.

Fanning SW, Mayne CG, Dharmarajan V, Carlson KE, Martin TA, Novick SJ, Toy W, Green B, Panchamukhi S, Katzenellenbogen BS, Tajkhorshid E, Griffin PR, Shen Y, Chandarlapaty S, Katzenellenbogen JA, Greene GL.   Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation. Elife. 2016 Feb 2;5. pii: e12792. PMCID: PMC4821807.

He W, Bai G, Zhou H, Wei N, White NM, Lauer J, Liu H, Shi Y, Dan Dumitru C, Lettieri K, Shubayev V, Jordanova A, Guergueltcheva V, Griffin PR, Burgess RW, Pfaff SL, Yang XL. Corrigendum: CMT2D neuropathy is linked to the neomorphic binding activity of glycyl-tRNA synthetase. Nature. 2016 Jan 20.  [Epub ahead of print]

Chang MR, Dharmarajan V, Doebelin C, Garcia-Ordonez RD, Novick SJ, Kuruvilla DS, Kamenecka TM, Griffin PR. Synthetic RORγt Agonists Enhance Protective Immunity. ACS Chem Biol. 2016 Jan 25. [Epub ahead of print]

Srinivasan S, Dharmarajan V, Reed DK, Griffin PR, Schmid SL. Identification and function of conformational dynamics in the multidomain GTPase dynamin. EMBO J. 2016 Jan 18. pii: e201593477. [Epub ahead of print]

van Marrewijk LM, Polyak SW, Hijnen M, Kuruvilla D, Chang MR, Shin Y, Kamenecka TM, Griffin PR, Bruning JB.  SR2067 Reveals a Unique Kinetic and Structural Signature for PPARy Partial Agonism. ACS Chem Biol. 2016 Jan 15;11(1):273-83.

Choi S, Kim ES, Jung JE, Marciano DP, Jo A, Koo JY, Choi SY, Yang YR, Jang HJ, Kim EK, Park J, Kwon HM, Lee IH, Park SB, Myung KJ, Suh PG, Griffin PR, Choi JH. PPARγ antagonist Gleevec improves insulin sensitivity and promotes the browning of white adipose tissue. Diabetes. 2016, Jan 6. pii: db151382. [Epub ahead of print]

Zhang H, Sturchler E, Zhu J, Nieto A, Cistrone PA, Xie J, He L, Yea K, Jones T, Turn R, Di Stefano PS, Griffin PR, Dawson PE, McDonald PH, Lerner RA.  Autocrine selection of a GLP-1R G-protein biased agonist with potent antidiabetic effects.  Nat Commun. 2015, Dec 1;6:8918. PMID: 26621478

He W, Bai G, Zhou H, Wei N, White NM, Lauer J, Liu H, Shi Y, Dumitru CD, Lettieri K, Shubayev V, Jordanova A, Guergueltcheva V, Griffin PR, Burgess RW, Pfaff SL, Yang XL.  CMT2D neuropathy is linked to the neomorphic binding activity of flycyl-tRNA synthetase. Nature. 2015 Oct 29;526(7575):710-4.  PMID: 26503042

Zhao LH, Zhou XE, Yi W, Wu Z, Liu Y, Kang Y, Hou L, de Waal PW, Li S, Jiang Y, Scaffidi A, Flematti GR, Smith SM, Lam VQ, Griffin PR, Wang Y, Li J, Melcher K, Xu HE. Destabilizatin of strigolactone receptor DWARF14 by binding of ligand and E3-ligase signaling effector DWARF3. Cell Res. 2015 Nov;25(11):1219-36.  PMID: 26470846

Marciano DP, Kuruvilla DS, Pascal BD, Griffin PR. Identification of Bexarotene as a PPARγ Antagonist with HDX. PPAR Res. 2015;  2015:254560. Epub 2015 Sep 15.  PMID: 26451138

Mari Y, West GM, Scharager-Tapia C, Pascal BD, Garcia-Ordonez RD, Griffin PR. SERBP1 Is a Component of the Liver Receptor Homologue-1 Transcriptional Complex. J Proteome Res. 2015 Nov 6;14(11):4571-80. PMID: 26398198

Asteian A, Blayo AL, He Y, Koenig M, Shin Y, Kuruvilla DS, Corzo CA, Cameron MD, Lin L, Ruiz C, Khan S, Kumar N, Busby S, Marciano DP, Garcia-Ordonez RD, Griffin PR, Kamenecka TM. Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists.  ACS Med Chem Lett. 2015 Aug 4;6(9):998-1003.  PMID: 26396687

Kojetin DJ, Matta-Camacho E, Hughes TS, Srinivasan S, Nwachukwu JC, Cavett V, Nowak J, Chalmers MJ, Marciano DP, Kamenecka TM, Shulman AI, Rance M, Griffin PR, Bruning JB, Nettles KW. Structural mechanism for signal transduction in RXR nuclear receptor heterodimers.  Nat Commun. 2015 6:8013.  PMID: 26289479

Peng Y, Zeng W, Ye H, Han KH, Dharmarajan V, Novick S, Wilson IA, Griffin PR, Friedman JM, Lerner RA. A General Method for Insertion of Functional Proteins within Proteins via Combinatorial Selection of Permissive Junctions. Chem Biol. 2015 Aug 20;22(8):1134-43  PMID: 26278185

Pascal BD, West GM, Scharager-Tapia C, Flefil R, Moroni T, Martinez-Acedo P, Griffin PR, Carvalloza AC. Software Analysis of Uncorrelated MS1 Peaks for Discovery of Post-Translational Modifications. J Am Soc Mass Spectrom. 2015 Aug 12. [Epub ahead of print] PMID:26265041

Zhang F, Yao J, Ke J, Zhang L, Lam VQ, Xin XF, Zhou XE, Chen J, Brunzelle J, Griffin PR, Zhou M, Xu HE, Melcher K, He SY. Structural basis of JAZ repression of MYC transcription factors in jasmonate signalling. Nature. 2015 Sep 10;525(7568):269-73.  PMID: 26258305

Yang L, Yang D, de Graaf C, Moeller A, West GM, Dharmarajan V, Wang C, Siu FY, Song G, Reedtz-Runge S, Pascal BD, Wu B, Potter CS, Zhou H, Griffin PR, Carragher B, Yang H, Wang MW, Stevens RC, Jiang H. Conformational states of the full-length glucagon receptor. Nat Commun. 2015 Jul 31;6:7859. PMID: 26227798

Kang Y, Zhou XE, Gao X, He Y, Liu W, Ishchenko A, Barty A, White TA, Yefanov O, Han GW, Xu Q, de Waal PW, Ke J, Tan MH, Zhang C, Moeller A, West GM, Pascal BD, Van Eps N, Caro LN, Vishnivetskiy SA, Lee RJ, Suino-Powell KM, Gu X, Pal K, Ma J, Zhi X, Boutet S, Williams GJ, Messerschmidt M, Gati C, Zatsepin NA, Wang D, James D, Basu S, Roy-Chowdhury S, Conrad CE, Coe J, Liu H, Lisova S, Kupitz C, Grotjohann I, Fromme R, Jiang Y, Tan M, Yang H, Li J, Wang M, Zheng Z, Li D, Howe N, Zhao Y, Standfuss J, Diederichs K, Dong Y, Potter CS, Carragher B, Caffrey M, Jiang H, Chapman HN, Spence JC, Fromme P, Weierstall U, Ernst OP, Katritch V, Gurevich VV, Griffin PR, Hubbell WL, Stevens RC, Cherezov V, Melcher K, Xu HE. Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser. Nature. 2015 Jul 30;523(7562):561-7.  Epub 2015 Jul 22. PMID:26200343

Marciano DP, Kuruvilla DS, Boregowda SV, Asteian A, Hughes TS, Garcia-Ordonez R, Corzo CA, Khan TM, Novick SJ, Park H, Kojetin DJ, Phinney DG, Bruning JB, Kamenecka TM, Griffin PR. Pharmacological repression of PPARγ promotes osteogenesis, Nat Commun. 2015 Jun 12;6:7443.  PMID: 26068133

Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, Palmer M, Shamji AF, Wawer MJ, McManus O, Wu M, Zou B, Yu H, Golden JE, Schoenen FJ, Simeonov A, Jadhav A, Jackson MR, Pinkerton AB, Chung TD, Griffin PR, Cravatt BF, Hodder PS, Roush WR, Roberts E, Chung DH, Jonsson CB, Noah JW, Severson WE, Ananthan S, Edwards B, Oprea TI, Conn PJ, Hopkins CR, Wood MR, Stauffer SR, Emmitte KA; NIH Molecular Libraries Project Team. Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes. Cell, 2015, Jun 4;161(6):1252-65. Review.  PMID: 26046436

Chang MR, He Y, Khan TM, Kuruvilla DS, Garcia-Ordonez R, Corzo CA, Unger TJ, White DW, Khan S, Lin L, Cameron MD, Kamenecka TM, Griffin PR. Antiobesity Effect of a Small Molecule Repressor of RORγ.  Mol Pharmacol., 2015,Jul;88(1):48-56. PMID: 25904554

Goswami D, Tuske S, Pascal BD, Bauman, JD, Patel D, Arnold E, Griffin PR. Differential isotopic enrichment to facilitate characterization of asymmetric multimeric proteins using hydrogen/deuterium exchange mass spectrometry. Anal Chem., 2015, Apr 7;87(7):4015-22. PMID: 25763479

Brown NE, Goswami D, Branch MR, Ramineni S, Ortlund EA, Griffin PR, Hepler JR. Integration of G protein α (Gα) signaling by the regulator of G protein signaling 14 (RGS14). J Biol Chem. 2015, Apr 3;290(14):9037-49. PMID: 25666614

Corzo C, Mari Y, Chang MR, Kuruvilla D, Nuhant P, Kumar N, West GM, Duckett DR, Roush WR, Griffin PR. Anti-proliferation Activity of a Small Molecule Repressor of LRH-1. Mol Pharmacol. 2015, Feb;87(2):296-304. PMID: 25473120

Marciano DP, Dharmarajan V, Griffin PR. HDX-MS guided drug discovery: small molecules and biopharmaceuticals. Curr Opin Struct Biol. 2014, Oct;28:105-11. Review. PMID: 25179005

Shkriabai N, Dharmarajan V, Slaughter A, Kessl JJ, Larue RC, Feng L, Fuchs JR, Griffin PR, Kvaratskhelia M. A critical role of the C-terminal segment for allosteric inhibitor-induced aberrant multimerization of HIV-1 integrase. J Biol Chem. 2014 Sep 19;289(38):26430-40. Epub 2014 Aug 12. PMID: 25118283

Cameron M, Kamenecka T, Madoux F, Chase P, Roush W, Hodder P, Griffin PR. ML368 Identification of Imidazopyridines as Selective Inhibitors of the Cytochrome P450 Enzyme CYP3A4. Probe Reports from the NIH Molecular Libraries Program [Internet].
Bethesda (MD): National Center for Biotechnology Information (US); 2010-2013 Apr 15 [updated 2014 Sep 18]. PMID: 24479199

West GM, Willard FS, Sloop KW, Showalter AD, Pascal BD, Griffin PR. Glucagon-like peptide-1 receptor ligand interactions: structural cross talk between ligands and the extracellular domain. PLoS One. 2014 Sep 2;9(9):e105683. eCollection 2014. PMID: 25180755

Carson MW, Zhang J, Chalmers MJ, Bocchinfuso WP, Holifield KD, Masquelin T, Stites RE, Stayrook KR, Griffin PR, Dodge JA. HDX reveals unique fragment ligands for the vitamin D receptor. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3459-63. Epub 2014 May 29. PMID: 24974344

Goswami D, Callaway C, Pascal BD, Kumar R, Edwards DP, Griffin PR. Influence of domain interactions on conformational mobility of the progesterone receptor detected by hydrogen/deuterium exchange mass spectrometry. Structure. 2014 Jul 8;22(7):961-73. Epub 2014 Jun 5. PMID: 24909783

Kirschke E, Goswami D, Southworth D, Griffin PR, Agard DA. Glucocorticoid receptor function regulated by coordinated action of the Hsp90 and Hsp70 chaperone cycles. Cell. 2014 Jun 19;157(7):1685-97. PMID: 24949977

Armstrong EH, Goswami D, Griffin PR, Noy N, Ortlund EA. Structural basis for ligand regulation of the fatty acid-binding protein 5, peroxisome proliferator-activated receptor β/δ (FABP5-PPARβ/δ) signaling pathway. J Biol Chem. 2014 May 23;289(21):14941-54. Epub 2014 Apr 1. PMID: 24692551

Nwachukwu JC, Srinivasan S, Bruno NE, Parent AA, Hughes TS, Pollock JA, Gjyshi O, Cavett V, Nowak J, Garcia-Ordonez RD, Houtman R, Griffin PR, Kojetin DJ, Katzenellenbogen JA, Conkright MD, Nettles KW. Resveratrol modulates the inflammatory response via an estrogen receptor-signal integration network. Elife. 2014 Apr 25;3:e02057. PMID: 24771768

Yan F, Yu Y, Chow DC, Palzkill T, Madoux F, Hodder P, Chase P, Griffin PR, O'Malley BW, Lonard DM. Identification of verrucarin a as a potent and selective steroid receptor coactivator-3 small molecule inhibitor. PLoS One. 2014 Apr 17;9(4):e95243. eCollection
2014. PMID: 24743578

Hughes TS, Giri PK, de Vera IM, Marciano DP, Kuruvilla DS, Shin Y, Blayo AL, Kamenecka TM, Burris TP, Griffin PR, Kojetin DJ. An alternate binding site for PPARγ ligands. Nat Commun. 2014 Apr 7;5:3571. PMID: 24705063

Qiang G, Xue S, Yang JJ, Du G, Pang X, Li X, Goswami D, Griffin PR, Ortlund EA, Chan CB, Ye K. Identification of a small molecular insulin receptor agonist with potent antidiabetes activity. Diabetes. 2014 Apr;63(4):1394-409. PMID: 24651808

Underbakke ES, Iavarone AT, Chalmers MJ, Pascal BD, Novick S, Griffin PR, Marletta MA. Nitric oxide-induced conformational changes in soluble guanylate cyclase. Structure. 2014 Apr 8;22(4):602-11. Epub 2014 Feb 20. PMID: 24560804

Chang MR, Lyda B, Kamenecka TM, Griffin PR. Pharmacologic repression of retinoic acid receptor-related orphan nuclear receptor γ is therapeutic in the collagen-induced arthritis experimental model. Arthritis Rheumatol. 2014 Mar;66(3):579-88. PMID: 24574218

Wang Y, Lonard DM, Yu Y, Chow DC, Palzkill TG, Wang J, Qi R, Matzuk AJ, Song X, Madoux F, Hodder P, Chase P, Griffin PR, Zhou S, Liao L, Xu J, O'Malley BW. Bufalin is a potent small-molecule inhibitor of the steroid receptor coactivators SRC-3 and SRC-1. Cancer Res. 2014 Mar 1;74(5):1506-17. Epub 2014 Jan 3. PMID: 24390736

Lewallen DM, Sreelatha A, Dharmarajan V, Madoux F, Chase P, Griffin PR, Orth K, Hodder P, Thompson PR. Inhibiting AMPylation: a novel screen to identify the first small molecule inhibitors of protein AMPylation. ACS Chem Biol. 2014 Feb 21;9(2):433-42. Epub 2013 Nov 25. PMID: 24274060

Marciano DP, Chang MR, Corzo CA, Goswami D, Lam VQ, Pascal BD, Griffin PR. The therapeutic potential of nuclear receptor modulators for treatment of metabolic disorders: PPARγ, RORs, and Rev-erbs. Cell Metab. 2014 Feb 4;19(2):193-208. Epub 2014 Jan 16. Review. PMID: 24440037

Boerma LJ, Xia G, Qui C, Cox BD, Chalmers MJ, Smith CD, Lobo-Ruppert S, Griffin PR, Muccio DD, Renfrow MB. Defining the communication between agonist and coactivator binding in the retinoid Xreceptor α ligand binding domain. J Biol Chem. 2014 Jan 10;289(2):814-26. Epub 2013 Nov 1. PMID: 24187139

Chang MR, Rosen H, Griffin PR. RORs in autoimmune disease. Curr Top Microbiol Immunol. 2014; 378:171-82. Review. PMID: 24728598

Corzo C, Griffin PR. Targeting the Peroxisome Proliferator-Activated Receptor-γ to Counter the Inflammatory Milieu in Obesity. Diabetes Metab J. 2013 Dec;37(6):395-403. PMID: 24404510

Zhang Y, Goswami D, Wang D, Wang TS, Sen S, Magliery TJ, Griffin PR, Wang F, Schultz PG. An antibody with a variable-region coiled-coil "knob" domain. Angew Chem Int Ed Engl. 2014 Jan 3;53(1):132-5. Epub 2013 Nov 19. PMID: 24254636

Landgraf RR, Goswami D, Rajamohan F, Harris MS, Calabrese MF, Hoth LR, Magyar R, Pascal BD, Chalmers MJ, Busby SA, Kurumbail RG, Griffin PR. Activation of AMP-activated protein kinase revealed by hydrogen/deuterium exchange mass spectrometry. Structure. 2013 Nov 5;21(11):1942-53. Epub 2013 Sep 26. PMID: 24076403

Goswami D, Devarakonda S, Chalmers MJ, Pascal BD, Spiegelman BM, Griffin PR. Time window expansion for HDX analysis of an intrinsically disordered protein. J Am Soc Mass Spectrom. 2013 Oct 24(10):1584-92. Epub 2013 Jul 25. PMID: 23884631

Musille PM, Pathak M, Lauer JL, Griffin PR, Ortlund EA. Divergent sequence tunes ligand sensitivity in phospholipid-regulated hormone receptors. J Biol Chem. 2013 Jul 12;288(28):20702-12. Epub 2013 Jun 4. PMID:23737522

Kumar R, Moure CM, Khan SH, Callaway C, GrimmSL, Goswami D, Griffin PR, Edwards DP. Regulation of the structurally dynamic N-terminal domain of progesterone receptor by protein-induced folding. J Biol Chem. 2013 Oct 18;288(42):30285-99. Epub 2013 Aug 30. PMID: 23995840

Harms MJ, Eick GN, Goswami D, Colucci JK, Griffin PR, Ortlund EA, Thornton JW. Biophysical mechanisms for large-effect mutations in the evolution of steroid hormone receptors. Proc Natl Acad Sci U S A. 2013 Jul 9;110(28):11475-80. Epub 2013 Jun 24. PMID: 23798447

Kumar N, Kamenecka T, Lyda B, Khan P, Chang MR, Garcia-Ordonez RD, Cameron M, Ferguson J, Mercer BA, Hodder P, Rosen H, Griffin PR. Identification of a novel selective inverse agonist probe and analogs for the Retinoic acid receptor-related Orphan Receptor Gamma (RORγ). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.2012 Apr 16 [updated 2013 Mar 14]. PMID: 23762937

Kumar N, Nuhant P, Solt LA, Conkright JJ, Wang Y, Istrate MA, Busby SA, Ruben DGO, Burris TP, Cameron M, Mercer BA, Hodder P, Roush WR, Rosen H, Griffin PR. Identification of a novel selective inverse agonist probe and analogs for the Retinoic acid receptor-related Orphan Receptor Alpha (RORα). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2010 Sep 1 [updated 2013 Mar 14]. PMID: 23762959

Kamenecka TM, Busby SA, Kumar N, Choi JH, Banks AS, Vidovic D, Cameron MD, Schurer C, Mercer BA, Hodder P, Spiegelman BM, Griffin PR. Potent Anti-Diabetic Actions of a Novel Non-Agonist PPARγ Ligand that Blocks Cdk5-Mediated Phosphorylation. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology nformation (US); 2010-2011 Jul 5 [updated 2013 Mar 7]. PMID: 23762958

Kamenecka TM, Lyda B, Chang MR and Griffin PR, Synthetic modulators of the retinoic acid receptor-related orphan receptors, Med. Chem. Commun., 2013, Advance Article, DOI: 10.1039/C3MD00005B

West GM, Pascal BD, Ng LM, Soon FF, Melcher K, Xu HE, Chalmers MJ, Griffin PR. Protein Conformation Ensembles Monitored by HDX Reveal a Structural Rationale for Abscisic Acid Signaling Protein Affinities and Activities, Structure, 2013, Feb 5;21(2):229-35. doi: 10.1016/j.str.2012.12.001. Epub 2013 Jan 3. PMID:23290725

Khan PM, El-Gendy Bel-D, Kumar N, Garcia-Ordonez R, Lin L, Ruiz CH, Cameron MD, Griffin PR, Kamenecka TM. Small molecule amides as potent ROR-y selective modulators. Bioorg Med Chem Lett., 2013, Jan 15; 23(2): 532-6. Epub 2012 Nov 22. PMID: 23232056

Chang MR, Goswami D, Mercer BA, Griffin PR, The therapeutic potential of RORγ modulators in the treatment of human disease, J. Exp. Pharmacol., 2012, 4, 141 – 148, DOI:

Busby S, Nuhant P, Cameron M, Mercer BA, Hodder P, Roush WR, Griffin PR. Discovery of Inverse Agonists for the Liver Receptor Homologue-1 (LRH1;NR5A2). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2010 Oct 12 [updated 2011 Dec 12]. PMID:23166964

Khan SH, Awasthi S, Guo C, Goswami D, Ling J, Griffin PR, Simons SS Jr, Kumar R. Binding of the N-terminal region of coactivator TIF2 to the intrinsically disordered AF1 domain of the glucocorticoid receptor is accompanied by conformational reorganizations. J Biol Chem., 2012 Dec 28;287(53):44546-60. doi: 10.1074/jbc.M112.411330. Epub 2012 Nov 6. PMID: 23132854

Harmey D, Griffin PR, Kenny PJ. Development of novel pharmacotherapeutics for tobaccco dependence: progress and future directions. Nicotine Tob Res., 2012, Nov;(11):1300-18. Epub 2012 Sep 27. PMID:23024249

Ye L, Kleiner S, Wu J, Sah R, Gupta RK, Banks AS, Cohen P, Khandekar MJ, Boström P, Mepani RJ, Laznik D, Kamenecka TM, Song X, Liedtke W, Mootha VK, Puigserver P, Griffin PR, Clapham DE, Spiegelman BM. TRPV4 is a regulator of adipose oxidative metabolism, inflammation, and energy homeostasis. Cell. 2012,Sep 28;151(1): 96-110. PMID:23021218

Solt LA, Kumar N, He Y, Kamenecka TM, Griffin PR, Burris TP. Identification of a selective RORy ligand that suppresses T(H)17 cells and stimulates T regulatory cells. ACS Chem Biol. 2012 Sep 21;7(9):1515-9. Epub 2012 Jul 9. PMID:22769242

Pascal BD, Willis S, Lauer JL, Landgraf RR, West GM, Marciano D, Novick S, Goswami D, Chalmers MJ, Griffin PR. HDX workbench: software for the analysis of H/D exchange MS data. J Am Soc Mass Spectrom. 2012 Sep;23(9):1512-21. Epub 2012 Jun 13. PMID: 22692830

Chalmers MJ, Wang Y, Novick S, Sato M, Bryant HU, Montrose-Rafizdeh C, Griffin PR, Dodge JA. Hydrophobic Interactions Improve Selectivity to ERalpha for Ben-zothiophene SERMs. ACS Med Chem Lett. 2012, Mar 8;3(3): 207-210. PMID: 22582136

Musille PM, Pathak MC, Lauer JL, Hudson WH, Griffin PR, Ortlund EA. Antidiabetic phospholipid-nuclear receptor complex reveals the mechanism for phospholipid-driven gene regulation. Nat Struct Mol Biol. 2012 Apr 15;19(5):532-7, S1-2. PMID 22504882

Kumar N, Lyda B, Chang MR, Lauer JL, Solt LA, Burris TP, Kamenecka TM, Griffin PR. Identification of SR2211: a ptent synthetic RORy-selective modulator. ACS Chem Biol. 2012 Apr 20;7 (4):672-7. Epub 2012 Feb 13. PMID: 22292739

Burris TP, Busby SA, Griffin PR. Targeting orphan nuclear receptors for treatment of metabolic diseases and autoimmunity. Chem Biol. 2012 Jan 27;19(1):51-9. Review.19, 51-9. PMID:22284354

Hughes TS, Chalmers MJ, Novick S, Kuruvilla DS, Chang MR, Kamenecka TM, Rance M, Johnson BA, Burris TP, Griffin PR, Kojetin DJ. Ligand and receptor dynamics contribute to the mechanism of graded PPARy agonism. Structure. 2012 Jan 11;20(1):139-50. PMID:22244763

Mizwicki MT, Menegaz D, Zhang J, Barrientos-Durán A, Tse S, Cashman JR, Griffin PR, Fiala M. Genomic and nongenomic signaling induced by 1a,25(OH)2-vitamin D3 promotes the recovery of amyloid-beta phagocytosis by Alzheimer's disease macrophages. J Alzheimers Dis., 2012; 29(1):51-62. PMID:22207005

Landgraf RR, Chalmers MJ, Griffin PR. Automated hydrogen/deuterium exchange electron transfer dissociation high resolution mass spectrometry measured at single-amide resolution. J Am Soc Mass Spectrom. 2012 Feb 23(2):301-9. Epub 2011 Dec 1. PMID: 22131230

Canny SA, Cruz Y, Southern MR, Griffin PR. PubChem promiscuity: a web resource for gathering compound promiscuity data from PubChem.Bioinformatics. 2012 Jan 1;28(1):140-1. Epub 2011 Nov 13. PMID: 22084255

Ng LM, Soon FF, Zhou XE, West GM, Kovach A, Suino-Powell KM, Chalmers MJ, Li J, Yong EL, Zhu JK, Griffin PR, Melcher K, Xu HE. Structural Basis for basal activity and autoactivation of abscisic acid (ABA) signaling SnRK2 kinases. Proc Natl Acad Sci U S A. 2011 Dec 27; 108(52):21259-64. Epub 2011 Dec 12. PMID:22160701

Soon FF, Ng LM, Zhou XE, West GM, Kovach A, Tan MH, Suino-Powell KM, He Y, Xu Y, Chalmers MJ, Brunzelle JS, Zhang H, Yang H, Jiang H, Li J, Yong EL, Cutler S, Zhu JK, Griffin PR, Melcher K, Xu HE., Molecular Mimicry Regulates ABA Signaling by SnRK2 Kinases and PP2C Phosphatases., Science, 2011 Nov 24. PMID:22116026

Malapaka RR, Khoo S, Zhang J, Choi JH, Zhou XE, Xu Y, Gong Y, Li J, Yong EL, Chalmers MJ, Chang L, Resau JH, Griffin PR, Chen YE, Xu HE. J Biol Chem. 2012 Jan 2;287(1):183-95. Epub 2011 Oct 28. PMID: 22039047

Devarakonda S, Gupta K, Chalmers MJ, Hunt JF, Griffin PR, Van Duyne GD, Spiegelman BM., Disorder-to-order transition underlies the structural basis for the assembly of a transcriptionally active PGC-1α/ERRγ complex. Proc Natl Acad Sci U S A., 2011 Nov 15; 108(46):18678-83. 18678-83. doi: 10.1073/pnas.1113813108. Epub 2011 Nov 2. PMID: 22049338

Choi JH, Banks AS, Kamenecka TM, Busby SA, Chalmers MJ, Kumar N, Kuruvilla DS, Shin Y, He Y, Bruning JB, Marciano DP, Cameron MD, Laznik D, Jurczak MJ, Schürer SC, Vidović D, Shulman GI, Spiegelman BM, and Griffin PR., Anti-Diabetic Actions of a Non-Agonist PPARγ Ligand Blocking Cdk5-Mediated Phosphorylation, Nature, 2011 Sep 4;477(7365):477-81.doi 10.1038/nature10383. PMID:21892191

West GM, Chien EYT, Katritch V, Gatchalian J, Chalmers MJ, Stevens RC, Griffin PR., Ligand-dependent perturbation of the conformational ensemble for the GPCR beta2 adrenergic receptor revealed by HDX, Structure, 2011 Oct 12;19(10): 1424-32. Epub 2011 Sep 1. PMID:21889352

Lee JM, Lee YK, Mamrosh KL, Busby SA, Griffin PR, Pathak MC, Ortlund EA and Moore DD, Antidiabetic Effects of a Novel Agonist Ligand for the Nuclear Receptor LRH-1, Nature, 2011 May 25;474(7352):506-10. PMID: 21614002

Chalmers MJ, Pascal BD, Willis S, Zhang J, Iturria SJ, Dodge JA, Griffin PR. Methods for the Analysis of High Precision Differential Hydrogen Deuterium Exchange Data. Int J Mass Spectrom. 2011 Apr 30;302(1-3):59-68. PMID:21528013

Solt LA, Kumar N, Nuhant P, Wang Y, Lauer JL, Liu J, Istrate MA, Kamenecka TM, Roush WR, Vidovic D, Schurer S, Xu J, Wagoner G, Drew PD, Griffin PR, and Burris TP, Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand, Nature, 2011, Apr 28;472(7344): 491-4. Epub 2011 Apr 17. PMID: 21499262

Zhang J, Chalmers MJ, Stayrook KR, Burris LL, Wang Y, Busby SA, Pascal BD, Garcia-Ordonez RD, Bruning JB, Istrate MA, Kojetin DJ, Dodge JA, Burris TP and Griffin PR, DNA binding alters coactivator interaction surfaces of the intact VDR–RXR complex, Nat Struct Mol Biol, 2011 May 18(5): 556-63. Epub 2011 Apr 10. PMID:21478866

Heidebrecht T, Christodoulou E, Chalmers MJ, Jan S, Ter Riet B, Grover RK, Joosten RP, Littler D, van Luenen H, Griffin PR, Wentworth P Jr, Borst P, Perrakis A., The structural basis for recognition of base J containing DNA by a novel DNA binding domain in JBP1, Nucleic Acids Res., 2011 Jul 39(13): 5715-28. doi: 10.1093/nar/gkr125.Epub 2011 Mar 16. PMID: 21415010

Willis S and Griffin PR, Mutual Information identifies sequence positions conserved within the nuclear receptor superfamily: approach reveals functionally important regions for DNA binding specificity, NURSA, 2011 Feb 25;9:e001. PMID: 21383938

Busby SA, Kumar N, Kuruvilla DS, Istrate MA, Conkright JJ, Wang Y, Kamenecka TM, Cameron MD, Roush WR, Burris TP, Griffin PR., Identification of a Novel Non-retinoid Pan Inverse Agonist of the Retinoic Acid Receptors, ACS Chem Biol., 2011 Jun 17;6(6):618-27. Epub 2011 Mar 17. PMID: 21381756

Chalmers MJ, Busby SA, Pascal BD, West GM and Griffin PR, Differential hydrogen/deuterium exchange mass spectrometry analysis of protein-ligand interactions, Expert Rev Proteomics, 2011 Feb 8(1):43-59. Review. PMID: 21329427

Istrate MA, Spicer TP, Wang Y, Bernard JA, Helvering LM, Bocchinfuso WP, Richardson TI, Zink R, Kumar N, Montrose-Rafizadeh C, Dodge JA, Hodder P and Griffin PR, Development of an HTS-Compatible Assay for Discovery of RORα Modulators Using AlphaScreen Technology, J Biomol Screen, 2011 Feb16(2):183-91. PMID: 21297105

Wright E, Busby SA, Wisecarver S, Vincent J, Griffin PR, Fernandez EJ, Helix 11 dynamics is critical for constitutive androstane receptor activity, Structure, 2011,Jan 12;19(1):37-44. PMID:21220114

Southern MR and Griffin PR, A Java API for working with PubChem datasets, Bioinformatics, 2011, Mar 1;27(5):741-2. Epub 2011 Jan 6. PMID: 21216779

Vidović D, Busby SA, Griffin PR, Schürer SC, A combined ligand- and structure-based virtual screening protocol identifies submicromolar PPARγ partial agonists, ChemMedChem, 2011, Jan 3;6(1);94-103. PMID: 21162086

Kumar N, Kojetin DJ, Solt LA, Kumar KG, Nuhant P, Duckett DR, Cameron MD, Butler AA, Roush WR, Griffin PR, Burris TP., Identification of SR3335 (ML-176): A Synthetic RORα Selective Inverse Agonist, ACS Chem Biol. 2011 Mar 18;6(3):218-22. Epub 2010 Dec 6. PMID: 21090593

Fanning SW, Mayne CG, Dharmarajan V, Carlson KE, Martin TA, Novick SJ, Toy W, Green B, Panchamukhi S, Katzenellenbogen BS, Tajkhorshid E, Griffin PR, Shen Y, Chandarlapaty S, Katzenellenbogen JA, Greene GL. Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation.Elife. 2016 Feb 2;5.

Zhang J, Chalmers MJ, Stayrook KR, Burris LL, Garcia-Ordonez RD, Pascal BD, Burris TP, Dodge JA and Griffin PR, Hydrogen/Deuterium Exchange Reveals Distinct Agonist/Partial Agonist Receptor Dynamics within the intact Vitamin D Receptor/Retinoid X Receptor Heterodimer, Structure, 2010,Oct 13;18(10): 1332-41. PMID: 20947021

Wang Y, Kumar N, Nuhant P, Cameron MD, Istrate MA, Roush WR, Griffin PR, Burris TP. Identification of SR1078, a synthetic agonist for the orphan nuclear receptors RORalpha and RORgamma, ACS Chemical Biology, 2010 Nov 19;5(11):1029-34. PMID: 20735016

Kumar N, Solt LA, Conkright J, Wang Y, Istrate MA, Busby SA, Garcia-Ordonez RD, Nuhant P, Burris T, Mercer BA, Hodder P, Roush WR, Rosen H, Griffin PR. Campaign to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR). Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010.

Choi JH, Banks AS, Estall JL, Kajimura S, Boström P, Laznik D, Ruas JL, Chalmers MJ, Kamenecka TM, Blüher M, Griffin PR, Spiegelman BM, Anti-diabetic drugs inhibit obesity-linked phosphorylation of PPARgamma by Cdk5, Nature, 2010, Jul 22; 466(7305):451-6. PMID: 20651683

Solt LA, Griffin PR and Burris TP Ligand regulation of retinoic acid receptor-related orphan receptors: implications for development of novel therapeutics, Current Opin Lipidol, 2010,Jun 21;(3):204-11. doi:10.1097/MOL.0b013e328338ca18. Review. PMID: 0463469

Kumar N, Solt LA, Wang Y, Rogers PM, Bhattacharyya G, Kamenecka TM, Stayrook KR, Crumbley C, Floyd ZE, Gimble JM, Griffin PR and Burris TP Regulation of adipogenesis by natural and synthetic REV-ERB ligands, Endocrinology, 2010, Jul;151(7): 3015-5. Epub 2010 Apr 28. PMID: 20427485

Wang Y, Kumar N, Crumbley C, Griffin PR and Burris TP A second class of nuclear receptors for oxysterols: Regulation of RORalpha and RORgamma activity by 24S-hydroxycholesterol (cerebrosterol), Biochim Biophys Acta. 2010 Aug; 1801(8):917-923. Epub 2010 Mar 6. PMID: 20211758

Zhang X, Chien EYT, Chalmers MJ, Pascal BD, Gatchalian J, Stevens RC, and Griffin PR, Dynamics of the beta2-adrenergic G-protein coupled receptor revelaed by hydrogen/deuterium exchange, Analytical Chem. 2010 Feb 1;82(3):1100-8. PMID: 20058880

Wang Y, Kumar N, Solt LA, Richardson TI, Helvering LM, Crumbley C, Garcia-Ordonez RD, Stayrook KR, Zhang X, Novick S, Chalmers MJ, Griffin PR, Burris TP., Modulation of retinoic acid receptor-related orphan receptor alpha and gamma activity by 7-oxygenated sterol ligands., J Biol Chem., 2010 Feb 12;285(7):5013-25. Epub 2009 Dec 4. PMID: 19965867

Kumar N, Solt LA, Conkright JJ, Wang Y, Istrate MA, Garcia-Ordonez R, Burris TP, and Griffin PR, The benzenesulfoamide T0901317 is a novel RORalpha/gamma inverse agonist, Mol Pharmacol. 2010, Feb;77(2):228-36. Epub 2009 Nov 3. PMID: 19887649

Dai S., Burris TP, Dodge JA., Montrose-Rafizadeh C., Wang Y., Pascal B., Chalmers MJ, and Griffin PR, Unique ligand binding patterns between estrogen receptor α and β revealed by hydrogen/deuterium exchange, Biochemistry, 2009 Oct 13;48(40): 9668-76. PMID: 19739677

Noël R, Song X, Jiang R, Chalmers MJ, Griffin PR, Kamenecka TM., Efficient methodology for the synthesis of 3-amino-1,2,4-triazoles, J Org Chem, 2009 Oct 2;74(19):7595-7. PMID: 19731897

Avvaru BS, Busby SA, Chalmers MJ, Griffin PR, Venkatakrishnan B, Agbandje-McKenna M, Silverman DN, McKenna R, Apo-human carbonic anhydrase II revisited: implications of the loss of a metal in protein structure, stability, and solvent network, Biochemistry, 2009 Aug 11;48(31):7365-72. PMID: 19583303

Lauer-Fields JL, Chalmers MJ, Busby SA, Minond D, Griffin PR, Fields GB., Identification of specific hemopexin-like domain residues that facilitate matrix metalloproteinase collagenolytic activity, J Biol Chem., 2009 Sep 4;284(36):24017-24. Epub 2009 Jul 1. PMID: 19574232

Pascal BD, Chalmers MJ, Busby SA, Griffin PR, HD desktop: an integrated platform for the analysis and visualization of H/D exchange data, J Am Soc Mass Spectrom. 2009 Apr;20(4):20, 601-10. Epub 2008 Dec 6. PMID: 19135386

Dai, S.Y., Chalmers, M.J., Bruning, J., Bramlett, K.S., Osborne, H.E., Montrose-Rafizadeh, C., Barr, R.J., Wang, M., Burris, T.P., Dodge, J.A., Griffin, P.R., Prediction of the tissue-specificity of selective estrogen receptor modulators using a single biochemical method. Proc. Natl. Acad. Sci. U. S. A., 2008 May 20;105(20):7171-6. Epub 2008 May 12. PMID: 18474858

Madoux F, Li X, Chase P, Zastrow G, Cameron MD, Conkright JJ, Griffin PR, Thacher S, Hodder P., Potent, selective and cell penetrant inhibitors of SF-1 by functional ultra-high-throughput screening, Mol Pharmacol, 2008 Jun;73(6):1776-84. Epub 2008 Mar 11. PMID: 18334597

Bruning JB, Chalmers MJ, Prasad S, Busby SA, Kamenecka TM, He Y, Nettles KW, Griffin PR., Partial agonists activate PPARgamma using a helix 12 independent mechanism, Structure, 2007 Oct;15(10):1258-71. PMID: 17937915

Chalmers MJ, Busby SA, Pascal BD, Southern MR, Griffin PR. A two-stage differential hydrogen euterium exchange method for the rapid characterization of protein/ligand interactions. J Biomol Tech. 2007 Sep;18(4): 194-204. PMID:17916792

Hamuro Y, Coales SJ, Morrow JA, Molnar KS, Tuske SJ, Southern MR, Griffin PR. Hydrogen/deuterium-exchange (HD-Ex) of PPARgamma LBD in the presence of various modulators. Protein Sci. 2006 Aug;15(8):1883-92. Epub 2006 Jul 5. PMID: 16819819

Quint P, Ayala I, Busby SA, Chalmers MJ, Griffin PR, Rocca J, Nick HS, Silverman DN. Structural mobility in human manganese superoxide dismutase. Biochemistry.2006 Jul 11;45(27):8209-15. PMID: 16819819

Chalmers MJ, Busby SA, Pascal BD, He Y, Hendrickson CL, Marshall AG, Griffin PR. Probing protein ligand interactions by automated hydrogen/deuterium exchange mass spectrometry. Anal Chem. 2006 Feb 15;78(4):1005-14. PMID: 16478090

Hamuro Y, Weber PC, Griffin PR. High-throughput analysis of protein structure by hydrogen
/deuterium exchange mass spectrometry. Methods Biochem Anal. 2005;45:131-57. Review.
PMID: 19235294

Feng L, Dharmarajan V, Serrao E, Hoyte A, Larue RC, Slaughter A, Sharma A, Plumb MR, Kessl JJ, Fuchs JR, Bushman FD, Engelman AN, Griffin PR, Kvaratskhelia M.  The Competitive Interplay between Allosteric HIV-1 Integrase Inhibitor BI/D and LEDGF/p75 during the Early Stage of HIV-1 Replication Adversely Affects Inhibitor Potency. ACS Chem Biol. 2016 May 20;11(5):1313-21.  PMCID:  PMC4874862.

Stechschulte LA, Czernik PJ, Rotter ZC, Tausif FN, Corzo CA, Marciano DP, Asteian A, Zheng J, Bruning JB, Kamenecka TM, Rosen CJ, Griffin PR, Lecka-Czernik B.PPARG Post-translational Modifications Regulate Bone Formation and Bone Resorption. EBioMedicine. 2016 Jun 29. pii: S2352-3964(16)30297-3. PMID: 27422345


Company Ember is launched and website is live.

Nat Struct Mol Biol. 2012 Apr 15. doi: 10.1038/nsmb.2279. [Epub ahead of print]

Scientists Establish New Class of Anti-Diabetic Compound

NIH Research Matters: Designing New Diabetes Drugs

Patrick Griffin and Paul Kenny Awarded Grant to Create National Anti-Addiction Network

Scripps Florida is Awarded Grant to Create National Anti-Addiction Network

Bicoastal Team Pinpoints Shape-Shifting Mechanism Critical to Protein Signaling

Building a Bridge from Basic Science to New Therapies

The Scripps Research Molecular Screening Center