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• Mol Pharmacol.2010 Jan;77(1):46-57.Epub 2009 Oct 16.PMID: 19837904
  Selective and brain penetrant neuropeptide Y Y2 receptor antagonists discovered by whole-cell high-throughput screenin
  Brothers SP, Saldanha SA, Spicer TP, Camgeron M, Mercer BA, Chase P, McDonald P, Wahlestedt C, Hodder PS
  - The Scripps Research Institute, Jupiter, Florida
  
  
• J Neurosci. 2010 Oct 6;30(40):13513-24. PMID: 20926677 
  Serotonin, but not N-methyltryptamines, activates the serotonin 2A receptor via a β-arrestin2/Src/Akt signaling complex in vivo.
  Schmid CL, Bohn LM.
  - Departments of Molecular Therapeutics and Neuroscience
  Hallucinogens mediate many of their psychoactive effects by activating serotonin 2A receptors (5-HT(2A)R.
  
  
• Methods Mol Biol. 2011;670:263-74. PMID: 20967596 [Epub ahead of print] PMID: 21054685 
  Epigenetic changes in the brain: measuring global histone modifications.
  Rumbaugh G, Miller CA.
  - Department of Neursocience
  Recent years have witnessed an explosion of research on the role of epigenetic modifications, such as DNA methylation and histone protein acetylation and phosphorylation, in neuroscience.
  
  
• Addict Biol. 2010 Nov 4. doi: 10.1111/j.1369-1600.2010.00253. [Epub ahead of print] PMID: 21054685 
  Impact of food restriction and cocaine on locomotion in ghrelin- and ghrelin-receptor knockout mice.
  Clifford S, Zeckler RA, Buckman S, Thompson J, Hart N, Wellman PJ, Smith RG.
  - Department of Metabolism and Aging
  Food restriction (FR) augments the behavioral and reinforcing effects of psychomotor stimulants such as cocaine or amphetamine....
  
  
• Mamm Genome. 2010 Jun;21(5-6):247-57. Epub 2010 May 29. PMID: 20512339 
  Quantitative trait locus analysis identifies Gabra3 as a regulator of behavioral despair in mice.
  Miller BH, Schultz LE, Long BC, Pletcher MT.
  - Department of Neuroscience
  The Tail Suspension Test (TST), which measures behavioral despair, is widely used as an animal model of human depressive disorders and antidepressant efficacy.
  
  
• Stem Cells. 2010 Oct 22. [Epub ahead of print]PMID: 20973030 
  Twist, EMT, and Stem Cells.
  Phinney DG.
  - Department of Molecular Therapeutics
  
  
• PLoS One. 2010 Oct 4;5(10). pii: e13177. PMID: 20957177 
  RNAi Screen Indicates Widespread Biological Function for Human Natural Antisense Transcripts.
  Faghihi MA, Kocerha J, Modarresi F, Engström PG, Chalk AM, Brothers SP, Koesema E, St Laurent G, Wahlestedt C.
  -Department of Neuroscience
  Natural antisense transcripts represent a class of regulatory RNA molecules, which are characterized by their complementary sequence to another RNA transcript.
  
  
• Structure. 2010 Oct 13;18(10):1332-41. PMID: 20947021 
  Hydrogen/Deuterium Exchange Reveals Distinct Agonist/Partial Agonist Receptor Dynamics within Vitamin D Receptor/Retinoid X Receptor Heterodimer.
  Zhang J, Chalmers MJ, Stayrook KR, Burris LL, Garcia-Ordonez RD, Pascal BD, Burris TP, Dodge JA, Griffin PR.
  -Department of Molecular Therapeutics
  Regulation of nuclear receptor (NR) activity is driven by alterations in the conformational dynamics of the receptor upon ligand binding.
  
  
• J Neurosci. 2010 Oct 6;30(40):13513-24. PMID: 20926677 
  Serotonin, But Not N-Methyltryptamines, Activates the Serotonin 2A Receptor Via a β-Arrestin2/Src/Akt Signaling Complex In Vivo.
  Schmid CL, Bohn LM.
  -Departments of Molecular Therapeutics and Neuroscience
  Hallucinogens mediate many of their psychoactive effects by activating serotonin 2A receptors (5-HT(2A)R).
  
  
• Drug Metab Dispos. 2010 Jul;38(7):1238-45. Epub 2010 Apr 9. PMID: 20382753 
  Cytochrome P450-mediated bioactivation of the epidermal growth factor receptor inhibitor erlotinib to a reactive electrophile.
  Li X, Kamenecka TM, Cameron MD.
  -Translational Research Institute
  The epidermal growth factor receptor tyrosine kinase inhibitor erlotinib (ERL) is approved for treatment of non-small-cell lung cancer. 
  
  
• PLoS Negl Trop Dis. 2010 Sep 14;4(9). pii: e825. PMID: 20856868 
  In Vitro and In Vivo Studies of the Trypanocidal Properties of WRR-483 against Trypanosoma cruzi.
  Chen YT, Brinen LS, Kerr ID, Hansell E, Doyle PS, McKerrow JH, Roush WR.
  -Department of Chemistry
  Cruzain, the major cysteine protease of Trypanosoma cruzi, is an essential enzyme for the parasite life cycle and has been validated as a viable target to treat Chagas' disease.
  
  
• J Gen Virol. 2010 Sep 29. [Epub ahead of print] PMID: 20881089 
  Dimerization-driven interaction of hepatitis c virus core protein with NS3 helicase.
  Mousseau G, Kota S, Takahashi V, Frick D, Strosberg AD.
  -Department of Infectology
  Hepatitis C virus (HCV) infects over 130 million people causing a worldwide epidemic of liver cirrhosis and hepatocellular-carcinoma. 
  
  
• Assay Drug Dev Technol. 2010 Sep 21. [Epub ahead of print] PMID: 20858054 
  A Predictive Nuclear Translocation Assayfor Spliced X-Box-Binding Protein 1 Identifies Compounds with Known Organ Toxicities.
  Hahmann C, Weiser A, Duckett D, Schroeter T.
  -Department of Molecular Therapeutics and Translational Research Institute
  Compound toxicity is still the main cause of attrition, emphasizing the need for novel predictive assays to identify toxic compounds early during drug development. 
  
  
• Genome Biol. 2010;11(5):R56. Epub 2010 May 27. PMID: 20507594 
  Evidence for natural antisense transcript-mediated inhibition of microRNA function.
  Faghihi MA, Zhang M, Huang J, Modarresi F, Van der Brug MP, Nalls MA, Cookson MR, St-Laurent G 3rd, Wahlestedt C..
  -Department of Neuroscience
  MicroRNAs (miRNAs) have the potential to regulate diverse sets of mRNA targets. 
  
  
• Chem Commun (Camb). 2010 Aug 25. [Epub ahead of print] PMID: 20740228 
  A fluopol-ABPP HTS assay to identify PAD inhibitors.
  Knuckley B, Jones JE, Bachovchin DA, Slack J, Causey CP, Brown SJ, Rosen H, Cravatt BF, *Thompson PR.
  -*Department of Chemistry 
  Protein Arginine Deiminase (PAD) activity is dysregulated in numerous diseases, e.g., Rheumatoid Arthritis.
  
  
• Org Lett. 2010 Aug 31. [Epub ahead of print] PMID: 20806914 
  Enantioselective Synthesis of (Z)-1,2-anti-2,5-anti-Triol Monosilyl Ethers Using a Cross-Metathesis Allylboration Sequence.
  Winbush SM, Roush WR.
  -Department of Chemistry 
  The enantioselective synthesis of (Z)-1,2-anti-2,5-anti-triol monosilyl ethers via a two-step sequence involving olefin cross-metathesis of beta-alkoxyallylboronate 4 and subsequent allylboration of the derived bisboryl intermediate 6 provides triol monoethers 7 with good to excellent diastereoselectivity.
  
  
• ACS Chem Biol. 2010 Aug 24. [Epub ahead of print] 
  Identification of a Synthetic Agonist for the Orphan Nuclear Receptors RORalpha and RORgamma, SR1078.
  Wang Y, Kumar N, Nuhant P, Cameron MD, Istrate MA, Roush WR, Griffin PR, Burris TP.
  -Department of Molecular Therapeutics 
  The retinoic acid receptor-related receptors (RORs) are members of the nuclear receptor (NR) superfamily of transcription factors. 
  
  
• Nat Neurosci. 2010 Aug 15. [Epub ahead of print] 
  MeCP2 controls BDNF expression and cocaine intake through homeostatic interactions with microRNA-212.
  Im HI, Hollander JA, Bali P, Kenny PJ.
  - Laboratory of Behavioral and Molecular Neuroscience, Department of Molecular Therapeutics 
  The X-linked transcriptional repressor methyl CpG binding protein 2 (MeCP2), known for its role in the neurodevelopmental disorder Rett syndrome, is emerging as an important regulator of neuroplasticity in postmitotic neurons
  
  
• Nature. 2010 Jul 22;466(7305):451-6. 
  Anti-diabetic drugs inhibit obesity-linked phosphorylation of PPARgamma by Cdk5.
  Choi JH, Banks AS, Estall JL, Kajimura S, Boström P, Laznik D, Ruas JL, Chalmers MJ, Kamenecka TM, Blüher M, Griffin PR*, Spiegelman BM.
  - *Department of Molecular Therapeutics, Scripps Florida; Department of Cancer Biology and Division of Metabolism and Chronic Disease, Dana-Farber Cancer Institute 
  Obesity induced in mice by high-fat feeding activates the protein kinase Cdk5 (cyclin-dependent kinase 5) in adipose tissues.
  
  
• Org Lett. 2010 May 21;12(10):2342-5. 
  Enantioselective synthesis of alpha-methylene-beta-hydroxy carboxylic acid derivatives via a diastereoselective aldol/beta-elimination sequence: application to the C(15)-C(21) fragment of tedanolide C.
  Barth R, Roush WR.
  - Department of Chemistry 
  An enantioselective synthesis of alpha-methylene-beta-hydroxy carboxylic acid derivatives via a highly diastereoselective, one-pot syn-aldol and beta-elimination sequence utilizing the chiral beta-(phenylselenyl)propionyl imide 15 is described. 
  
  
• Nat Rev Mol Cell Biol. 2010 Aug 11. [Epub ahead of print] 
  New functions of aminoacyl-tRNA synthetases beyond translation.
  Guo M, Yang XL, Schimmel P.
  - The Skaggs Institute for Chemical Biology and Department of Molecular Biology, Department of Cancer Biology 
  Over the course of evolution, eukaryotic aminoacyl-tRNA synthetases (aaRSs) progressively incorporated domains and motifs that have no essential connection to aminoacylation reactions.
  
  
• J Med Chem. 2010 Aug 12;53(15):5727-37. 
  Tetrahydroisoquinoline derivatives as highly selective and potent rho kinase inhibitors.
  Fang X, Yin Y, Chen YT, Yao L, Wang B, Cameron MD, Lin L, Khan S, Ruiz C, Schröter T, Grant W, Weiser A, Pocas J, Pachori A, Schürer S, Lograsso P, Feng Y.
  - Translational Research Institute and Department of Molecular Therapeutics 
  Rho kinase (ROCK) is a promising drug target for the treatment of many diseases including hypertension, multiple sclerosis, cancer, and glaucoma. 
  
  
• Expert Opin Drug Metab Toxicol. 2010 Aug 5. [Epub ahead of print] 
  Metabolism considerations for kinase inhibitors in cancer treatment.
  Duckett DR, Cameron MD
  - Department of Molecular Therapeutics 
  Importance of the field: A concerted effort by the pharmaceutical industry over the last decade has led to the successful clinical development of protein kinase inhibitors as effective targeted therapies for certain cancers. 
  
  
• J Am Chem Soc. 2010 Aug 25;132(33):11422-4. PMID: 20681603 
  Total Synthesis of Lehualide B by Allylic Alcohol-Alkyne Reductive Cross-Coupling.
  Jeso V, Micalizio GC.
  - Department of Chemistry 
  The total synthesis of anticancer marine natural product lehualide B is described. 
  
  
• Curr Opin Chem Biol. 2010 Jul 30. [Epub ahead of print] 
  Development of antibody surrogates for the treatment of cancers and autoimmune disease.
  Kodadek T.
  - Department of Chemistry 
  Some therapeutic monoclonal antibodies function by focusing the killing power of the immune system on particular cellular targets, a process known as antibody-dependent cell-mediated cytotoxicity (ADCC).
  
  
• Curr Opin Chem Biol. 2010 Jul 29. [Epub ahead of print] 
  Synthetic receptors with antibody-like binding affinities.
  Kodadek T.
  - Department of Chemistry 
  Antibodies are critical reagents in biological research and are increasingly being developed as therapeutic agents.
  
  
• J Biomol Screen.2010 Jul 26.Epub ahead of print.PMID: 20660794 
  An ultra-high throughput cell-based screen for Wee1 degradation inhibitors
  Madoux F, Simanski S, Chase P, Mishra JK, Roush WR, Ayad NG, **Hodder PS
  - **Scripps Florida 
  The tyrosine kinase Wee1 is part of a key cellular sensing mechanism that signals completion of DNA replication, ensuring proper timing of entry into mitosis. 
  
  
• Nat Chem. 2010 Aug;2(8):638-43. Epub 2010 May 23. 
  Convergent and stereospecific synthesis of complex skipped polyenes and polyunsaturated fatty acids.
  Macklin TK, Micalizio GC.
  - Department of Chemistry 
  Skipped polyenes (that is, 1,4-dienes and higher homologues) are stereodefined components of a vast array of biologically important natural products, including polyunsaturated fatty acids. 
  
  
• Nature. 2010 Jul 8;466(7303):197-202. 
  Striatal microRNA controls cocaine intake through CREB signalling.
  Hollander JA, Im HI, Amelio AL, Kocerha J, Bali P, Lu Q, Willoughby D, Wahlestedt C, Conkright MD, Kenny PJ.
  - Laboratory of Behavioral and Molecular Neuroscience, Department of Molecular Therapeutics 
  Cocaine addiction is characterized by a gradual loss of control over drug use, but the molecular mechanisms regulating vulnerability to this process remain unclear. 
  
  
• ACS Med Chem Lett.2010 Jul 8;1(4):150-154.PMID: 20625539 
  NH-1,2,3-triazole-based inhibitors of the VIM-2 metallo-beta-lactamase: synthesis and structure-activity studies.
  Weide T, Saldanha SA, Minond D, Fotsing JR, Spaargaren M, Frère JM, Bebrone C, Sharpless KB, **Hodder P, Fokin VV
  - **Scripps Florida 
  Metallo-ss-lactamases (MBL) are an emerging cause of bacterial resistance to antibiotic treatment.
  
  
• Drug Discov Today. 2010 Jul 8. [Epub ahead of print] 
  Role of Sirtuin 1 in metabolic regulation.
  Silva JP, Wahlestedt C.
  - Department of Neuroscience and Department of Molecular Therapeutics 
  Sirtuin proteins are an evolutionarily conserved family of NAD+-dependent protein deacetylases. 
  
  
• Assay Drug Dev Technol.2010 Jun 1.Epub ahead of print.PMID: 20515413 
  A high-throughput screening compatible assay for activators and inhibitors of methionine sulfoxide reductase A
  Brunell D, Weissbach H, **Hodder P, Brot N
  -** Scripps Florida 
  The methionine sulfoxide reductase (Msr) system has been shown to play an important role in protecting cells against oxidative damage. 
  
  
• Bioorg Med Chem Lett. 2010 Mar 15;20(6):1939-43. Epub 2010 Feb 1. 
  The development of benzimidazoles as selective rho kinase inhibitors.
  Sessions EH, Smolinski M, Wang B, Frackowiak B, Chowdhury S, Yin Y, Chen YT, Ruiz C, Lin L, Pocas J, Schröter T, Cameron MD, LoGrasso P, Feng Y, Bannister TD.
  - Department of Molecular Therapeutics and Translational Research Institute 
  Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. 
  
  
• J Am Chem Soc. 2010 Jul 21;132(28):9576-8. PMID: 20586460 
  Chemoselective Reductive Cross-Coupling of 1,5-Diene-3-ols with Alkynes: A Facile Entry to Stereodefined Skipped Trienes.
  Diez PS, Micalizio GC.
  - Department of Chemistry 
  A convergent synthesis of highly substituted and stereodefined skipped polyenes is described from the reductive cross-coupling of substituted 1,5-diene-3-ols with alkynes. 
  
  
• Biochemistry. 2010 May 18;49(19):4094-102 
  Mechanism of oxidative stress-induced ASK1-catalyzed MKK6 phosphorylation.
  Sturchler E, Feurstein D, McDonald P, Duckett D.
  - Department of Molecular Therapeutics and Translational Research Institute 
  Apoptosis signal-regulating kinase 1 (ASK1) is a serine/threonine kinase that responds to a plethora of stress-inducing signals. 
  
  
• Biol Chem. 2010 May 21;285(21):15668-73. Epub 2010 Mar 23 
  Regulation of FGF21 expression and secretion by retinoic acid receptor-related orphan receptor alpha
  Wang Y, Solt LA, Burris TP.
  - Department of Molecular Therapeutics 
  Fibroblast growth factor 21 (FGF21) is a hormone produced by fat and the liver that plays an important role in lipid metabolism. 
  
  
• EMBO Rep. 2010 Jul;11(7):555-60. Epub 2010 May 28. PMID: 20508641
  Nucleosome occupancy landscape and dynamics at mouse recombination hotspots.
  Getun IV, Wu ZK, Khalil AM, Bois PR.
  - Department of Cancer Biology 
  During meiosis, paternal and maternal homologous chromosomes recombine at specific recombination sites named hotspots. 
  
  
• PLoS One. 2010 May 19;5(5):e10679. 
  A helix replacement mechanism directs metavinculin functions.
  Rangarajan ES, Lee JH, Yogesha SD, Izard T.
  - Department of Cancer Biology 
  Cells require distinct adhesion complexes to form contacts with their neighbors or the extracellular matrix, and vinculin links these complexes to the actin cytoskeleton. 
  
  
• Mol Biosyst. 2010 Aug;6(8):1366-75. Epub 2010 Jun 7. 
  Chemistry and biology of orexin signaling.
  Kodadek T, Cai D.
  -Departments of Chemistry and Cancer Biology 
  The orexins are neurohormones that, in concert with their cognate receptors, regulate a number of important physiological processes, including feeding, sleep, reward seeking and energy homeostasis.
  
  
• Mamm Genome. 2010 May 29. [Epub ahead of print] 
  Quantitative trait locus analysis identifies Gabra3 as a regulator of behavioral despair in mice.
  Miller BH, Schultz LE, Long BC, Pletcher MT.
  -Department of Neuroscience 
  The Tail Suspension Test (TST), which measures behavioral despair, is widely used as an animal model of human depressive disorders and antidepressant efficacy.
  
  
• Nat Neurosci. 2010 May 23. [Epub ahead of print] 
  Cortical DNA methylation maintains remote memory.
  Miller CA, Gavin CF, White JA, Parrish RR, Honasoge A, Yancey CR, Rivera IM, Rubio MD, Rumbaugh G, Sweatt JD.
  -Department of Neuroscience 
  A behavioral memory's lifetime represents multiple molecular lifetimes, suggesting the necessity for a self-perpetuating signal. 
  
  
• J Am Chem Soc. 2010 Jun 16;132(23):7881-3. PMID: 20496899 
  Enantioselective Synthesis of (E)-delta-Stannyl Homoallylic Alcohols via Aldehyde Allylboration Using alpha-Stannylallylboranes Generated by Allene Hydroboration Followed by a Highly Diastereoselective 1,3-Boratropic Shift.
  Chen M, Ess DH, Roush WR.
  -Department of Chemistry 
  A highly enantioselective synthesis of (E)-delta-stannyl homoallylic alcohols 4 via aldehyde allylboration reactions of the double-chiral allylborane reagent 2a is reported. 
  
  
• Org Lett. 2010 Jun 18;12(12):2706-9. 
  Highly (E)-Selective BF(3).Et(2)O-Promoted Allylboration of Chiral Nonracemic alpha-Substituted Allylboronates and Analysis of the Origin of Stereocontrol.
  Chen M, Roush WR.
  -Department of Chemistry 
  delta-Methyl-substituted homoallylic alcohols 2 were prepared in 71-88% yield, E:Z >30:1 and 93% to >95% ee via BF(3).Et(2)O-promoted allylboration with alpha-Me-allylboronate 1. 
  
  
• Anal Chem. 2010 Feb 1;82(3):1100-8. 
  Dynamics of the beta2-adrenergic G-protein coupled receptor revealed by hydrogen-deuterium exchange.
  Zhang X, Chien EY, Chalmers MJ, Pascal BD, Gatchalian J, Stevens RC, Griffin PR.
  -Department of Molecular Therapeutics 
  To examine the molecular details of ligand activation of G-protein coupled receptors (GPCRs), emphasis has been placed on structure determination of these receptors with stabilizing ligands.
  
  
• J Am Chem Soc. 2010 Jun 9;132(22):7602-4. PMID: 20476790 
  Polyketide Assembly by Alkene-Alkyne Reductive Cross-Coupling: Spiroketals through the Union of Homoallylic Alcohols.
  Canterbury DP, Micalizio GC.
  -Department of Chemistry 
  A reaction sequence composed of regioselective formal hydroalkynylation, reductive ene-yne cross-coupling, and oxidative cyclization has been developed to prepare stereochemically dense spiroketals.
  
  
• J Biol Chem. 2010 Apr 16;285(16):11983-90. Epub 2010 Feb 2. 
  Mechanism of aldolase control of sorting nexin 9 function in endocytosis
  Rangarajan ES, Park H, Fortin E, Sygusch J, Izard T.
  -Department of Cancer Biology 
  Sorting nexin 9 (SNX9) functions in a complex with the GTPase dynamin-2 at clathrin-coated pits, where it provokes fission of vesicles to complete endocytosis. 
  
  
• J Biol Chem. 2010 Feb 12;285(7):5013-25. Epub 2009 Dec 4. 
  Modulation of retinoic acid receptor-related orphan receptor alpha and gamma activity by 7-oxygenated sterol ligands.
  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.
  -Department of Molecular Therapeutics 
  The retinoic acid receptor-related orphan receptors alpha and gamma (RORalpha (NR1F1) and RORgamma (NR1F3)) are orphan nuclear receptors and perform critical roles in regulation of development, metabolism, and immune function.
  
  
• Assay Drug Dev Technol. 2010 Feb;8(1):96-105. 
  A time-resolved fluorescence-resonance energy transfer assay for identifying inhibitors of hepatitis C virus core dimerization.
  Kota S, Scampavia L, Spicer T, Beeler AB, Takahashi V, Snyder JK, Porco JA, Hodder P, Strosberg AD.
  -Department of Infectology 
  Binding of hepatitis C virus (HCV) RNA to core, the capsid protein, results in the formation of the nucleocapsid, the first step in the assembly of the viral particle. 
  
  
• Curr Opin Lipidol. 2010 Jun;21(3):204-11. 
  Ligand regulation of retinoic acid receptor-related orphan receptors: implications for development of novel therapeutics.
  Solt LA, Griffin PR, Burris TP.
  -Department of Molecular Therapeutics 
  In the late 1980s, the cloning of several nuclear receptors led to the intense search and isolation of new members of this superfamily. Despite their identification, many of these receptors were dubbed 'orphan' receptors, as their physiological ligands remained unknown. 
  
  
• Org Lett. 2010 Apr 20. [Epub ahead of print] 
  Enantioselective Synthesis of alpha-Methylene-beta-hydroxy Carboxylic Acid Derivatives via a Diastereoselective Aldol/beta-Elimination Sequence: Application to the C(15)-C(21) Fragment of Tedanolide C.
  Barth R, Roush WR.
  -Department of Chemistry 
  An enantioselective synthesis of alpha-methylene-beta-hydroxy carboxylic acid derivatives via a highly diastereoselective, one-pot syn-aldol and beta-elimination sequence utilizing the chiral beta-(phenylselenyl)propionyl imide 15 is described.
  
  
• J Biol Chem. 2010 Jan 22;285(4):2221-6. Epub 2009 Dec 2. 
  No Splicing, no dicing: non-proteolytic roles of the ubiquitin-proteasome system in transcription.
  Kodadek T.
  -Department of Chemistry 
  The ubiquitin-proteasome pathway (UPP) is responsible for most programmed turnover of proteins in eukaryotic cells, and this activity has been known for some time to be involved in transcriptional regulation. 
  
  
• Angew Chem Int Ed Engl. 2010;49(5):912-7. 
  Anion-exchange-triggered 1,3-shift of an NH proton to iridium in protic n-heterocyclic carbenes: hydrogen-bonding and ion-pairing effects.
  Song G, Su Y, Periana RA, Crabtree RH, Han K, Zhang H, Li X.
  -Department of Chemistry
  
  
• Cell. 2010 Feb 19;140(4):456-8. 
  Rac in the act of forgetting.
  Davis RL.
  -Department of Neuroscience 
  Forgetting has been thought to occur as a result of the natural decay of the neuronal changes induced by learning or because of interference from other cognitive functions 
  
  
• J Biol Chem. 2010 Feb 26;285(9):6761-9. Epub 2009 Dec 28. 
  Activation domain-dependent degradation of somatic Wee1 kinase.
  Owens L, Simanski S, Squire C, Smith A, Cartzendafner J, Cavett V, Caldwell Busby J, Sato T, Ayad NG.
  -Department of Cancer Biology 
  Cell cycle progression is dependent upon coordinate regulation of kinase and proteolytic pathways. 
  
  
• Nat Neurosci. 2010 May;13(5):635-41. Epub 2010 Mar 28. 
  Dopamine D2 receptors in addiction-like reward dysfunction and compulsive eating in obese rats
  Johnson PM, Kenny PJ.
  -Laboratory of Behavioral and Molecular Neuroscience, Department of Molecular Therapeutic 
  We found that development of obesity was coupled with emergence of a progressively worsening deficit in neural reward responses. 
  
  
• Mol Cancer Res. 2010 Mar;8(3):353-62. Epub 2010 Mar 2. 
  Skp2 directs Myc-mediated suppression of p27Kip1 yet has modest effects on Myc-driven lymphomagenesis.
  Old JB, Kratzat S, Hoellein A, Graf S, Nilsson JA, Nilsson L, Nakayama KI, Peschel C, Cleveland JL, Keller UB.
  -Department of Biochemistry, St. Jude Children's Research Hospital 
  The universal cyclin-dependent kinase inhibitor p27(Kip1) functions as a tumor suppressor, and reduced levels of p27(Kip1) connote poor prognosis in several human malignancies.
  
  
• Brain Res. 2010 Jun 18;1338:89-99. Epub 2010 Mar 18. Review. 
  MicroRNA dysregulation in psychiatric disease.
  Miller BH, Wahlestedt C.
  -Department of Neuroscience 
  MicroRNAs (miRNAs) are small regulatory RNAs that individually regulate up to several hundred genes, and collectively may regulate as much as two-thirds of the transcriptome.
  
  
• Nat Biotechnol. 2010 Mar;28(3):241-2. 
  Navigating genomic maps of cancer cells.
  van der Brug MP, Wahlestedt C.
  -Departments of Neuroscience and Molecular Therapeutics 
  
  
• J Proteome Res. 2009 Nov;8(11):5253-63. 
  Mapping the phosphorylation sites of Ulk1.
  Dorsey FC, Rose KL, Coenen S, Prater SM, Cavett V, Cleveland JL, Caldwell-Busby J.
  - Department of Cancer Biology 
  Ulk1 is a serine/threonine kinase that controls macroautophagy, an essential homeostatic recycling pathway that degrades bulk cytoplasmic material and directs the turnover of organelles such as peroxisomes and mitochondria. 
  
  
• Nat Chem Biol. 2010 Mar;6(3):162-165. 
  Rethinking screening
  Kodadek T.
  - Department of Chemistry and the Department of Cancer Biology 
  Bioactive compounds are most frequently identified via high-throughput screening campaigns.;
  
  
• Mol Pharmacol.2010 Jan;77(1):46-57.Epub 2009 Oct 16.PMID: 19837904. 
  Selective and brain penetrant neuropeptide Y Y2 receptor antagonists discovered by whole-cell high-throughput screening
  Brothers SP, Saldanha SA, Spicer TP, Cameron M, Mercer BA, Chase P, McDonald P, Wahlestedt C, Hodder PS
  - The Scripps Research Institute, Jupiter, Florida
  
  
• Diabetes. 2010 Feb;59(2):323-9. 
  A recurring problem with the analysis of energy expenditure in genetic models expressing lean and obese phenotypes.
  Butler AA, Kozak LP.
  - Department of Metabolism and Aging
  
  
• Mol Pharmacol. 2010 Jan;77(1):46-57. Epub 2009 Oct 16. 
  Selective and brain penetrant neuropeptide y y2 receptor antagonists discovered by whole-cell high-throughput screening
  Brothers SP, Saldanha SA, Spicer TP, Cameron M, Mercer BA, Chase P, McDonald P, Wahlestedt C, Hodder PS.
  - Department of Neuroscience 
  The role of neuropeptide Y Y2 receptor (Y2R) in human diseases such as obesity, mood disorders, and alcoholism could be better resolved by the use of small-molecule chemical probes that are substantially different from the currently available Y2R antagonist....
  
  
• Curr Opin Cell Biol. 2010 Apr;22(2):218-25. Epub 2010 Jan 22. 
  Targeting the autophagy pathway for cancer chemoprevention.
  Steeves MA, Dorsey FC, Cleveland JL.
  - Department of Cancer Biology, Scripps Florida 
  Autophagy is crucial for maintaining cellular homeostasis, coping with metabolic stress, and limiting oxidative damage. 
  
  
• Bioorg Med Chem Lett.2010 Apr 1;20(7):2254-8.Epub 2010 Feb 6. PMID: 20207142 
  TOxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9) 
  Bachovchin DA, Wolfe MR, Masuda K, Brown SJ, Spicer TP, Fernandez-Vega V, Chase P, **Hodder PS, Rosen H, Cravatt BF
  - **Scripps Florida 
  We recently described a fluorescence polarization platform for competitive activity-based protein profiling (fluopol-ABPP) that enables high-throughput inhibitor screening for enzymes with poorly characterized biochemical activity.
  
  
• Chem Biol.2010 Feb 26;17(2):135-48.PMID: 20189104 
  Small molecule activators of TRPML3
  Grimm C, Jörs S, Saldanha SA, Obukhov AG, Pan B, Oshima K, Cuajungco MP, Chase P, **Hodder P, Heller S
  - **Scripps Florida 
  We conducted a high-throughput screen for small molecule activators of the TRPML3 ion channel, which, when mutated, causes deafness and pigmentation defects. 
  
  
• Assay Drug Dev Technol. 2010 Feb;8(1):47-62.PMID: 20085455. 
  Multiplexed random peptide library and phospho-specific antibodies facilitate human polo-like kinase 1 inihibor screen.
  Tanaka K, Koresawa M, Iida M, Fukasawa K, Stec EM, Cassaday J, Chase P, Rickert K, **Hodder P, Takagi T, Komatani H
  - **Translational Research Institute, Scripps Florida 
  One of the challenges to develop time-resolved fluorescence resonance energy transfer (TR-FRET) assay for serine/threonine (Ser/Thr) protein kinase is to select an optimal peptide substrate and a specific phosphor Ser/Thr antibody.
  
  
• Mol Biosyst. 2010 Jan;6(1):92-7. Epub 2009 Sep 29. 
  Rapid identification of orexin receptor binding ligands using cell-based screening accelerated with magnetic beads.
  Qi X, Astle J, Kodadek T.
  - Department of Chemistry, Scripps Florida 
  We report here a simple and rapid method by which to screen one bead one compound libraries for highly specific ligands to cell surface proteins such as G protein-coupled receptors.
• Science. 2010 Feb 12;327(5967):869-72. Epub 2009 Dec 31. 
  Darwinian Evolution of Prions in Cell Culture.
  Li J, Browning S, Mahal SP, Oelschlegel AM, Weissmann C.
  - Department of Infectology, Scripps Florida 
  Prions are infectious proteins consisting mainly of PrP(Sc), a beta sheet-rich conformer of the normal host protein PrP(C),( )and occur in different strains. Strain identity is thought to be encoded by PrP(Sc) conformation. 
  
  
• Anal Chem. 2010 Jan 8. [Epub ahead of print] 
  Dynamics of the beta(2)-Adrenergic G-Protein Coupled Receptor Revealed by Hydrogen-Deuterium Exchange
  Zhang X, Chien EY, Chalmers MJ, Pascal BD, Gatchalian J, Stevens RC, Griffin PR.
  - Department of Molecular Therapeutics, The Scripps Research Institute, Jupiter, Florida and Department of Molecular Biology, The Scripps Research Institute, La Jolla, California 
  To examine the molecular details of ligand activation of G-protein coupled receptors (GPCRs), emphasis has been placed on structure determination of these receptors with stabilizing ligands.
  
  
• Transfusion. [Epub ahead of print] 
  Evaluation of removal of prion infectivity from red blood cells with prion reduction filters using a new rapid and highly sensitive cell culture-based infectivity assay.
  Sowemimo-Coker SO, Demczyk CA, Andrade F, Baker CA.
  - Pall Medical R&D, Port Washington, New York; and the Department of Infectology, Scripps Florida, Jupiter, Florida. 
  The clearance of infectious prions from biologic fluids is usually quantified by bioassays based on intracerebral inoculation of hamsters or mice; these tests are slow, cumbersome, imprecise, and very expensive.
  
  
• J Med Chem. 2010 Jan 14;53(1):419-31 
  Synthesis, Biological Evaluation, X-ray Structure, and Pharmacokinetics of Aminopyrimidine c-jun-N-terminal Kinase (JNK) Inhibitors.
  Kamenecka T, Jiang R, Song X, Duckett D, Chen W, Ling YY, Habel J, Laughlin JD, Chambers J, Figuera-Losada M, Cameron MD, Lin L, Ruiz CH, Lograsso PV.
  - Department of Molecular Therapeutics, and Translational Research Institute, 
  Given the significant body of data supporting an essential role for c-jun-N-terminal kinase (JNK) in neurodegenerative disorders, we set out to develop highly selective JNK inhibitors with good cell potency and good brain penetration properties.
  
  
• Nature. 2011 Jan 30. [Epub ahead of print] PMID: 21278726
  Habenular α5 nicotinic receptor subunit signalling controls nicotine intake.
  Fowler CD, Lu Q, Johnson PM, Marks MJ, Kenny PJ.
  - Laboratory for Behavioral and Molecular Neuroscience, Department of Molecular Therapeutics
  Genetic variation in CHRNA5, the gene encoding the α5 nicotinic acetylcholine receptor subunit, increases vulnerability to tobacco addiction and lung cancer, but the underlying mechanisms are unknown.
  
  
• Stem Cells. 2011 Jan;29(1):3-4. doi: 10.1002/stem.553. PMID: 2128015
  Twist, Epithelial-to-Mesenchymal Transition, and Stem Cells.
  Phinney DG.
  - *Department of Molecular Therapeutics
  
  
• BIOLOGY OF REPRODUCTION : 94-94 196 Suppl. S 2010
  The CREB Coactivator CRTC1 Is Required for Energy Balance and Fertility
  Altarejos, JY; Goebel, N; *Conkright, MD; Inoue, H; Xie, JX; Arias, CM; Sawchenko, PE; Montminy, M
  - *Department of Cancer Biology
  
  
• Cell. 2011 Jan 7;144(1):132-42. PMID: 21215375
  Identification of Candidate IgG Biomarkers for Alzheimer's Disease via Combinatorial Library Screening.
  Reddy MM, Wilson R, Wilson J, Connell S, Gocke A, Hynan L, German D, Kodadek T.
  - Opko Health Laboratories
  The adaptive immune system is thought to be a rich source of protein biomarkers, but diagnostically useful antibodies remain unknown for a large number of diseases. 
  
  
• Bioinformatics. 2011 Jan 6. [Epub ahead of print] PMID: 21216779
  A Java API for working with PubChem data-sets.
  Southern M, Griffin P.
  - Translational Research Institute and Molecular Therapeutics,
  PubChem is a public repository of chemical structures and associated biological activities. 

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