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• Org Lett. 2009 Nov 5;11(21):4982-5.
  Convergent synthesis of piperidines by the union of conjugated alkynes with imines: a unique regioselective bond construction for heterocycle synthesis.
  Chen MZ, Micalizio GC.
  - Department of Chemistry, Scripps Florida
  A two-step process is described for the union of aromatic imines, conjugated alkynes, and aldehydes that results in a stereoselective synthesis of highly substituted piperidines.
  
  
• J Biol Chem. 2009 Dec 28. [Epub ahead of print]
  Activation domain dependent degradation of somatic Wee1 kinase.
  Owens L, Simanski S, Squires C, Smith A, Cartzendafner J, Cavett V, Busby JC, Sato T, Ayad NG.
  - Scripps Florida
  Cell cycle progression is dependent upon coordinate regulation of kinase and proteolytic pathways. Inhibitors of cell cycle transitions are degraded to allow progression into the subsequent cell cycle phase.
  
  
• 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.
  
  
• 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 Med Chem. 2009 Nov 30. [Epub ahead of print]
  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.
  
  J Am Chem Soc. 2009 Dec 9;131(48):17548-9.
  A convergent stereoselective synthesis of quinolizidines and indolizidines: chemoselective coupling of 2-hydroxymethyl-substituted allylic silanes with imines.
  Yang D, Micalizio GC.
  - Department of Chemistry
  A convergent synthesis of stereodefined indolizidines and quinolizidines through chemoselective allyl transfer between 2-hydroxymethyl-substituted allylic silanes and imines is described.
  
  
• J Am Chem Soc. 2009 Nov 5. [Epub ahead of print]
  Product Protection, the Key to Developing High Performance Methane Selective Oxidation Catalysts.
  Ahlquist M, Nielsen RJ, Periana RA, Goddard III WA.
  - Department of Chemistry
  Selective, direct conversion of methane to methanol might seem an impossible task since the C-H bond energy of methane is 105 kcal mol(-1) compared to the C-H bond energy for methanol of 94. We show here that the Catalytica catalyst is successful because the methanol is protected as methyl bisulfate, which is substantially less reactive than methanol toward the catalyst.
  
  
• Org Lett. 2009 Dec 3;11(23):5402-5
  Convergent Synthesis of Stereodefined exo-Alkylidene-gamma-Lactams from beta-Halo Allylic Alcohols.
  Umemura S, McLaughlin M, Micalizio GC.
  - Department of Chemistry
  A convergent process for the assembly of stereodefined mono- and bicyclic exo-alkylidene-gamma-lactams is described that proceeds through the union of beta-halo allylic alcohols, aromatic imines, and CO. Overall, regio- and stereoselective Ti-mediated reductive cross-coupling, followed by Pd-catalyzed carbonylation, can be performed in a one- or two-pot procedure, defining a highly selective three-component coupling process for heterocycle synthesis.
  
  
• Cell Mol Life Sci. 2010 Jan;67(2):171-7. Epub 2009 Nov 12.
  Rho-kinase inhibitors as therapeutics: from pan inhibition to isoform selectivity.
  Hahmann C, Schroeter T.
  - Discovery Biology, Translational Research Institute
  The emerging critical implications of Rho/Rho-kinase (ROCK) signaling in neurodegenerative diseases, glaucoma, renoprotection, diabetes and cancer have sparked growing interest in the pharmacological potential of ROCK inhibitors beyond their current application in cardiovascular disease.
  
  
• Obes Rev. 2009 Nov;10 Suppl 2:14-24.
  The role of melanocortin neuronal pathways in circadian biology: a new homeostatic output involving melanocortin-3 receptors?
  Begriche K, Sutton GM, Fang J, Butler AA.
  - Department of Metabolism and Aging,
  Obesity, insulin resistance and increased propensity for type 2 diabetes and cardiovascular disease result from an imbalance between energy intake and expenditure. The cloning of genes involved in energy homeostasis produced a simple feedback model for the homeostatic regulation of adipose mass.
  
  
• Org Lett. 2009 Dec 3;11(23):5538-41.
  Origin of Thermodynamic versus Kinetic Control of Allene Hydroboration with 9-Borabicyclo[3.3.1]nonane and 10(R)-Trimethylsilyl-9-Borabicyclo[3.3.2]decane.
  Ess DH, Kister J, Chen M, Roush WR.
  - Department of Chemistry
  Density functional theory was used to locate transition states for hydroboration reactions of allenes with 9-borabicyclo[3.3.1]nonane and 10-R-9-borabicyclo[3.3.2]decane, as well as transition states for [1,3]-boratropic shift and aldehyde addition reactions of the derived allylboranes.
  
  
• Mol Pharmacol. 2009 Nov 10. [Epub ahead of print]
  The benzenesulfonamide T0901317 is a novel ROR{alpha}/{gamma} Inverse Agonist.
  Kumar N, Solt LA, Conkright JJ, Wang Y, Istrate MA, Busby SA, Garcia-Ordonez R, Burris TP, Griffin PR.
  - Department of Molecular Therapeutics,
  Retinoic acid receptor-related orphan receptors (RORs) regulate a variety of physiological processing including hepatic gluconeogenesis, lipid metabolism, circadian rhythm and immune function.
  
  
• FASEB J. 2009 Oct 16. [Epub ahead of print]
  Central nervous system melanocortin-3 receptors are required for synchronizing metabolism during entrainment to restricted feeding during the light cycle.
  Sutton GM, Begriche K, Kumar KG, Gimble JM, Perez-Tilve D, Nogueiras R, McMillan RP, Hulver MW, Tschöp MH, *Butler AA.
  - *Department of Metabolism and Aging,
  Melanocortin-3 receptors (Mc3rs) in the central nervous system are involved in expression of anticipatory rhythms and synchronizing clocks maintaining circadian rhythms during restricted feeding (RF) [mice housed under a 12-h light-dark cycle with lights on between zeitgeber time (ZT) 0 to ZT12 fed 60% of normal calories between ZT7 and ZT11].
  
  
• J Org Chem. 2009 Nov 20;74(22):8626-37.
  Quantum-Mechanical Study of 10-R-9-borabicyclo[3.3.2]decane Alkene Hydroboration.
  Ess DH, Kister J, Chen M, Roush WR.
  - Department of Chemistry
  Density functional theory and correlated ab initio quantum mechanical methods were used to locate and analyze alkene hydroboration transition structures for 10-R-9-borabicyclo[3.3.2]decane reagents.
  
  
• Bioorg Med Chem Lett. 2009 Dec 1;19(23):6686-90. [Epub ahead of print]
  Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors.
  Yin Y, Lin L, Ruiz C, Cameron MD, Pocas J, Grant W, Schröter T, Chen W, Duckett D, Schürer S, Lograsso P, Feng Y.
  - Translational Research Institute and Department of Molecular Therapeutics
  A series of benzothiazole derivatives as ROCK inhibitors have been discovered.
  
  
• Org Lett. 2009 Oct 30. [Epub ahead of print]
  Convergent Synthesis of Stereodefined exo-Alkylidene-gamma-Lactams from beta-Halo Allylic Alcohols.
  Umemura S, McLaughlin M, Micalizio GC.
  - Department of Chemistry
  A convergent process for the assembly of stereodefined mono- and bicyclic exo-alkylidene-gamma-lactams is described that proceeds through the union of beta-halo allylic alcohols, aromatic imines, and CO.
  
  
• Org Lett. 2009 Oct 15;11(20):4596-9.
• Cell Metab. 2009 Aug;10(2):82-3.
  From GH to Billy Ghrelin.
  Smith RG.
  - Department of Metabolism and Aging
  The octanoylated peptide hormone ghrelin regulates episodic growth hormone release and energy balance.
  
  
• Org Lett. 2009 Oct 15;11(20):4596-9.
  Aliphatic imines in titanium-mediated reductive cross-coupling: unique reactivity of Ti(O-i-Pr)4/n-BuLi.
  Tarselli MA, Micalizio GC.
  - Department of Chemistry
  A procedure for the coupling of aliphatic imines with allylic and allenic alkoxides is described.
  
  
• Bioorg Med Chem. 2009 Jul 15;17(14):5027-37. Epub 2009 Jun 22.
  Inhibitors of VIM-2 by screening pharmacologically active and click-chemistry compound libraries.
  Minond D, Saldanha SA, Subramaniam P, Spaargaren M, Spicer T, Fotsing JR, Weide T, Fokin VV, Sharpless KB, Galleni M, Bebrone C, Lassaux P, Hodder P.
  - Lead Identification, Translational Research Institute
  VIM-2 is an Ambler class B metallo-beta-lactamase (MBL) capable of hydrolyzing a broad-spectrum of beta-lactam antibiotics.
  
  
• EMBO J. 2009 Sep 16;28(18):2733-47. Epub 2009 Jul 30.
  Bipartite functions of the CREB co-activators selectively direct alternative splicing or transcriptional activation.
  Amelio AL, Caputi M, Conkright MD.
  - Department of Cancer Biology
  The CREB regulated transcription co-activators (CRTCs) regulate many biological processes by integrating and converting environmental inputs into transcriptional responses.
  
  
• Chem Res Toxicol. 2009 Oct;22(10):1736-42.
  Bioactivation of the Epidermal Growth Factor Receptor Inhibitor Gefitinib: Implications for Pulmonary and Hepatic Toxicities.
  Li X, Kamenecka TM, Cameron MD.
  - Translational Research Institute and Department of Molecular Therapeutics
  Gefitinib is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase and has been approved for the treatment of nonsmall cell lung cancer refractory to established cancer treatments.
  
  
• J Org Chem. 2008 Dec 19;73(24):9657-67.
  Total synthesis of (+)-superstolide A..
  Tortosa M, Yakelis NA, Roush WR..
  - Department of Chemistry
  A convergent and highly stereocontrolled total synthesis of the cytotoxic macrolide (+)-superstolide A is described.
  
  
• J Org Chem. 2009 Oct 2;74(19):7595-7.
  Efficient Methodology for the Synthesis of 3-Amino-1,2,4-triazoles.
  Noël R, Song X, Jiang R, Chalmers MJ, Griffin PR, Kamenecka TM.
  - Department of Molecular Therapeutics and Translational Research Institute
  A general and efficient method for the preparation of 3-amino-1,2,4-triazoles has been developed.
  
  
• Cancer Res. 2009 Sep 22. [Epub ahead of print]
  Epidermal Growth Factor Receptor Variant III-Induced Glioma Invasion Is Mediated through Myristoylated Alanine-Rich Protein Kinase C Substrate Overexpression.
  Micallef J, Taccone M, Mukherjee J, Croul S, Busby J*, Moran MF, Guha A.
  - Arthur & Sonia Labatt Brain Tumor Center and Program in Molecular Structure and Function, Hospital for Sick Children; Departments of Pathology and Laboratory Medicine and Pathobiology, University Health Network, Division of Neurosurgery, Western Hospital, and McLaughlin Centre for Molecular Medicine and Department of Molecular Genetics, University of Toronto, Toronto, Ontario, Canada; and
  * Department of Molecular Therapeutics, The Scripps Research Institute, Jupiter, Florida
  Glioblastoma multiforme (GBM) is the most common and most malignant adult brain tumor.
  
  
• Drug Metab Dispos. 2009 Jun;37(6):1269-76. Epub 2009 Mar 26.
  Expression quantitative trait loci mapping identifies new genetic models of glutathione S-transferase variation.
  Hayes KR, Young BM, Pletcher MT.
  - Department of Molecular Therapeutics,
  Expression quantitative trait loci (eQTL) mapping can be used to identify the genetic variations that underlie inherited differences in gene transcription.
  
  
• J Clin Endocrinol Metab.2009 Jun;94(6):2178-83.Epub 2009 Mar 24.PMID: 19318454
  Inhibition of adrenocortical carcinoma cell proliferation by steroidogenic factor-1 inverse agonists
  Doghman M, Cazareth J, Douguet D, Madoux F, Hodder P, Lalli E
  - The Scripps Research Institute, Jupiter, Florida
• J Am Chem Soc. 2009 Oct 21;131(41):14602-3.
  Enantioselective Synthesis of 2-Methyl-1,2-syn- and 2-Methyl-1,2-anti-3-butenediols via Allene Hydroboration-Aldehyde Allylboration Reaction Sequences.
  Chen M, Handa M, Roush WR.
  - Department of Chemistry
  The hydroboration of allene 7 with ((d)Ipc)(2)BH at 0 degrees C provides the kinetic allylborane 12Z with >20:1 selectivity.
  
  
• Nat Rev Mol Cell Biol. 2009 Sep;10(9):637-43. Epub 2009 Jul 29.
  Regulatory roles of natural antisense transcripts.
  Faghihi MA, Wahlestedt C.
  - Molecular and Integrative Neurosciences Department
  Mammalian genomes encode numerous natural antisense transcripts, but the function of these transcripts is not well understood.
  
  
• Biochemistry.2009 Oct 13;48(40):9668-76.
  Unique Ligand Binding Patterns Between Estrogen Receptor and Revealed by Hydrogen/Deuterium Exchange.
  Dai SY, Burris TP, Dodge JA, Montrose-Rafizadeh C, Wang Y, Pascal BD, Chalmers MJ, Griffin PR
  - Department of Molecular Therapeutics, The Scripps Research Institute, Jupiter, Florida
  Here we present the use of hydrogen/deuterium exchange (HDX) mass spectrometry to analyze the estrogen receptor beta ligand binding domain (ERbetaLBD) in the absence and presence of a variety of chemical compounds with different binding modes and pharmacological properties.
  
  
• Biochemistry, 2009, 48 (31), pp 7365-7372
  Apo-Human Carbonic Anhydrase II Revisited: Implications of the Loss of a Metal in Protein Structure, Stability and Solvent Network.
  Balendu Sankara Avvaru, Scott A. Busby,* Michael J. Chalmers,* Patrick R. Griffin,* Balasubramanian Venkatakrishnan, Mavis Agbandje-McKenna, David N. Silverman and Robert McKenna.
  - Department of Biochemistry and Molecular Biology, Department of Pharmacology and Therapeutics University of Florida, Gainesville, Florida; *Department of Molecular Therapeutics, The Scripps Research Institute, Jupiter, Florida
  Human carbonic anhydrase II (HCA II) is a monomeric zinc-containing metalloenzyme that catalyzes the hydration of CO2 to form bicarbonate and a proton.
  
  
• Nat Rev Mol Cell Biol. 2009 Jul 29. [Epub ahead of print]
  Thoughts on mammalian prion strains.
  Faghihi MA, Wahlestedt C.
  - Molecular and Integrative Neurosciences Department
  Mammalian genomes encode numerous natural antisense transcripts, but the function of these transcripts is not well understood.
  
  
• Folia Neuropathol. 2009;47(2):104-13.
  Thoughts on mammalian prion strains.
  Weissmann C.
  - Department of Infectology
  A plethora of prion strains can be propagated indefinitely in hosts homozygous for the PrP gene.
  
  
• PLoS One. 2009 May 29;4(5):e5730
  Inhibitors of VIM-2 by screening pharmacologically active and click-chemistry compound libraries.
  Karapetyan YE, Saá P, Mahal SP, Sferrazza GF, Sherman A, Salès N, Weissmann C, Lasmézas CI.
  - Department of Infectology
  Prion strain discrimination based on rapid in vivo amplification and analysis by the cell panel assay
  
  
• Bioorg Med Chem. 2009 Jun 22. [Epub ahead of print]
  Inhibitors of VIM-2 by screening pharmacologically active and click-chemistry compound libraries.
  Minond D, Saldanha SA, Subramaniam P, Spaargaren M, Spicer T, Fotsing JR, Weide T, Fokin VV, Sharpless KB, Galleni M, Bebrone C, Lassaux P, Hodder P.
  - Lead Identification, Translational Research Institute
  VIM-2 is an Ambler class B metallo-beta-lactamase (MBL) capable of hydrolyzing a broad-spectrum of beta-lactam antibiotics.
  
  
• J Gen Virol. 2009 Mar 4. [Epub ahead of print]
  Peptide inhibitors of Hepatitis C virus core oligomerization and virus production.
  Kota S, Coito C, Mousseau G, Lavergne JP, Strosberg AD.
  - Department of Infectology
  Hepatitis C Virus (HCV) nucleocapsid assembly requires dimerization of the core protein, an essential step in the formation of the viral particle.
  
  
• Angew Chem Int Ed Engl. 2009;48(20):3648-52
  Complex allylation by the direct cross-coupling of imines with unactivated allylic alcohols.
  Takahashi M, McLaughlin M, Micalizio GC.
  - Department of Chemistry
  Regioselective, stereoselective: The convergent coupling of allylic alcohols with imines to deliver stereodefined homoallylic amines is described (see scheme).
  
  
• PLoS ONE. 2009 May 29;4(5):e5730
  Prion strain discrimination based on rapid in vivo amplification and analysis by the cell panel assay.
  Karapetyan YE, Saá P, Mahal SP, Sferrazza GF, Sherman A, Salès N, Weissmann C, Lasmézas CI.
  - Department of Infectology
  Prion strain identification has been hitherto achieved using time-consuming incubation time determinations in one or more mouse lines and elaborate neuropathological assessment.
  
  
• Bioorg Med Chem Lett. 2009 Jun 15;19(12):3344-7. Epub 2009 Mar 26Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors.
  Shin Y, Chen W, Habel J, Duckett D, Ling YY, Koenig M, He Y, Vojkovsky T, Lograsso P, Kamenecka TM.
  - Department of Molecular Therapeutics and Translational Research Institute
  A novel series of c-jun N-terminal kinase (JNK) inhibitors were designed and developed from a high-throughput-screening hit.
  
  
• Bioorg Med Chem Lett. 2008 Dec 15;18(24):6390-3. Epub 2008 Oct 25. Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.
  Sessions EH, Yin Y, Bannister TD, Weiser A, Griffin E, Pocas J, Cameron MD, Ruiz C, Lin L, Schürer SC, Schröter T, LoGrasso P, Feng Y.
  - Department of Molecular Therapeutics
  Inhibitors of Rho kinase have been developed based on two distinct scaffolds, benzimidazoles, and benzoxazoles.
  
  
• J Neuroendocrinol. 2009 Feb;21(2):83-9. Epub 2008 Dec 6.
  Diminished metabolic responses to centrally-administered apelin-13 in diet-induced obese rats fed a high-fat diet.
  Clarke KJ, Whitaker KW, Reyes TM.
  - Department of Molecular Therapeutics
  The central administration of apelin, a recently identified adipokine, has been shown to affect food and water intake.
  
  
• Proc Natl Acad Sci U S A. 2009 Mar 3;106(9):3507-12. Epub 2009 Feb 5.
  Monitoring the autophagy pathway in cancer.
  Dorsey FC, Steeves MA, Prater SM, Schröter T, Cleveland JL.
  - Department of Cancer Biology
  Autophagy is an ancient cell survival pathway that is induced by metabolic stress and that helps prevent bioenergetic failure.
  
  
• Methods Enzymol. 2009;453:251-71.
  MicroRNA-219 modulates NMDA receptor-mediated neurobehavioral dysfunction.
  Kocerha J, Faghihi MA, Lopez-Toledano MA, Huang J, Ramsey AJ, Caron MG, Sales N, Willoughby D, Elmen J, Hansen HF, Orum H, Kauppinen S, Kenny PJ, Wahlestedt C
  - Department of Molecular and Integrative Neurosciences
  N-methyl-D-aspartate (NMDA) glutamate receptors are regulators of fast neurotransmission and synaptic plasticity in the brain.
  
  
• J Biol Chem. 2009 Feb 13;284(7):4317-23. Epub 2008 Dec 1. The anaphase promoting complex induces substrate degradation during neuronal differentiation.
  Harmey D, Smith A, Simanski S, Zaki Moussa C, Ayad NG.
  - Department of Cancer Biology
  The Anaphase Promoting Complex (APC) is an E3 ubiquitin ligase required for the metaphase to anaphase transition and mitotic exit.
  
  
• J Am Chem Soc. 2008 Dec 3;130(48):16407-16.
  Total syntheses of (+)-tedanolide and (+)-13-deoxytedanolide.
  Dunetz JR, Julian LD, Newcom JS, Roush WR.
  - Department of Chemistry
  Convergent total syntheses of the potent cytotoxins (+)-tedanolide (1) and (+)-13-deoxytedanolide (2) are described.
  
  
• Prion. 2007 Jul;1(3):198-206. Epub 2007 Jul 15.
  Toxic effects of intracerebral PrP antibody administration during the course of BSE infection in mice.
  Lefebvre-Roque M, Kremmer E, Gilch S, Zou WQ, Féraudet C, Gilles CM, Salès N, Grassi J, Gambetti P, Baron T, Schätzl H, Lasmézas CI.
  - Department of Infectology
  The absence of specific immune response is a hallmark of prion diseases.
  
  
• Drug Metab Dispos. 2009 Jun;37(6):1242-50. Epub 2009 Mar 12.
  Characterization of dasatinib and its structural analogs as CYP3A4 mechanism based inactivators and the proposed bio-activation pathways.
  Li X, He Y, Ruiz CH, Koenig M, Cameron MD.
  - Translational Research Institute
  Dasatinib was approved in 2006 for the treatment of imatinib resistant chronic myelogenous leukemia and primarily functions through the inhibition of BCR/ABL and Src kinase.
  
  
• Methods Mol Biol. 2009;510:85-94.
  Purification and crystallization of NS5A domain I of hepatitis C virus.
  Marcotrigiano J, Tellinghuisen T.
  - Department of Infectology
  The NS5A protein of HCV is an essential component of the viral RNA replication machinery and may also function in modulation of the host cell environment.
  
  
• Methods Enzymol. 2009;453C:251-271.
  Chapter 12 Monitoring the Autophagy Pathway in Cancer.
  Dorsey FC, Steeves MA, Prater SM, Schröter T, Cleveland JL.
  - Department of Cancer Biology
  Autophagy is an ancient cell survival pathway that is induced by metabolic stress and that helps prevent bioenergetic failure.
  
  
• Cancer Res. 2009 Jan 15;69(2):547-53.
  Targeting ornithine decarboxylase impairs development of MYCN-amplified neuroblastoma.
  Rounbehler RJ, Li W, Hall MA, Yang C, Fallahi M, Cleveland JL.
  - Department of Cancer Biology
  Neuroblastoma is a pediatric malignancy that arises from the neural crest, and patients with high-risk neuroblastoma, which typically harbor amplifications of MYCN, have an extremely poor prognosis.
  
  
• J Am Chem Soc. 2009 Jan 22. [Epub ahead of print]
  Oxy-Functionalization of Nucleophilic Rhenium(I) Metal Carbon Bonds Catalyzed by Selenium(IV).
  Tenn WJ, Conley BL, Hövelmann CH, Ahlquist M, Nielsen RJ, Ess DH, Oxgaard J, Bischof SM, Goddard WA, Periana RA.
  - Scripps Energy Laboratories, The Scripps Research Institute, UCLA, and California Institute of Technology
  We report that SeO(2) catalyzes the facile oxy-functionalization of (CO)(5)Re(I)-Me(delta-) with IO(4)(-) to generate methanol.
  
  
• J Org Chem. 2009 Jan 13. [Epub ahead of print]
  Distortion, Interaction, and Conceptual DFT Perspectives of MO(4)-Alkene (M = Os, Re, Tc, Mn) Cycloadditions.
  Ess DH.
  - Department of Chemistry
  The reaction pathways (including the transition states) of ethylene addition to osmium tetroxide (OsO(4), and amine ligated), rhenate (ReO(4)(-)), technetate (TcO(4)(-)), and permanganate (MnO(4)(-)) have been studied by qualitative and quantitative analyses.
  
  
• Proc Natl Acad Sci U S A. 2008 Dec 9;105(49):19480-5. Epub 2008 Nov 24.
  Insular hypocretin transmission regulates nicotine reward.
  Hollander JA, Lu Q, Cameron MD, Kamenecka TM, Kenny PJ.
  - Department of Molecular Therapeutics
  Damage to the insular cortex can profoundly disrupt tobacco addiction in human smokers, reflected in spontaneous cessation of the tobacco habit and persistently decreased urge to smoke.
  
  
• Bioorg Med Chem Lett. 2008 Nov 15;18(22):5860-3.
  Synthesis of macrocyclic trypanosomal cysteine protease inhibitors.
  Chen YT, Lira R, Hansell E, McKerrow JH, Roush WR.
  - Department of Chemistry
  The importance of cysteine proteases in parasites, compounded with the lack of redundancy compared to their mammalian hosts makes proteases attractive targets for the development of new therapeutic agents.
  
  
• Org Lett. 2008 Oct 16;10(20):4613-6. Epub 2008 Sep 23.
  Studies on the synthesis of durhamycin A: stereoselective synthesis of a model aglycone.
  Pragani R, Roush WR
  - Department of Chemistry
  A stereoselective synthesis of the model aglycone corresponding to the anti-HIV aureolic acids durhamycins A (1) and B (2) is described.
  
  
• Curr Opin Drug Discov Devel. 2008 Nov;11(6):778-92.
  Applications of chiral allylmetallating agents toward the synthesis of oxygen heterocyles.
  Bates RH, Chen M, Roush WR.
  - Department of Chemistry
  Oxygen heterocycles represent an important structural feature in many biologically active natural products.
  
  
• J Med Chem. 2008 Nov 13;51(21):6642-5. Epub 2008 Oct 4.
  Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.
  Feng Y, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter T, Lograsso P.
  - Department of Molecular Therapeutics and Translational Research Institute
  The identification of a new class of potent and selective ROCK-II inhibitors is presented.
  
  
• J Neuroendocrinol. 2008 Dec 6. [Epub ahead of print]
  Diminished metabolic responses to centrally administered apelin-13 in diet-induced obese (DIO) rats fed a high fat diet.
  Clarke KJ, Whitaker KW, Reyes TM.
  - Department of Molecular Therapeutics
  The central administration of apelin, a recently identified adipokine, has been shown to affect food and water intake.
  
  
• Methods Mol Biol. 2009;510:165-75.
  Reverse Transcription PCR-Based Sequence Analysis of Hepatitis C Virus Replicon RNA.
  Tellinghuisen TL, Lindenbach BD.
  - Department of Infectology
  Since the advent of efficient cell-culture methods for HCV replication and, more recently, infection, there has been a need to efficiently sequence the viral RNA in these systems.
  
  
• Bioorg Med Chem Lett. 2008 Dec 15;18(24):6406-9. Epub 2008 Oct 22.
  Chroman-3-amides as potent Rho kinase inhibitors.
  Chen YT, Bannister TD, Weiser A, Griffin E, Lin L, Ruiz C, Cameron MD, Schürer S, Duckett D, Schröter T, Lograsso P, Feng Y.
  - Department of Molecular Therapeutics and Translational Research Institute
  Inhibition of Rho kinase (ROCK) is an attractive strategy for the treatment of diseases such as hypertension, glaucoma, and cancer.
  
  
• Org Lett. 2008 Oct 2;10(19):4343-6.
  Stereoselective syntheses of the C(1)-C(9) fragment of amphidinolide C.
  Bates RH, Shotwell JB, Roush WR.
  - Department of Chemistry
  Stereoselective syntheses of the C(1)-C(9) fragments 18 and 28 of amphidinolide C have been developed.
  
  
• Curr Opin Drug Discov Devel. 2008 Nov;11(6):778-92
  Applications of chiral allylmetallating agents toward the synthesis of oxygen heterocyles.
  Bates RH, Chen M, Roush WR.
  - Department of Chemistry
  Oxygen heterocycles represent an important structural feature in many biologically active natural products.
  
  
• J Med Chem. 2008 Oct 4. [Epub ahead of print]
  Discovery of Substituted 4-(Pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as Potent and Highly Selective Rho Kinase (ROCK-II) Inhibitors.
  Feng Y, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter T, Lograsso P
  - Department of Molecular Therapeutics, and Translational Research Institute
  The identification of a new class of potent and selective ROCK-II inhibitors is presented.
  
  
• ACS Chem Biol. 2008 Aug 15;3(8):486-98. Epub 2008 Jul 1
  Ligand-binding pocket shape differences between sphingosine 1-phosphate (S1P) receptors S1P1 and S1P3 determine efficiency of chemical probe identification by ultrahigh-throughput screening.
  Schürer SC, Brown SJ, Gonzalez-Cabrera PJ, Schaeffer MT, Chapman J, Jo E, Chase P, Spicer T, Hodder P, Rosen H.
  - Department of Scientific Computing
  We have studied the sphingosine 1-phosphate (S1P) receptor system to better understand why certain molecular targets within a closely related family are much more tractable when identifying compelling chemical leads.
  
  
• Arch Biochem Biophys. 2008 Sep 15;477(2):324-9. Epub 2008 Jun 5.
  Mechanistic characterization for c-jun-N-Terminal Kinase 1alpha1.
  Ember B, LoGrasso P.
  - Department of Molecular Therapeutics and Drug Discovery
  c-jun-N-terminal kinase 1alpha1 (JNK1alpha1) is a serine/threonine kinase of the mitogen-activated protein (MAP) kinase family that phosphorylates protein transcription factors after activation by a variety of environmental stressors.
  
  
• Nat Chem Biol. 2008 Apr;4(4):241-7. Epub 2008 Mar 16.
  NFκB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses.
  Nettles KW, Bruning JB, Gil G, Nowak J, Sharma SK, Hahm JB, Kulp K, Hochberg RB, Zhou H, Katzenellenbogen JA, Katzenellenbogen BS, Kim Y, Joachmiak A, Greene GL.
  - Department of Cancer Biology
  Our understanding of how steroid hormones regulate physiological functions has been significantly advanced by structural biology approaches.
  
  
• Biochem Biophys Res Commun. 2008 Sep 19;374(2):356-60. Epub 2008 Jul 16.
  Detection of myosin light chain phosphorylation--a cell-based assay for screening Rho-kinase inhibitors.
  Schröter T, Griffin E, Weiser A, Feng Y, LoGrasso P.
  - Translational Research Institute
  Here, we describe the first example of a cell-based myosin light chain phosphorylation assay in 96-well format that allows for the rapid screening of novel Rho-kinase inhibitors.
  
  
• Org Lett. 2008 Aug 7;10(15):3371-4. Epub 2008 Jun 28.
  Highly stereoselective and modular syntheses of 10-hydroxytrilobacin and three diastereomers via stereodivergent [3 + 2]-annulation reactions.
  Huh CW, Roush WR.
  - Department of Chemistry
  A convergent synthesis of the annonaceous acetogenin, 10-hydroxytrilobacin ( 4a), was accomplished by using the [3 + 2]-annulation reaction of tetrahydrofuranyl carboxaldehyde 2a and allylsilane 3.
  
  
• Nat Med. 2008 Jul;14(7):723-30. Epub 2008 Jun 29.
  Expression of a noncoding RNA is elevated in Alzheimer's disease and drives rapid feed-forward regulation of beta-secretase.
  Faghihi MA, Modarresi F, Khalil AM, Wood DE, Sahagan BG, Morgan TE, Finch CE, St Laurent G 3rd, Kenny PJ, Wahlestedt C.
  - Molecular and Integrative Neurosciences Department
  Recent efforts have revealed that numerous protein-coding messenger RNAs have natural antisense transcript partners, most of which seem to be noncoding RNAs.
  
  
• Neuropsychopharmacology. 2008 May;33(6):1312-22. Epub 2007 Jul 4.
  Genetic regulation of behavioral and neuronal responses to fluoxetine.
  Miller BH, Schultz LE, Gulati A, Cameron MD, Pletcher MT.
  - Department of Molecular Therapeutics
  Despite widespread use of antidepressants, the factors underlying the behavioral response to antidepressants are unknown.
  
  
• Behav Pharmacol. 2008 Sep;19(5-6):461-84.
  Subtypes of nicotinic acetylcholine receptors in nicotine reward, dependence, and withdrawal: evidence from genetically modified mice.
  Fowler CD, Arends MA, Kenny PJ.
  - Department of Molecular Therapeutics, Florida and Committee on the Neurobiology of Addictive Disorders, California, The Scripps Research Institute
  Neuronal nicotinic acetylcholine receptors (nAChRs) can regulate the activity of many neurotransmitter pathways throughout the central nervous system and are considered to be important modulators of cognition and emotion.
  
  
• PLoS ONE. 2008 Jan 23;3(1):e1486.
  A Novel RNA Transcript with Antiapoptotic Function Is Silenced in Fragile X Syndrome
  Khalil AM, Faghihi MA, Modarresi F, Brothers SP, Wahlestedt C.
  - Molecular and Integrative Neurosciences Department (MIND), The Scripps Research Institute, Jupiter, Florida
  Several genome-wide transcriptomics efforts have shown that a large percentage of the mammalian genome is transcribed into RNAs, however, only a small percentage (1-2%) of these RNAs is translated into proteins.
  
  
• Mini Rev Med Chem. 2008 Jul;8(8):755-66.
  Inhibitors of c-jun-N-Terminal Kinase (JNK).
  Lograsso P, Kamenecka T.
  - Department of Molecular Therapeutics and Drug Discovery
  Inhibitors of c-jun-N-Terminal Kinase (JNK) have many potential therapeutic indications ranging from neurodegenerative disease, to metabolic disorders, inflammation, cardiovascular disease, and cancer.
  
  
• Biochem Biophys Res Commun. 2008 Jul 16. [Epub ahead of print]
  Detection of myosin light chain phosphorylation-A cell-based assay for screening Rho-kinase inhibitors.
  Schröter T, Griffin E, Weiser A, Feng Y, Lograsso P.
  - Translational Research Institute
  Here, we describe the first example of a cell-based myosin light chain phosphorylation assay in 96-well format that allows for the rapid screening of novel Rho-kinase inhibitors.
  
  
• Org Lett. 2008 May 15;10(10):2059-62.
  Concerning the Synthesis of the Tedanolide C(13)—C(23) Fragment via Anti-Aldol Reaction
  Dunetz JR, Roush WR.
  - Department of Chemistry
  Synthesis of C(13)-C(23) aldehyde 4, an important intermediate in a planned total synthesis of tedanolide, is described...
  
  
• Nat Med. 2008 Jul;14(7):723-30.
  Expression of a noncoding RNA is elevated in Alzheimer's disease and drives rapid feed-forward regulation of beta-secretase.
  Faghihi MA, Modarresi F, Khalil AM, Wood DE, Sahagan BG, Morgan TE, Finch CE, St Laurent Iii G, Kenny PJ, Wahlestedt C.
  - Molecular and Integrative Neurosciences Department
  Recent efforts have revealed that numerous protein-coding messenger RNAs have natural antisense...
  
  
• Tetrahedron. 2007 Jun 25;63(26):5768-5796.
  Total Synthesis of Amphidinolide E and Amphidinolide E Stereoisomers.
  Va P, Roush WR.
  - Departments of Chemistry and Biochemistry
  Four amphidinolide E stereoisomers, amphidinolide E (1), 2-epi-amphidinolide E (2), 19-epi-amphidinolide E (3), and 2-epi-19-epi-amphidinolide E (4), have been synthesized...
  
  
• Methods Mol Biol. 2008;459:49-68.
  Assaying Prions in Cell Culture : The Standard Scrapie Cell Assay (SSCA) and the Scrapie Cell Assay in End Point Format (SCEPA).
  Mahal SP, Demczyk CA, Smith EW Jr, Klohn PC, Weissmann C.
  -Department of Infectology
  Prions are usually quantified by bioassays based on intracerebral inoculation of animals, which are slow, imprecise, and costly...
  
  
• Mol Cell Biol. 2008 Jun 23. [Epub ahead of print]
  Selection Against PUMA Gene Expression in Myc-Driven B Cell Lymphomagenesis.
  Garrison SP, Jeffers JR, Yang C, Nilsson JA, Hall MA, Rehg JE, Yue W, Yu J, Zhang L, Onciu M, Sample JT, Cleveland JL, Zambetti GP.
  -Department of Cancer Biology, The Scripps Research Institute-Florida, et al.
  The p53 tumor suppressor pathway limits oncogenesis by inducing cell cycle arrest or apoptosis. A key p53 target gene is PUMA...
  
  
• Proc Natl Acad Sci U S A. 2008 May 20;105(20):7171-6.
  Prediction of the tissue-specificity of selective estrogen receptor modulators by using a single biochemical method.
  Dai SY, Chalmers MJ, Bruning J, Bramlett KS, Osborne HE, Montrose-Rafizadeh C, Barr RJ, Wang Y, Wang M, Burris TP, Dodge JA, Griffin PR
  -Department of Molecular Therapeutics
  Here, we demonstrate that a single biochemical assay is able to predict the tissue-selective pharmacology of an array of selective estrogen receptor modulators (SERMs)..
  
  
• Bioorg Med Chem Lett. 2007 Nov 15;17(22):6378-82.
  3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors.
  Jiang R, Duckett D, Chen W, Habel J, Ling YY, LoGrasso P, Kamenecka TM
  -Department of Medicinal Chemistry
  The structure-based design and synthesis of a novel series of c-Jun N-terminal kinase (JNK) inhibitors ...
  
  
• Arch Biochem Biophys. 2008 Jun 5. [Epub ahead of print]
  Mechanistic characterization for c-jun-N-Terminal Kinase 1alpha1
  Ember B, Lograsso P.
  - Department of Molecular Therapeutics and Drug Discovery
  c-jun-N-terminal kinase 1alpha1 (JNK1alpha1) is a serine/threonine kinase...
  
  
• Mol Pharmacol. 2008 Jun;73(6):1776-84.
  Potent, selective and cell penetrant inhibitors of SF-1 by functional uHTS.
  Madoux F, Li X, Chase P, Zastrow G, Cameron MD, Conkright JJ, Griffin PR, Thacher S, Hodder P.
  -The Scripps Research Institute
  The Steroidogenic factor 1 (SF-1, also known as NR5A1) is a transcription factor belonging to the nuclear receptor superfamily...
  
  
• Assay Drug Dev Technol.2008 Jun;6(3):361-74.PMID: 18452391
  A fluorescence-based thiol quantification assay for ultra-high-throughput screening for inhibitors of coenzyme A production
  Chung CC, Ohwaki K, Schneeweis JE, Stec E, Varnerin JP, Goudreau PN, Chang A, Cassaday J, Yang L, Yamakawa T, Kornienko O,Hodder P, Inglese J, Ferrer M, Strulovici B, Kusunoki J, Tota MR, Takagi T
  -The Scripps Research Institute,, Jupiter, Florida
  
  
• Biochemistry. 2008 Mar 11;47(10):3076-84. Epub 2008 Feb 13.
  Kinetic mechanism and inhibitor characterization for c-jun-N-terminal kinase 3α1.
  Ember B, Kamenecka T, LoGrasso P.
  -epartment of Molecular Therapeutics and Drug Discovery
  c-jun-N-Terminal kinase 3α1 (JNK3α1) is a mitogen-activated protein (MAP) kinase family...


• Epigenetics. 2008 Jan 10;3(1). [Epub ahead of print]
  Epigenetic mechanisms of gene regulation during mammalian spermatogenesis.
  Khalil A.M., Wahlestedt C.
  -Molecular and Integrative Neurosciences Department (MIND)
  The process of spermatogenesis is a unique form of cellular differentiation...


• Bioorg Med Chem Lett. 2008 Apr 15;18(8):2628-32. Epub 2008 Mar 14
  Genomic variants at the PINK1 locus are associated with transcript abundance and plasma nonesterified fatty acid concentrations in European whites
  Franks PW, Scheele C, Loos RJ, Nielsen AR, Finucane FM, Wahlestedt C*, Pedersen BK, Wareham NJ, Timmons JA.
  -*Department of Biochemistry
  The purpose of this study was to characterize associations between PINK1 genotypes...


• Bioorg Med Chem Lett. 2008 Apr 15;18(8):2628-32. Epub 2008 Mar 14
  Concerning the synthesis of the tedanolide C(13)-C(23) fragment via anti-aldol reaction.
  Dunetz JR, Roush WR.
  -Department of Chemistry
  Synthesis of C(13)-C(23) aldehyde 4, an important intermediate...


• Org Lett. 2008 Feb 21;10(4):681-4. Epub 2008 Jan 19.
  Synthesis of the C(26)-C(42) and C(43)-C(67) pyran-containing fragments of amphidinol 3 via a common pyran intermediate.
  Hicks JD, Roush WR.
  -Department of Chemistry
  The pyran-containing fragments 1 and 2 of AM3 have been synthesized from...


• J Org Chem. 2008 Mar 7;73(5):1818-29. Epub 2008 Jan 24
  Total synthesis of (-)-spinosyn A: examination of structural features that govern the stereoselectivity of the key transannular Diels-Alder reaction.
  Winbush SM, Mergott DJ, Roush WR.
  -Department of Chemistry
  A study of elements of stereochemical control in transannular Diels-Alder reactions leading to the decahydro-as-indacene core...


• Pharmacol Biochem Behav. 2008 Apr 4 [Epub ahead of print]
  Decreased brain reward function during nicotine withdrawal in C57BL6 mice: Evidence from intracranial self-stimulation (ICSS) studies.
  Johnson PM, Hollander JA, Kenny PJ.
  -Department of Molecular Therapeutics
  Deficits in brain reward function during nicotine withdrawal may serve as an important substrate for negative reinforcement...


• Nucleic Acids Research, 2008 Apr 17 [Epub ahead of print]
  Analysis of siRNA specificity on targets with double-nucleotide mismatches.
  Dahlgren C, Zhang HY, Du Q, Grahn M, Norstedt G, Wahlestedt C, Liang Z.
  -Karolinska Institutet, Peking University, and Molecular and Integrative Neurosciences Department, Scripps Florida
  Although RNA interference as a tool for gene knockdown is a great promise for future applications, the specificity of small interfering RNA (siRNA)...


• Neuropsychopharmacology, 2008 Apr 16 [Epub ahead of print]
  NMDA Receptors Regulate Nicotine-Enhanced Brain Reward Function and Intravenous Nicotine Self-Administration: Role of the Ventral Tegmental Area and Central Nucleus of the Amygdala.
  Kenny PJ, Chartoff E, Roberto M, Carlezon WA Jr, Markou A.
  -Department of Molecular Therapeutics
  Nicotine is considered an important component of tobacco responsible for the smoking habit in humans. Nicotine increases glutamate-mediated transmission...


• Bioorg Med Chem Lett. 2008 Apr 15;18(8):2628-32.
  Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds.
  Roth J, Madoux F, Hodder P, Roush WR.
  -Department of Chemistry
  Three synthetic routes were developed for structure-activity relationship (SAR) studies...


• Addict Biol. 2008 Mar;13(1):88-94.
  Association between the nociceptin receptor gene (OPRL1) single nucleotide polymorphisms and alcohol dependence.
  Huang J, Young B, Pletcher MT, Heilig M, Wahlestedt C.
  -Molecular and Integrative Neurosciences Department
  OPRL1 encodes the nociceptin receptor, which has been shown to be involved in alcohol dependence in previous studies...


• PLoS Pathog. 2008 Mar 21;4(3):e1000032.
  Regulation of hepatitis C virion production via phosphorylation of the NS5A protein.
  Tellinghuisen TL, Foss KL, Treadaway J.
  - Department of Infectology
  Hepatitis C virus (HCV) is a significant pathogen, infecting some 170 million people worldwide...
  
  
• Bioorg Med Chem. 2008 Mar 6 [Epub ahead of print]
  High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate.
  Lauer-Fields JL, Minond D, Chase PS, Baillargeon PE, Saldanha SA, Stawikowska R, Hodder P, Fields GB.
  -Scripps and Florida Atlantic University
  The major components of the cartilage extracellular matrix are type II collagen and aggrecan...
  
  
• J Am Chem Soc. 2008 Mar 5;130(9):2722-3.
  Total synthesis of +-superstolide A.
  Tortosa M, Yakelis NA, Roush WR.
  -Department of Chemistry
  A convergent and highly stereocontrolled synthesis of +-superstolide A (1) has been accomplished...
  
  
• J Virol. 2008 Feb;82(3):1073-83.
  Identification of residues required for RNA replication in domains II and III of the hepatitis C virus NS5A protein.
  Tellinghuisen TL, Foss KL, Treadaway JC, Rice CM.
  -Department of Infectology and Laboratory of Virology and Infectious Disease, Center for the Study of Hepatitis C, The Rockefeller University
  The NS5A protein of hepatitis C virus (HCV) plays an important but undefined role in viral RNA replication...
  
  
• Anal Biochem.2008 Feb 1;373(1):43-51.Epub 2007 Sep 15.
  Screening of potential a disintegrin and metalloproteinase with thrombospondin motifs-4 inhibitors using a collagen model fluorescence resonance energy transfer substrate
  Lauer-Fields JL, Spicer TP, Chase PS, Cudic M, Burstein GD, Nagase H, Hodder P, Fields GB
  - Scripps Florida
  
  
• PLoS ONE. 2008 Jan 23;3(1):e1486.
  A novel RNA transcript with antiapoptotic function is silenced in fragile x syndrome.
  Khalil AM, Faghihi MA, Modarresi F, Brothers SP, Wahlestedt C.
  -Molecular and Integrative Neurosciences Department (MIND)
  Several genome-wide transcriptomics efforts have shown that a large percentage of the mammalian genome is transcribed into RNAs...
  
  
• J Biomol Screen. 2008 Jan;13(1):17-28.
  Comparison of miniaturized time-resolved fluorescence resonance energy transfer and enzyme-coupled luciferase high-throughput screening assays to discover inhibitors of Rho-kinase II (ROCK-II).
  Schröter T, Minond D, Weiser A, Dao C, Habel J, Spicer T, Chase P, Baillargeon P, Scampavia L, Schürer S, Chung C, Mader C, Southern M, Tsinoremas N, LoGrasso P, Hodder P. -Department of Molecular Therapeutics and Drug Discovery
  Kinases are important drug discovery targets for a wide variety of therapeutic indications; consequently, the measurement of kinase activity remains a common high-throughput screening (HTS) application...
  
  
• Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20314-9.
  A coactivator trap identifies NONO (p54nrb) as a component of the cAMP-signaling pathway.
  Amelio AL, Miraglia LJ, Conkright JJ, Mercer BA, Batalov S, Cavett V, Orth AP, Busby J, Hogenesch JB, Conkright MD.
  -Departments of Cancer Biology, Molecular Therapeutics, and Translational Research Institute
  Signal transduction pathways often use a transcriptional component to mediate adaptive cellular responses...

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