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• 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 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.
  
  
• 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...
  
  

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