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Douglas J. Sheffler - Publications

Affiliations: 
Vanderbilt University, Nashville, TN 
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44 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2018 Barnes SA, Sheffler DJ, Semenova S, Cosford NDP, Bespalov A. Metabotropic Glutamate Receptor 5 as a Target for the Treatment of Depression and Smoking: Robust Preclinical Data but Inconclusive Clinical Efficacy. Biological Psychiatry. PMID 29628194 DOI: 10.1016/j.biopsych.2018.03.001  0.304
2017 Walker AG, Sheffler DJ, Lewis AS, Dickerson JW, Foster DJ, Senter RK, Moehle MS, Lv X, Stansley BJ, Xiang Z, Rook JM, Emmitte KA, Lindsley CW, Conn PJ. Co-Activation of Metabotropic Glutamate Receptor 3 and Beta-Adrenergic Receptors Modulates Cyclic-AMP, Long-Term Potentiation, and Disrupts Memory Reconsolidation. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. PMID 28664928 DOI: 10.1038/Npp.2017.136  0.745
2015 Smith E, Chase P, Niswender CM, Utley TJ, Sheffler DJ, Noetzel MJ, Lamsal A, Wood MR, Conn PJ, Lindsley CW, Madoux F, Acosta M, Scampavia L, Spicer T, Hodder P. Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4). Journal of Biomolecular Screening. PMID 25877150 DOI: 10.1177/1087057115581770  0.55
2014 Dhanya RP, Sheffler DJ, Dahl R, Davis M, Lee PS, Yang L, Nickols HH, Cho HP, Smith LH, D'Souza MS, Conn PJ, Der-Avakian A, Markou A, Cosford ND. Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence. Journal of Medicinal Chemistry. 57: 4154-72. PMID 24735492 DOI: 10.1021/Jm5000563  0.472
2014 Sheffler DJ, Nedelovych MT, Williams R, Turner SC, Duerk BB, Robbins MR, Jadhav SB, Niswender CM, Jones CK, Conn PJ, Daniels RN, Lindsley CW. Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: development of a [3.3.0]-based series and other piperidine bioisosteres. Bioorganic & Medicinal Chemistry Letters. 24: 1062-6. PMID 24462664 DOI: 10.1016/J.Bmcl.2014.01.011  0.346
2014 Jones CK, Sheffler DJ, Williams R, Jadhav SB, Felts AS, Morrison RD, Niswender CM, Daniels JS, Conn PJ, Lindsley CW. Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead. Bioorganic & Medicinal Chemistry Letters. 24: 1067-70. PMID 24461352 DOI: 10.1016/J.Bmcl.2014.01.013  0.356
2013 Poslusney MS, Melancon BJ, Gentry PR, Sheffler DJ, Bridges TM, Utley TJ, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR. Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule. Bioorganic & Medicinal Chemistry Letters. 23: 1860-4. PMID 23416001 DOI: 10.1016/J.Bmcl.2013.01.017  0.466
2013 Melancon BJ, Poslusney MS, Gentry PR, Tarr JC, Sheffler DJ, Mattmann ME, Bridges TM, Utley TJ, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR. Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule. Bioorganic & Medicinal Chemistry Letters. 23: 412-6. PMID 23237839 DOI: 10.1016/J.Bmcl.2012.11.092  0.505
2013 Sheffler DJ, Sevel C, Le U, Lovell KM, Tarr JC, Carrington SJ, Cho HP, Digby GJ, Niswender CM, Conn PJ, Hopkins CR, Wood MR, Lindsley CW. Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism. Bioorganic & Medicinal Chemistry Letters. 23: 223-7. PMID 23200253 DOI: 10.1016/J.Bmcl.2012.10.132  0.442
2013 Le U, Melancon BJ, Bridges TM, Vinson PN, Utley TJ, Lamsal A, Rodriguez AL, Venable D, Sheffler DJ, Jones CK, Blobaum AL, Wood MR, Daniels JS, Conn PJ, Niswender CM, et al. Discovery of a selective Mâ‚„ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. Bioorganic & Medicinal Chemistry Letters. 23: 346-50. PMID 23177787 DOI: 10.1016/J.Bmcl.2012.10.073  0.477
2012 Digby GJ, Utley TJ, Lamsal A, Sevel C, Sheffler DJ, Lebois EP, Bridges TM, Wood MR, Niswender CM, Lindsley CW, Conn PJ. Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode. Acs Chemical Neuroscience. 3: 1025-36. PMID 23259038 DOI: 10.1021/Cn300103E  0.768
2012 Tarr JC, Turlington ML, Reid PR, Utley TJ, Sheffler DJ, Cho HP, Klar R, Pancani T, Klein MT, Bridges TM, Morrison RD, Blobaum AL, Xiang Z, Daniels JS, Niswender CM, et al. Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169. Acs Chemical Neuroscience. 3: 884-95. PMID 23173069 DOI: 10.1021/Cn300068S  0.776
2012 Poslusney MS, Sevel C, Utley TJ, Bridges TM, Morrison RD, Kett NR, Sheffler DJ, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR. Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists. Bioorganic & Medicinal Chemistry Letters. 22: 6923-8. PMID 23062550 DOI: 10.1016/J.Bmcl.2012.09.011  0.49
2012 Sidique S, Dhanya RP, Sheffler DJ, Nickols HH, Yang L, Dahl R, Mangravita-Novo A, Smith LH, D'Souza MS, Semenova S, Conn PJ, Markou A, Cosford ND. Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence. Journal of Medicinal Chemistry. 55: 9434-45. PMID 23009245 DOI: 10.1021/Jm3005306  0.446
2012 Melancon BJ, Utley TJ, Sevel C, Mattmann ME, Cheung YY, Bridges TM, Morrison RD, Sheffler DJ, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR. Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012. Bioorganic & Medicinal Chemistry Letters. 22: 5035-40. PMID 22749871 DOI: 10.1016/J.Bmcl.2012.06.018  0.485
2012 Salovich JM, Vinson PN, Sheffler DJ, Lamsal A, Utley TJ, Blobaum AL, Bridges TM, Le U, Jones CK, Wood MR, Daniels JS, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR. Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor. Bioorganic & Medicinal Chemistry Letters. 22: 5084-8. PMID 22738637 DOI: 10.1016/J.Bmcl.2012.05.109  0.476
2012 Digby GJ, Noetzel MJ, Bubser M, Utley TJ, Walker AG, Byun NE, Lebois EP, Xiang Z, Sheffler DJ, Cho HP, Davis AA, Nemirovsky NE, Mennenga SE, Camp BW, Bimonte-Nelson HA, et al. Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models. The Journal of Neuroscience : the Official Journal of the Society For Neuroscience. 32: 8532-44. PMID 22723693 DOI: 10.1523/Jneurosci.0337-12.2012  0.781
2012 Conrad KL, Davis AR, Silberman Y, Sheffler DJ, Shields AD, Saleh SA, Sen N, Matthies HJ, Javitch JA, Lindsley CW, Winder DG. Yohimbine depresses excitatory transmission in BNST and impairs extinction of cocaine place preference through orexin-dependent, norepinephrine-independent processes. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 37: 2253-66. PMID 22617356 DOI: 10.1038/Npp.2012.76  0.583
2012 Sheffler DJ, Wenthur CJ, Bruner JA, Carrington SJ, Vinson PN, Gogi KK, Blobaum AL, Morrison RD, Vamos M, Cosford ND, Stauffer SR, Daniels JS, Niswender CM, Conn PJ, Lindsley CW. Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM. Bioorganic & Medicinal Chemistry Letters. 22: 3921-5. PMID 22607673 DOI: 10.1016/J.Bmcl.2012.04.112  0.481
2012 Melancon BJ, Gogliotti RD, Tarr JC, Saleh SA, Chauder BA, Lebois EP, Cho HP, Utley TJ, Sheffler DJ, Bridges TM, Morrison RD, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, et al. Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor. Bioorganic & Medicinal Chemistry Letters. 22: 3467-72. PMID 22507963 DOI: 10.1016/J.Bmcl.2012.03.088  0.768
2012 Melancon BJ, Lamers AP, Bridges TM, Sulikowski GA, Utley TJ, Sheffler DJ, Noetzel MJ, Morrison RD, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Wood MR. Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012. Bioorganic & Medicinal Chemistry Letters. 22: 1044-8. PMID 22197142 DOI: 10.1016/J.Bmcl.2011.11.110  0.443
2011 Sheffler DJ, Pinkerton AB, Dahl R, Markou A, Cosford ND. Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators. Acs Chemical Neuroscience. 2: 382-93. PMID 22860167 DOI: 10.1021/Cn200008D  0.432
2011 Lebois EP, Digby GJ, Sheffler DJ, Melancon BJ, Tarr JC, Cho HP, Miller NR, Morrison R, Bridges TM, Xiang Z, Daniels JS, Wood MR, Conn PJ, Lindsley CW. Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071. Bioorganic & Medicinal Chemistry Letters. 21: 6451-5. PMID 21930376 DOI: 10.1016/J.Bmcl.2011.08.084  0.756
2011 Sheffler DJ, Gregory KJ, Rook JM, Conn PJ. Allosteric modulation of metabotropic glutamate receptors. Advances in Pharmacology (San Diego, Calif.). 62: 37-77. PMID 21907906 DOI: 10.1016/B978-0-12-385952-5.00010-5  0.512
2011 Reid PR, Bridges TM, Sheffler DJ, Cho HP, Lewis LM, Days E, Daniels JS, Jones CK, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Wood MR. Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe. Bioorganic & Medicinal Chemistry Letters. 21: 2697-701. PMID 21194936 DOI: 10.1016/J.Bmcl.2010.12.015  0.42
2011 Dhanya RP, Sidique S, Sheffler DJ, Nickols HH, Herath A, Yang L, Dahl R, Ardecky R, Semenova S, Markou A, Conn PJ, Cosford ND. Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats. Journal of Medicinal Chemistry. 54: 342-53. PMID 21155570 DOI: 10.1021/Jm1012165  0.351
2010 Strachan RT, Allen JA, Sheffler DJ, Roth BL. p90 Ribosomal S6 kinase 2, a novel GPCR kinase, is required for growth factor-mediated attenuation of GPCR signaling. Biochemistry. 49: 2657-71. PMID 20136148 DOI: 10.1021/bi901921k  0.75
2009 Weaver CD, Sheffler DJ, Lewis LM, Bridges TM, Williams R, Nalywajko NT, Kennedy JP, Mulder MM, Jadhav S, Aldrich LA, Jones CK, Marlo JE, Niswender CM, Mock MM, Zheng F, et al. Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe. Current Topics in Medicinal Chemistry. 9: 1217-26. PMID 19807667 DOI: 10.2174/156802609789753635  0.497
2009 Sheffler DJ, Williams R, Bridges TM, Xiang Z, Kane AS, Byun NE, Jadhav S, Mock MM, Zheng F, Lewis LM, Jones CK, Niswender CM, Weaver CD, Lindsley CW, Conn PJ. A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Molecular Pharmacology. 76: 356-68. PMID 19407080 DOI: 10.1124/Mol.109.056531  0.547
2009 Ayala JE, Chen Y, Banko JL, Sheffler DJ, Williams R, Telk AN, Watson NL, Xiang Z, Zhang Y, Jones PJ, Lindsley CW, Olive MF, Conn PJ. mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 34: 2057-71. PMID 19295507 DOI: 10.1038/Npp.2009.30  0.707
2009 Strachan RT, Sheffler DJ, Willard B, Kinter M, Kiselar JG, Roth BL. Ribosomal S6 kinase 2 directly phosphorylates the 5-hydroxytryptamine 2A (5-HT2A) serotonin receptor, thereby modulating 5-HT2A signaling. The Journal of Biological Chemistry. 284: 5557-73. PMID 19103592 DOI: 10.1074/Jbc.M805705200  0.592
2008 Sheffler DJ, Conn PJ. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology. 55: 419-27. PMID 18625258 DOI: 10.1016/j.neuropharm.2008.06.047  0.47
2008 Lewis LM, Sheffler D, Williams R, Bridges TM, Kennedy JP, Brogan JT, Mulder MJ, Williams L, Nalywajko NT, Niswender CM, Weaver CD, Conn PJ, Lindsley CW. Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. Bioorganic & Medicinal Chemistry Letters. 18: 885-90. PMID 18178088 DOI: 10.1016/J.Bmcl.2007.12.051  0.493
2006 Sheffler DJ, Kroeze WK, Garcia BG, Deutch AY, Hufeisen SJ, Leahy P, Brüning JC, Roth BL. p90 ribosomal S6 kinase 2 exerts a tonic brake on G protein-coupled receptor signaling. Proceedings of the National Academy of Sciences of the United States of America. 103: 4717-22. PMID 16537434 DOI: 10.1073/Pnas.0600585103  0.575
2006 Davies MA, Setola V, Strachan RT, Sheffler DJ, Salay E, Hufeisen SJ, Roth BL. Pharmacologic analysis of non-synonymous coding h5-HT2A SNPs reveals alterations in atypical antipsychotic and agonist efficacies. The Pharmacogenomics Journal. 6: 42-51. PMID 16314884 DOI: 10.1038/sj.tpj.6500342  0.713
2005 Yan F, Mosier PD, Westkaemper RB, Stewart J, Zjawiony JK, Vortherms TA, Sheffler DJ, Roth BL. Identification of the molecular mechanisms by which the diterpenoid salvinorin A binds to kappa-opioid receptors. Biochemistry. 44: 8643-51. PMID 15952771 DOI: 10.1021/Bi050490D  0.62
2004 Davies MA, Sheffler DJ, Roth BL. Aripiprazole: a novel atypical antipsychotic drug with a uniquely robust pharmacology. Cns Drug Reviews. 10: 317-36. PMID 15592581 DOI: 10.1111/J.1527-3458.2004.Tb00030.X  0.495
2004 Bhatnagar A, Sheffler DJ, Kroeze WK, Compton-Toth B, Roth BL. Caveolin-1 interacts with 5-HT2A serotonin receptors and profoundly modulates the signaling of selected Galphaq-coupled protein receptors. The Journal of Biological Chemistry. 279: 34614-23. PMID 15190056 DOI: 10.1074/Jbc.M404673200  0.698
2004 Roth BL, Sheffler DJ, Kroeze WK. Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia. Nature Reviews. Drug Discovery. 3: 353-9. PMID 15060530 DOI: 10.1038/nrd1346  0.461
2004 Roth BL, Kroeze WK, Sheffler DJ. Fast dissociation rates predict neither efficacy nor lack of side-effects Nature Reviews Drug Discovery. 3: 894-894. DOI: 10.1038/Nrd1346-C2  0.408
2003 Kroeze WK, Sheffler DJ, Roth BL. G-protein-coupled receptors at a glance. Journal of Cell Science. 116: 4867-9. PMID 14625380 DOI: 10.1242/jcs.00902  0.491
2003 Sheffler DJ, Roth BL. Salvinorin A: the "magic mint" hallucinogen finds a molecular target in the kappa opioid receptor. Trends in Pharmacological Sciences. 24: 107-9. PMID 12628350 DOI: 10.1016/S0165-6147(03)00027-0  0.571
2003 Roth BL, Sheffler D, Potkin SG. Atypical antipsychotic drug actions: Unitary or multiple mechanisms for 'atypicality'? Clinical Neuroscience Research. 3: 108-117. DOI: 10.1016/S1566-2772(03)00021-5  0.545
2001 Gray JA, Sheffler DJ, Bhatnagar A, Woods JA, Hufeisen SJ, Benovic JL, Roth BL. Cell-type specific effects of endocytosis inhibitors on 5-hydroxytryptamine(2A) receptor desensitization and resensitization reveal an arrestin-, GRK2-, and GRK5-independent mode of regulation in human embryonic kidney 293 cells. Molecular Pharmacology. 60: 1020-30. PMID 11641430 DOI: 10.1124/Mol.60.5.1020  0.726
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