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Douglas J. Sheffler · SciRah

Researcher profile · Semantic Scholar

Douglas J. Sheffler

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Douglas J. Sheffler — researcher profile on SciRah

h-index: 32
Works: 90
Citations: 4,732

Most-cited papers

Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia
B. Roth, Douglas J. Sheffler, W. Kroeze
2004Nature reviews. Drug discovery1,144 citations
Semantic Scholar
Small molecule inhibition of the autophagy kinase ULK1 and identification of ULK1 substrates
Daniel F. Egan, M. Chun, M. Vamos, Haixia Zou +11 more
2015Molecules and Cells667 citations Open access
Semantic Scholar
G-protein-coupled receptors at a glance
W. Kroeze, Douglas J. Sheffler, B. Roth
2003Journal of Cell Science373 citations Open access
Semantic Scholar
mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning
J. Ayala, Ye-Lin Chen, J. Banko, Douglas J. Sheffler +9 more
2009Neuropsychopharmacology216 citations Open access
Semantic Scholar
Caveolin-1 Interacts with 5-HT2A Serotonin Receptors and Profoundly Modulates the Signaling of Selected Gαq-coupled Protein Receptors*
A. Bhatnagar, Douglas J. Sheffler, W. Kroeze, Beth A. Compton-Toth +1 more
2004Journal of Biological Chemistry177 citations Open access
Semantic Scholar
Aripiprazole: a novel atypical antipsychotic drug with a uniquely robust pharmacology.
M. Davies, Douglas J. Sheffler, B. Roth
2006CNS drug reviews169 citations Open access
Semantic Scholar
Salvinorin A: the "magic mint" hallucinogen finds a molecular target in the kappa opioid receptor.
Douglas J. Sheffler, B. Roth
2003TIPS - Trends in Pharmacological Sciences157 citations
Semantic Scholar
A Novel Selective Muscarinic Acetylcholine Receptor Subtype 1 Antagonist Reduces Seizures without Impairing Hippocampus-Dependent Learning
Douglas J. Sheffler, R. Williams, T. M. Bridges, Zixiu Xiang +11 more
2009Molecular Pharmacology127 citations Open access
Semantic Scholar
Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models
Gregory J. Digby, M. Noetzel, M. Bubser, T. J. Utley +20 more
2012Journal of Neuroscience112 citations Open access
Semantic Scholar
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.
J. A. Gray, Douglas J. Sheffler, A. Bhatnagar, J. Woods +3 more
2001Molecular Pharmacology100 citations
Semantic Scholar
Identification of the Molecular Mechanisms by Which the Diterpenoid Salvinorin A Binds to κ-Opioid Receptors†
Feng-Xiang Yan, P. Mosier, R. Westkaemper, Jeremy Stewart +4 more
200597 citations Open access
Semantic Scholar
Atypical antipsychotic drug actions: unitary or multiple mechanisms for ‘atypicality’?
B. Roth, Douglas J. Sheffler, S. Potkin
200393 citations
Semantic Scholar
The mGluR2 positive allosteric modulator BINA decreases cocaine self-administration and cue-induced cocaine-seeking and counteracts cocaine-induced enhancement of brain reward function in rats
Xin-Chun Jin, S. Semenova, Li Yang, R. Ardecky +5 more
2010Neuropsychopharmacology83 citations Open access
Semantic Scholar
Impaired Hippocampus-Dependent and Facilitated Striatum-Dependent Behaviors in Mice Lacking the Delta Opioid Receptor
K. Conrad, Adeola R. Davis, Yuval Silberman, Douglas J. Sheffler +7 more
2013Neuropsychopharmacology64 citations Open access
Semantic Scholar
Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer.
Huiyu Ren, N. A. Bakas, M. Vamos, A. Chaikuad +10 more
2020Journal of Medicinal Chemistry61 citations Open access
Semantic Scholar
Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN Probe
Paul R. Reid, T. M. Bridges, Douglas J. Sheffler, Hyekyung P. Cho +9 more
2010Bioorganic & Medicinal Chemistry Letters59 citations Open access
Semantic Scholar
Design and Synthesis of an Orally Active Metabotropic Glutamate Receptor Subtype-2 (mGluR2) Positive Allosteric Modulator (PAM) that Decreases Cocaine Self-administration in Rats
R. Dhanya, Shyama Sidique, Douglas J. Sheffler, H. Nickols +8 more
2010Journal of Medicinal Chemistry52 citations Open access
Semantic Scholar
Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators.
Douglas J. Sheffler, A. Pinkerton, R. Dahl, A. Markou +1 more
2011ACS Chemical Neuroscience49 citations Open access
Semantic Scholar
Pharmacologic analysis of non-synonymous coding h5-HT2A SNPs reveals alterations in atypical antipsychotic and agonist efficacies
M. Davies, V. Setola, Ryan T. Strachan, Douglas J. Sheffler +3 more
2006The Pharmacogenomics Journal49 citations Open access
Semantic Scholar
Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 1a Differentially Modulate Independent Signaling Pathways in Baby Hamster Kidney Cells
Douglas J. Sheffler, P. Conn
2008Neuropharmacology47 citations Open access
Semantic Scholar
p90 ribosomal S6 kinase 2 exerts a tonic brake on G protein-coupled receptor signaling.
Douglas J. Sheffler, W. Kroeze, Bonnie Garcia, A. Deutch +4 more
2006Proceedings of the National Academy of Sciences of the United States of America46 citations Open access
Semantic Scholar
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.
J. C. Tarr, M. Turlington, Paul R. Reid, T. J. Utley +14 more
2012ACS Chemical Neuroscience44 citations Open access
Semantic Scholar
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM
Douglas J. Sheffler, Cody J. Wenthur, J. A. Bruner, Sheridan J. S. Carrington +11 more
2012Bioorganic & Medicinal Chemistry Letters41 citations Open access
Semantic Scholar
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
R. Dhanya, Douglas J. Sheffler, R. Dahl, Melinda R Davis +10 more
2014Journal of Medicinal Chemistry38 citations Open access
Semantic Scholar
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
J. M. Salovich, P. Vinson, Douglas J. Sheffler, A. Lamsal +11 more
2012Bioorganic & Medicinal Chemistry Letters37 citations Open access
Semantic Scholar
Discovery of a selective M4 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
Uyen M. Le, B. Melancon, T. M. Bridges, P. Vinson +13 more
2012Bioorganic & Medicinal Chemistry Letters35 citations Open access
Semantic Scholar
Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.
Gregory J. Digby, T. J. Utley, A. Lamsal, Christian Sevel +7 more
2012ACS Chemical Neuroscience35 citations Open access
Semantic Scholar
Development of a Highly Selective, Orally Bioavailable and CNS Penetrant M1 Agonist Derived from the MLPCN Probe ML071
Evan P. Lebois, Gregory J. Digby, Douglas J. Sheffler, Bruce J. Melancon +10 more
2011Bioorganic & Medicinal Chemistry Letters34 citations Open access
Semantic Scholar
Metabotropic glutamate receptor 5 as a target for the treatment of depression and smoking: robust preclinical data but inconclusive clinical efficacy
S. Barnes, Douglas J. Sheffler, S. Semenova, N. Cosford +1 more
2018Biological Psychiatry33 citations Open access
Semantic Scholar
Ribosomal S6 Kinase 2 Directly Phosphorylates the 5-Hydroxytryptamine 2A (5-HT2A) Serotonin Receptor, Thereby Modulating 5-HT2A Signaling*
Ryan T. Strachan, Douglas J. Sheffler, B. Willard, M. Kinter +2 more
2009Journal of Biological Chemistry33 citations Open access
Semantic Scholar
Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia
N. Bata, A. Chaikuad, N. A. Bakas, A. Limpert +12 more
2021Journal of Medicinal Chemistry32 citations Open access
Semantic Scholar
Yohimbine Depresses Excitatory Transmission in BNST and Impairs Extinction of Cocaine Place Preference Through Orexin-Dependent, Norepinephrine-Independent Processes
K. Conrad, Adeola R. Davis, Yuval Silberman, Douglas J. Sheffler +7 more
2012Neuropsychopharmacology32 citations Open access
Semantic Scholar
Synthesis and preliminary studies of a novel negative allosteric modulator [11C]QCA for imaging of metabotropic glutamate receptor 2
Xiaofei Zhang, K. Kumata, T. Yamasaki, Ran Cheng +10 more
2017ACS Chemical Neuroscience28 citations Open access
Semantic Scholar
Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule
M. Poslusney, B. Melancon, P. R. Gentry, Douglas J. Sheffler +7 more
2013Bioorganic & Medicinal Chemistry Letters27 citations Open access
Semantic Scholar
Orally Active Metabotropic Glutamate Subtype 2 Receptor Positive Allosteric Modulators: Structure-Activity Relationships and Assessment in a Rat Model of Nicotine Dependence
Shyama Sidique, R. Dhanya, Douglas J. Sheffler, H. Nickols +9 more
2012Journal of Medicinal Chemistry27 citations Open access
Semantic Scholar
Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4)
Emery Smith, P. Chase, C. Niswender, T. J. Utley +11 more
2015Journal of biomolecular screening25 citations Open access
Semantic Scholar
Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: Continued optimization of an MLPCN probe molecule
B. Melancon, M. Poslusney, P. R. Gentry, J. C. Tarr +9 more
2012Bioorganic & Medicinal Chemistry Letters21 citations Open access
Semantic Scholar
Novel potent azetidine-based compounds irreversibly inhibit Stat3 activation and induce antitumor response against human breast tumor growth in vivo
Pei-Bin Yue, Yinsong Zhu, C. Brotherton-Pleiss, Wen-Huan Fu +18 more
2022Cancer Letters20 citations Open access
Semantic Scholar
P90 RIBOSOMAL S6 KINASE 2, A NOVEL GPCR KINASE, IS REQUIRED FOR GROWTH FACTOR-MEDIATED ATTENUATION OF GPCR SIGNALING
Ryan T. Strachan, John A. Allen, Douglas J. Sheffler, B. Roth
2010Biochemistry19 citations Open access
Semantic Scholar
Synthesis and preliminary studies of 11C-labeled tetrahydro-1,7-naphthyridine-2-carboxamides for PET imaging of metabotropic glutamate receptor 2
Xiaofei Zhang, Yi-Ding Zhang, Zhen Chen, T. Shao +19 more
2020Theranostics17 citations Open access
Semantic Scholar
A cellular target engagement assay for the characterization of SHP2 (PTPN11) phosphatase inhibitors
C. Romero, L. J. Lambert, Douglas J. Sheffler, L. D. De Backer +9 more
2020Journal of Biological Chemistry17 citations Open access
Semantic Scholar
Co-Activation of Metabotropic Glutamate Receptor 3 and Beta-Adrenergic Receptors Modulates Cyclic-AMP and Long-Term Potentiation, and Disrupts Memory Reconsolidation
Adam G. Walker, Douglas J. Sheffler, Andrew Lewis, Jonathan W. Dickerson +10 more
2017Neuropsychopharmacology17 citations Open access
Semantic Scholar
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
C. Weaver, Douglas J. Sheffler, L. Lewis, T. M. Bridges +13 more
2009Current Topics in Medicinal Chemistry15 citations Open access
Semantic Scholar
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.
L. Lewis, Douglas J. Sheffler, R. Williams, T. M. Bridges +9 more
2008Bioorganic & Medicinal Chemistry Letters15 citations Open access
Semantic Scholar
Benzodiazepinone Derivatives Protect against Endoplasmic Reticulum Stress-Mediated Cell Death in Human Neuronal Cell Lines
Haixia Zou, A. Limpert, J. Zou, Anna G. Dembo +11 more
2014ACS Chemical Neuroscience14 citations Open access
Semantic Scholar
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor
B. Melancon, R. Gogliotti, J. C. Tarr, Sam A. Saleh +12 more
2012Bioorganic & Medicinal Chemistry Letters14 citations Open access
Semantic Scholar
Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012
B. Melancon, T. J. Utley, Christian Sevel, M. Mattmann +9 more
2012Bioorganic & Medicinal Chemistry Letters14 citations Open access
Semantic Scholar
Allosteric Modulation of Metabotropic Glutamate Receptors
Douglas J. Sheffler, K. J. Gregory, J. Rook, P. Conn
2011Advances in Pharmacology10 citations Open access
Semantic Scholar
Corticotropin Releasing Factor Binding Protein as a Novel Target to Restore Brain Homeostasis: Lessons Learned From Alcohol Use Disorder Research
Dallece E. Curley, A. Webb, Douglas J. Sheffler, C. Haass-Koffler
2021Frontiers in Behavioral Neuroscience9 citations Open access
Semantic Scholar
Identification and Development of A New Positron Emission Tomography Ligand 4-(2-Fluoro-4-[11C]methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide for Imaging Metabotropic Glutamate Receptor Subtype 2 (mGlu2)
T. Yamasaki, Xiaofei Zhang, K. Kumata, Yi-Ding Zhang +16 more
2020Journal of Medicinal Chemistry9 citations Open access
Semantic Scholar

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