D. Sheffler

发表

Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia

B. Roth, D. Sheffler, W. Kroeze, 2004, Nature Reviews Drug Discovery.

Bryan L Roth, B. Roth, D. Sheffler, 2003, Journal of Cell Science.

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

D. Sheffler, A. Der-Avakian, N. Cosford, 2014, Journal of medicinal chemistry.

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).

Steven H. Liang, Ming-Rong Zhang, D. Sheffler, 2020, Journal of medicinal chemistry.

A Combination of Flow and Batch Mode Processes for the Efficient Preparation of mGlu2/3 Receptor Negative Allosteric Modulators (NAMs).

D. Sheffler, N. Cosford, A. Herath, 2018, Tetrahedron.

Atypical antipsychotic drug actions: unitary or multiple mechanisms for ‘atypicality’?

Steven G Potkin, Bryan L Roth, S. Potkin, 2003, Clinical Neuroscience Research.

Metabotropic Glutamate Receptor 5 as a Target for the Treatment of Depression and Smoking: Robust Preclinical Data but Inconclusive Clinical Efficacy

D. Sheffler, N. Cosford, S. Semenova, 2018, Biological Psychiatry.

Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators.

D. Sheffler, N. Cosford, A. Pinkerton, 2011, ACS chemical neuroscience.

Synthesis and preliminary studies of a novel negative allosteric modulator [11C]QCA for imaging of metabotropic glutamate receptor 2

Steven H. Liang, Ming-Rong Zhang, D. Sheffler, 2017 .

Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.

Brian A. Chauder, Bruce J. Melancon, D. Sheffler, 2012, Bioorganic & medicinal chemistry letters.

Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.

D. Sheffler, C. Lindsley, C. Hopkins, 2013, Bioorganic & medicinal chemistry letters.

Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.

D. Sheffler, C. Lindsley, E. Lebois, 2012, ACS chemical neuroscience.

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.

Bruce J. Melancon, Anna L. Blobaum, D. Sheffler, 2013, Bioorganic & medicinal chemistry letters.

Synthesis and preliminary studies of 11C-labeled tetrahydro-1,7-naphthyridine-2-carboxamides for PET imaging of metabotropic glutamate receptor 2

Steven H. Liang, Ming-Rong Zhang, D. Sheffler, 2020, Theranostics.

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors.

D. Sheffler, N. Cosford, L. J. Lambert, 2020, Journal of visualized experiments : JoVE.

Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.

D. Sheffler, C. Lindsley, Hyekyung P. Cho, 2011, Bioorganic & medicinal chemistry letters.

Co-Activation of Metabotropic Glutamate Receptor 3 and Beta-Adrenergic Receptors Modulates Cyclic-AMP and Long-Term Potentiation, and Disrupts Memory Reconsolidation

D. Sheffler, Z. Xiang, C. Lindsley, 2017, Neuropsychopharmacology.

Yohimbine Depresses Excitatory Transmission in BNST and Impairs Extinction of Cocaine Place Preference Through Orexin-Dependent, Norepinephrine-Independent Processes

D. Sheffler, J. Javitch, Heinrich J.G. Matthies, 2012, Neuropsychopharmacology.

Identification and Development of A New Positron Emission Tomography Ligand 4-(2-Fluoro-4-[ 11 C]methoxyphenyl)-5-((1-methyl-1 H -pyrazol-3-yl)methoxy)picolinamide for Imaging Metabotropic Glutamate Receptor Subtype 2 (mGlu 2 )

Steven H. Liang, Ming-Rong Zhang, D. Sheffler, 2021 .

Extended Probe Characterization: Development of an M4 PAM with Improved Activity and Brain Exposure, while Avoiding Species Bias

Julie L. Engers, Bruce J. Melancon, D. Sheffler, 2013 .

Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells

D. Sheffler, P. Conn, P. Jeffrey Conn, 2008, Neuropharmacology.

Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates.

John M Asara, Peter Teriete, Chad J. Miller, 2015, Molecular cell.

Identification of the Molecular Mechanisms by Which the Diterpenoid Salvinorin A Binds to κ-Opioid Receptors†

Bryan L Roth, Philip D Mosier, B. Roth, 2005 .

The Regulation of G Protein-Coupled Receptor (GPCR) Signal Transduction by p90 Ribosomal S6 Kinase 2 (RSK2)

D. Sheffler, 2006 .

Salvinorin A: the "magic mint" hallucinogen finds a molecular target in the kappa opioid receptor.

B. Roth, D. Sheffler, 2003, Trends in pharmacological sciences.

Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists.

D. Sheffler, C. Lindsley, P. Conn, 2012, Bioorganic & medicinal chemistry letters.

Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.

Bruce J. Melancon, D. Sheffler, C. Lindsley, 2012, Bioorganic & medicinal chemistry letters.

Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.

Bruce J. Melancon, D. Sheffler, C. Lindsley, 2012, Bioorganic & medicinal chemistry letters.

Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.

D. Sheffler, J. P. Kennedy, C. Lindsley, 2008, Bioorganic & medicinal chemistry letters.

Pharmacologic analysis of non-synonymous coding h5-HT2A SNPs reveals alterations in atypical antipsychotic and agonist efficacies

Ryan T. Strachan, V. Setola, B. Roth, 2006, The Pharmacogenomics Journal.

Benzodiazepinone Derivatives Protect against Endoplasmic Reticulum Stress-Mediated Cell Death in Human Neuronal Cell Lines

D. Sheffler, John Calvin Reed, N. Cosford, 2014, ACS chemical neuroscience.

A cellular target engagement assay for the characterization of SHP2 (PTPN11) phosphatase inhibitors

D. Sheffler, E. Sergienko, N. Cosford, 2020, The Journal of Biological Chemistry.

Aripiprazole: a novel atypical antipsychotic drug with a uniquely robust pharmacology.

B. Roth, D. Sheffler, M. Davies, 2006, CNS drug reviews.

Corticotropin Releasing Factor Binding Protein as a Novel Target to Restore Brain Homeostasis: Lessons Learned From Alcohol Use Disorder Research

D. Sheffler, A. Webb, C. Haass‐Koffler, 2021, Frontiers in Behavioral Neuroscience.

Caveolin-1 Interacts with 5-HT2A Serotonin Receptors and Profoundly Modulates the Signaling of Selected Gαq-coupled Protein Receptors*

B. Roth, D. Sheffler, W. Kroeze, 2004, Journal of Biological Chemistry.

Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia.

S. Knapp, D. Sheffler, N. Cosford, 2021, Journal of medicinal chemistry.

A Novel Selective Muscarinic Acetylcholine Receptor Subtype 1 Antagonist Reduces Seizures without Impairing Hippocampus-Dependent Learning

S. Jadhav, D. Sheffler, Z. Xiang, 2009, Molecular Pharmacology.

Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.

Anna L. Blobaum, D. Sheffler, C. Lindsley, 2012, Bioorganic & medicinal chemistry letters.

Allosteric modulation of metabotropic glutamate receptors

K. Gregory, D. Sheffler, P. Conn, 2013 .

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.

S. Knapp, D. Sheffler, R. Shaw, 2020, Journal of medicinal chemistry.

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

D. Sheffler, N. Cosford, P. Conn, 2010, Neuropsychopharmacology.

Novel Allosteric Agonists of M1 Muscarinic Acetylcholine Receptors Induce Brain Region-Specific Responses That Correspond with Behavioral Effects in Animal Models

M. Foster Olive, J. Scott Daniels, P. Jeffrey Conn, 2012, The Journal of Neuroscience.

p90 Ribosomal S6 kinase 2, a novel GPCR kinase, is required for growth factor-mediated attenuation of GPCR signaling.

Ryan T. Strachan, B. Roth, D. Sheffler, 2010, Biochemistry.

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.

Anna L. Blobaum, D. Sheffler, C. Lindsley, 2012, ACS chemical neuroscience.

Activation of Group II Metabotropic Glutamate Receptors (mGluR2 and mGluR3) as a Novel Approach for Treatment of Schizophrenia

D. Sheffler, P. Conn, 2010 .

5-HT Receptor-Associated Proteins (FRAPs)

B. Roth, D. Sheffler, Zongqin Xia, 2006 .

Cell-type specific effects of endocytosis inhibitors on 5-hydroxytryptamine2A receptor desensitization and resensitization reveal an arrestin-, GRK2-, and GRK5-independent mode of regulation in human embryonic kidney 293 cells

B. Roth, S. Hufeisen, D. Sheffler, 2001 .

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.

B. Roth, S. Hufeisen, D. Sheffler, 2001, Molecular Pharmacology.

p90 ribosomal S6 kinase 2 exerts a tonic brake on G protein-coupled receptor signaling.

A. Deutch, B. Roth, S. Hufeisen, 2006, Proceedings of the National Academy of Sciences of the United States of America.

Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4)

Peter Hodder, Louis Scampavia, Franck Madoux, 2015, Journal of biomolecular screening.

Novel potent azetidine-based compounds irreversibly inhibit Stat3 activation and induce antitumor response against human breast tumor growth in vivo

C. Brotherton-Pleiss, P. Yue, Yinsong Zhu, 2022, Cancer letters.

Synthesis and Preliminary Studies of a Novel Negative Allosteric Modulator, 7-((2,5-Dioxopyrrolidin-1-yl)methyl)-4-(2-fluoro-4-[11C]methoxyphenyl) quinoline-2-carboxamide, for Imaging of Metabotropic Glutamate Receptor 2.

Steven H. Liang, Ming-Rong Zhang, D. Sheffler, 2017, ACS chemical neuroscience.

Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.

D. Sheffler, N. Cosford, P. Conn, 2012, Journal of medicinal chemistry.

Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead.

Andrew S. Felts, D. Sheffler, C. Lindsley, 2014, Bioorganic & medicinal chemistry letters.

Ribosomal S6 Kinase 2 Directly Phosphorylates the 5-Hydroxytryptamine 2A (5-HT2A) Serotonin Receptor, Thereby Modulating 5-HT2A Signaling*

Ryan T. Strachan, B. Roth, D. Sheffler, 2009, Journal of Biological Chemistry.

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.

Anna L. Blobaum, D. Sheffler, C. Lindsley, 2012, Bioorganic & medicinal chemistry letters.

mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning

M. Foster Olive, P. Jeffrey Conn, Craig W. Lindsley, 2009, Neuropsychopharmacology.

Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

D. Sheffler, Z. Xiang, C. Lindsley, 2011, Bioorganic & medicinal chemistry letters.

Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats.

D. Sheffler, N. Cosford, P. Conn, 2011, Journal of medicinal chemistry.

Neuroscience targets and human studies: future translational efforts in the stress system

D. Sheffler, C. Haass‐Koffler, 2023, Neuropsychopharmacology.

Screening for Small Molecule Inhibitors of Statin-Induced APP C-terminal Toxic Fragment Production

D. Sheffler, D. Bredesen, N. Cosford, 2017, Front. Pharmacol..

Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: development of a [3.3.0]-based series and other piperidine bioisosteres.

D. Sheffler, C. Lindsley, P. Conn, 2014, Bioorganic & medicinal chemistry letters.

Development and use of a high-throughput screen to identify novel modulators of the corticotropin releasing factor binding protein

A. Bonci, D. Sheffler, M. Hedrick, 2022, SLAS discovery : advancing life sciences R & D.

Allosteric modulation of metabotropic glutamate receptors.

K. Gregory, D. Sheffler, P. Conn, 2011, Advances in pharmacology.

Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.

D. Sheffler, C. Lindsley, P. Conn, 2013, Bioorganic & medicinal chemistry letters.

Development of the First Selective mGlu3 NAM from an mGlu5 PAM Hit

Julie L. Engers, Joshua A. Brunner, Anna L. Blobaum, 2013 .

Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.

D. Sheffler, C. Lindsley, Margrith E. Mattmann, 2013, Bioorganic & medicinal chemistry letters.

Fast dissociation rates predict neither efficacy nor lack of side-effects

B. Roth, D. Sheffler, W. Kroeze, 2004, Nature Reviews Drug Discovery.