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Allosteric Modulation of Seven Transmembrane Spanning Receptors: Theory, Practice, and Opportunities for Central Nervous System Drug Discovery

Journal of medicinal chemistry, 2012-02, Vol.55 (4), p.1445-1464

2012

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Structural basis of positive allosteric modulation of metabotropic glutamate receptor activation and internalization

Nature communications, 2024-08, Vol.15 (1), p.6498-17, Article 6498

2024

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Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease

Drug discovery today, 2013-12, Vol.18 (23-24), p.1185-1199

2013

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Antipsychotic Drug-Like Effects of the Selective M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator VU0152100

Neuropsychopharmacology (New York, N.Y.), 2014-06, Vol.39 (7), p.1578-1593

2014

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A structural model for binding of the serine-rich repeat adhesin GspB to host carbohydrate receptors

PLoS pathogens, 2011-07, Vol.7 (7), p.e1002112

2011

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Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents

ACS chemical neuroscience, 2014-10, Vol.5 (10), p.920-942

2014

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Structural insights into HDAC6 tubulin deacetylation and its selective inhibition

Nature chemical biology, 2016-09, Vol.12 (9), p.748

2016

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On the Recent Changes to Animal Protection Measures in United States Food and Drug Administration Policy

Assay and drug development technologies, 2023-01, Vol.21 (1), p.1

Melancon, Bruce J

2023

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Challenges in the development of an M 4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs

Bioorganic & medicinal chemistry letters, 2017-01, Vol.27 (2), p.171-175

2017

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Forging Ahead with ASSAY

Assay and drug development technologies, 2022-04, Vol.20 (3), p.107

Melancon, Bruce J

2022

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Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354

Bioorganic & medicinal chemistry letters, 2014-10, Vol.24 (19), p.4708-4713

2014

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Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia

ACS medicinal chemistry letters, 2017-02, Vol.8 (2), p.233-238

2017

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Call for Special Issue Papers: New Modalities in Chemical Probes and Pharmacological Tools in Drug Discovery

Assay and drug development technologies, 2022-04, Vol.20 (3), p.103

2022

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4040 Investigation of a Series of 1,4-diaryl-pyrazolo-pyridinones as Anti-Leishmanial Agents

Journal of clinical and translational science, 2020-06, Vol.4 (s1), p.10-10

2020

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

Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (21), p.6451-6455

2011

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mGlu1-mediated restoration of prefrontal cortex inhibitory signaling reverses social and cognitive deficits in an NMDA hypofunction model in mice

Neuropsychopharmacology (New York, N.Y.), 2022-09, Vol.47 (10), p.1826-1835

2022

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Development of a target-free high-throughput screening platform for the discovery of antileishmanial compounds

International journal of antimicrobial agents, 2019-10, Vol.54 (4), p.496-501

2019

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Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds

Bioorganic & medicinal chemistry letters, 2021-10, Vol.50, p.128342-128342, Article 128342

2021

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2-Hydroxypropyl-β-cyclodextrin is the active component in a triple combination formulation for treatment of Niemann-Pick C1 disease

Biochimica et biophysica acta. Molecular and cell biology of lipids, 2019-10, Vol.1864 (10), p.1545-1561

2019

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A concise Diels–Alder strategy leading to congeners of the ABC ring system of the marine alkaloid ‘upenamide

Tetrahedron letters, 2016-07, Vol.57 (30), p.3252-3253

2016

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Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs

Bioorganic & medicinal chemistry letters, 2021-01, Vol.32, p.127724-127724, Article 127724

2021

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Lead optimization of the VU0486321 series of mGlu 1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs

Bioorganic & medicinal chemistry letters, 2021-01, Vol.32, p.127724

2021

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The succinct synthesis of AT13387, a clinically relevant Hsp90 inhibitor

Synthetic communications, 2019-06, Vol.49 (11), p.1436-1443

2019

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Microplate-based assay for identifying small molecules that bind a specific intersubunit interface within the assembled HIV-1 capsid

Antimicrobial agents and chemotherapy, 2015-09, Vol.59 (9), p.5190-5195

2015

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Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides

Bioorganic & medicinal chemistry letters, 2017-12, Vol.27 (23), p.5179-5184

2017

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Allosteric Modulation of Seven Transmembrane Spanning Receptors: Theory, Practice, and Opportunities for Central Nervous System Drug Discovery

Structural basis of positive allosteric modulation of metabotropic glutamate receptor activation and internalization

Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease

Antipsychotic Drug-Like Effects of the Selective M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator VU0152100

A structural model for binding of the serine-rich repeat adhesin GspB to host carbohydrate receptors

Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents

Structural insights into HDAC6 tubulin deacetylation and its selective inhibition

On the Recent Changes to Animal Protection Measures in United States Food and Drug Administration Policy

Challenges in the development of an M 4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs

Forging Ahead with ASSAY

Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia

Call for Special Issue Papers: New Modalities in Chemical Probes and Pharmacological Tools in Drug Discovery

4040 Investigation of a Series of 1,4-diaryl-pyrazolo-pyridinones as Anti-Leishmanial Agents

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

mGlu1-mediated restoration of prefrontal cortex inhibitory signaling reverses social and cognitive deficits in an NMDA hypofunction model in mice

Development of a target-free high-throughput screening platform for the discovery of antileishmanial compounds

Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds

2-Hydroxypropyl-β-cyclodextrin is the active component in a triple combination formulation for treatment of Niemann-Pick C1 disease

A concise Diels–Alder strategy leading to congeners of the ABC ring system of the marine alkaloid ‘upenamide

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs

Lead optimization of the VU0486321 series of mGlu 1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs

The succinct synthesis of AT13387, a clinically relevant Hsp90 inhibitor

Microplate-based assay for identifying small molecules that bind a specific intersubunit interface within the assembled HIV-1 capsid

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides

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