Structure-based discovery and development of metabotropic glutamate receptor 5 negative allosteric modulators

From Structure to Clinical Development: Allosteric Modulation of G Protein-Coupled Receptors - Advances in Pharmacology ◽

10.1016/bs.apha.2020.03.001 ◽

2020 ◽

pp. 35-58

Author(s):

Kirstie A. Bennett ◽

John A. Christopher ◽

Benjamin G. Tehan

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate

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Faculty Opinions recommendation of Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.732704940.793543297 ◽

2018 ◽

Author(s):

Dario Doller

Keyword(s):

G Protein ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

G Protein Coupled Receptor ◽

Metabotropic Glutamate Receptor 5 ◽

X Ray ◽

Metabotropic Glutamate ◽

G Protein Coupled

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Mechanisms of Skin Toxicity Associated with Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators

Cell Chemical Biology ◽

10.1016/j.chembiol.2017.06.003 ◽

2017 ◽

Vol 24 (7) ◽

pp. 858-869.e5 ◽

Author(s):

Falgun Shah ◽

Antonia F. Stepan ◽

Alison O'Mahony ◽

Sharlene Velichko ◽

Alexandra E. Folias ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Skin Toxicity ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate

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Integrated In Silico Fragment-Based Drug Design: Case Study with Allosteric Modulators on Metabotropic Glutamate Receptor 5

The AAPS Journal ◽

10.1208/s12248-017-0093-5 ◽

2017 ◽

Vol 19 (4) ◽

pp. 1235-1248 ◽

Author(s):

Yuemin Bian ◽

Zhiwei Feng ◽

Peng Yang ◽

Xiang-Qun Xie

Keyword(s):

Drug Design ◽

Glutamate Receptor ◽

In Silico ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Design Case ◽

Design Case Study

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Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2015.10.050 ◽

2015 ◽

Vol 25 (24) ◽

pp. 5792-5796 ◽

Author(s):

John M. Ellard ◽

Andrew Madin ◽

Oliver Philps ◽

Mark Hopkin ◽

Scott Henderson ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Preclinical Model ◽

Allosteric Modulators ◽

Improve Performance ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.7b01722 ◽

2018 ◽

Vol 62 (1) ◽

pp. 207-222 ◽

Author(s):

John A. Christopher ◽

Zoltán Orgován ◽

Miles Congreve ◽

Andrew S. Doré ◽

James C. Errey ◽

...

Keyword(s):

G Protein ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

G Protein Coupled Receptor ◽

Metabotropic Glutamate Receptor 5 ◽

X Ray ◽

Metabotropic Glutamate ◽

G Protein Coupled

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Metabotropic glutamate receptor 5-negative allosteric modulators for the treatment of psychiatric and neurological disorders (2009–July 2013)

Pharmaceutical Patent Analyst ◽

10.4155/ppa.13.58 ◽

2013 ◽

Vol 2 (6) ◽

pp. 767-802 ◽

Author(s):

Guiying Li ◽

Morten Jørgensen ◽

Brian M Campbell

Keyword(s):

Glutamate Receptor ◽

Neurological Disorders ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate

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A novel series of metabotropic glutamate receptor 5 negative allosteric modulators based on a 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine core

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2013.06.044 ◽

2013 ◽

Vol 23 (16) ◽

pp. 4523-4527 ◽

Author(s):

Guillaume Duvey ◽

Benjamin Perry ◽

Emmanuel Le Poul ◽

Sonia Poli ◽

Beatrice Bonnet ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate

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N-Aryl Piperazine Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators Possess Efficacy in Preclinical Models of NMDA Hypofunction and Cognitive Enhancement

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.113.206623 ◽

2013 ◽

Vol 347 (2) ◽

pp. 438-457 ◽

Author(s):

K.J. Gregory ◽

E.J. Herman ◽

A.J. Ramsey ◽

A.S. Hammond ◽

N.E. Byun ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Cognitive Enhancement ◽

Allosteric Modulators ◽

Preclinical Models ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators

ACS Medicinal Chemistry Letters ◽

10.1021/acsmedchemlett.6b00292 ◽

2016 ◽

Vol 7 (12) ◽

pp. 1082-1086 ◽

Author(s):

Matthew D. Hill ◽

Haiquan Fang ◽

Jeffrey M. Brown ◽

Thaddeus Molski ◽

Amy Easton ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators: Discovery of 2-Chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (Basimglurant, RO4917523), a Promising Novel Medicine for Psychiatric Diseases

Journal of Medicinal Chemistry ◽

10.1021/jm501642c ◽

2015 ◽

Vol 58 (3) ◽

pp. 1358-1371 ◽

Author(s):

Georg Jaeschke ◽

Sabine Kolczewski ◽

Will Spooren ◽

Eric Vieira ◽

Nadia Bitter-Stoll ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Psychiatric Diseases ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate

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