Integration of Lead Optimization with Crystallography for a Membrane-Bound Ion Channel Target: Discovery of a New Class of AMPA Receptor Positive Allosteric Modulators

Simon E. Ward; Mark Harries; Laura Aldegheri; Nigel E. Austin; Stuart Ballantine; Elisa Ballini; Daniel M. Bradley; Benjamin D. Bax; Brian P. Clarke; Andrew J. Harris; Stephen A. Harrison; Rosemary A. Melarange; Claudette Mookherjee; Julie Mosley; Gianni Dal Negro; Beatrice Oliosi; Kathrine J. Smith; Kevin M. Thewlis; Patrick M. Woollard; Shahnaz P. Yusaf

doi:10.1021/jm100679e

Integration of Lead Optimization with Crystallography for a Membrane-Bound Ion Channel Target: Discovery of a New Class of AMPA Receptor Positive Allosteric Modulators

Journal of Medicinal Chemistry ◽

10.1021/jm100679e ◽

2011 ◽

Vol 54 (1) ◽

pp. 78-94 ◽

Cited By ~ 45

Author(s):

Simon E. Ward ◽

Mark Harries ◽

Laura Aldegheri ◽

Nigel E. Austin ◽

Stuart Ballantine ◽

...

Keyword(s):

Ion Channel ◽

Ampa Receptor ◽

Lead Optimization ◽

Allosteric Modulators ◽

Target Discovery ◽

New Class ◽

Membrane Bound ◽

Positive Allosteric Modulators

Download Full-text

Auxiliary Proteins are the Predominant Determinants of Differential Efficacy of Clinical Candidates Acting as AMPA Receptor Positive Allosteric Modulators

Molecular Pharmacology ◽

10.1124/mol.119.118554 ◽

2020 ◽

Vol 97 (5) ◽

pp. 336-350

Author(s):

Toshiyuki Ishii ◽

Jacob R. Stolz ◽

Geoffrey T. Swanson

Keyword(s):

Ampa Receptor ◽

Allosteric Modulators ◽

Positive Allosteric Modulators

Download Full-text

Structural requirements for molecular design of positive allosteric modulators of AMPA receptor

Mendeleev Communications ◽

10.1016/j.mencom.2017.11.029 ◽

2017 ◽

Vol 27 (6) ◽

pp. 623-625 ◽

Cited By ~ 6

Author(s):

Eugene V. Radchenko ◽

Dmitry S. Karlov ◽

Mstislav I. Lavrov ◽

Vladimir A. Palyulin

Keyword(s):

Ampa Receptor ◽

Molecular Design ◽

Allosteric Modulators ◽

Structural Requirements ◽

Positive Allosteric Modulators

Download Full-text

A Combined Bioinformatics and Chemoinformatics Approach for Developing Asymmetric Bivalent AMPA Receptor Positive Allosteric Modulators as Neuroprotective Agents

ChemMedChem ◽

10.1002/cmdc.201200554 ◽

2012 ◽

Vol 8 (2) ◽

pp. 226-230 ◽

Cited By ~ 20

Author(s):

Haijun Chen ◽

Cheng Z. Wang ◽

Chunyong Ding ◽

Christopher Wild ◽

Bryan Copits ◽

...

Keyword(s):

Ampa Receptor ◽

Allosteric Modulators ◽

Neuroprotective Agents ◽

Positive Allosteric Modulators

Download Full-text

AMPA receptor-positive allosteric modulators for the treatment of schizophrenia: an overview of recent patent applications

Future Medicinal Chemistry ◽

10.4155/fmc.15.4 ◽

2015 ◽

Vol 7 (4) ◽

pp. 473-491 ◽

Cited By ~ 9

Author(s):

Simon E Ward ◽

Lewis E Pennicott ◽

Paul Beswick

Keyword(s):

Ampa Receptor ◽

Allosteric Modulators ◽

Patent Applications ◽

Positive Allosteric Modulators

Download Full-text

CHAPTER 6. AMPA Receptor Positive Allosteric Modulators – a Case History

Ion Channel Drug Discovery - Drug Discovery ◽

10.1039/9781849735087-00105 ◽

2014 ◽

pp. 105-134

Author(s):

Simon E Ward

Keyword(s):

Ampa Receptor ◽

Case History ◽

Allosteric Modulators ◽

Positive Allosteric Modulators

Download Full-text

Back Cover: A Combined Bioinformatics and Chemoinformatics Approach for Developing Asymmetric Bivalent AMPA Receptor Positive Allosteric Modulators as Neuroprotective Agents (ChemMedChem 2/2013)

ChemMedChem ◽

10.1002/cmdc.201390004 ◽

2013 ◽

Vol 8 (2) ◽

pp. 344-344

Author(s):

Haijun Chen ◽

Cheng Z. Wang ◽

Chunyong Ding ◽

Christopher Wild ◽

Bryan Copits ◽

...

Keyword(s):

Ampa Receptor ◽

Allosteric Modulators ◽

Neuroprotective Agents ◽

Back Cover ◽

Positive Allosteric Modulators

Download Full-text

AMPA receptor positive allosteric modulators attenuate morphine tolerance and dependence

Neuropharmacology ◽

10.1016/j.neuropharm.2018.04.020 ◽

2018 ◽

Vol 137 ◽

pp. 50-58 ◽

Cited By ~ 5

Author(s):

Xiaoyu Hu ◽

Xuebi Tian ◽

Xiao Guo ◽

Ying He ◽

Haijun Chen ◽

...

Keyword(s):

Ampa Receptor ◽

Morphine Tolerance ◽

Allosteric Modulators ◽

Positive Allosteric Modulators

Download Full-text

AMPA Receptor Positive Allosteric Modulators: Potential for the Treatment of Neuropsychiatric and Neurological Disorders

Current Topics in Medicinal Chemistry ◽

10.2174/1568026616666160627114507 ◽

2016 ◽

Vol 16 (29) ◽

pp. 3536-3565 ◽

Cited By ~ 10

Author(s):

Tristan Reuillon ◽

Simon E. Ward ◽

Paul Beswick

Keyword(s):

Ampa Receptor ◽

Neurological Disorders ◽

Allosteric Modulators ◽

Positive Allosteric Modulators

Download Full-text

Discovery of Pyrazolo[1,5-a]pyrazin-4-ones as Potent and Brain Penetrant GluN2A-Selective Positive Allosteric Modulators Reducing AMPA Receptor Binding Activity

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2021.116576 ◽

2021 ◽

pp. 116576

Author(s):

Fumie Sakurai ◽

Takafumi Yukawa ◽

Asato Kina ◽

Masataka Murakami ◽

Kazuaki Takami ◽

...

Keyword(s):

Ampa Receptor ◽

Receptor Binding ◽

Binding Activity ◽

Allosteric Modulators ◽

Receptor Binding Activity ◽

Positive Allosteric Modulators

Download Full-text

MM-GBSA and MM-PBSA performance in activity evaluation of AMPA receptor positive allosteric modulators

Journal of Biomolecular Structure and Dynamics ◽

10.1080/07391102.2017.1360208 ◽

2017 ◽

Vol 36 (10) ◽

pp. 2508-2516 ◽

Cited By ~ 15

Author(s):

Dmitry S. Karlov ◽

Mstislav I. Lavrov ◽

Vladimir A. Palyulin ◽

Nikolay S. Zefirov

Keyword(s):

Ampa Receptor ◽

Allosteric Modulators ◽

Activity Evaluation ◽

Positive Allosteric Modulators

Download Full-text