Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy-Reference-Cited by-同舟云学术

Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy

Published:2021-03-22 Issue:7 Volume:64 Page:3843-3869
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Terrett Jack A.¹^ORCID,Chen Huifen¹^ORCID,Shore Daniel G.¹,Villemure Elisia¹,Larouche-Gauthier Robin²,Déry Martin²,Beaumier Francis²,Constantineau-Forget Léa²,Grand-Maître Chantal²,Lépissier Luce²,Ciblat Stéphane²,Sturino Claudio²,Chen Yong³,Hu Baihua³,Lu Aijun³,Wang Yunli³,Cridland Andrew P.⁴,Ward Stuart I.⁴,Hackos David H.⁵,Reese Rebecca M.⁵,Shields Shannon D.⁵,Chen Jun⁶,Balestrini Alessia⁷,Riol-Blanco Lorena⁷,Lee Wyne P.⁸,Liu John⁸,Suto Eric⁸,Wu Xiumin⁸,Zhang Juan⁸,Ly Justin Q.⁹,La Hank⁹,Johnson Kevin⁹^ORCID,Baumgardner Matt⁹,Chou Kang-Jye¹⁰,Rohou Alexis¹¹,Rougé Lionel¹¹,Safina Brian S.¹^ORCID,Magnuson Steven¹,Volgraf Matthew¹

Affiliation:

1. Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

2. Paraza Pharma, Inc. 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada

3. Pharmaron-Beijing Co. Ltd., 6 Taihe Road, BDA, Beijing 100176, PR China

4. Charles River Laboratories, 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom

5. Department of Neurosciences, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

6. Department of Biochemical and Cellular Pharmacology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

7. Department of Discovery Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

8. Department of Translational Immunology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

9. Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

10. Department of Small Molecule Pharmaceutical Sciences, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

11. Department of Structural Biology, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.0c02023

Reference54 articles.

1. An Ankyrin-like Protein with Transmembrane Domains Is Specifically Lost after Oncogenic Transformation of Human Fibroblasts

2. ANKTM1, a TRP-like Channel Expressed in Nociceptive Neurons, Is Activated by Cold Temperatures

3. TRPA1 as a drug target—promise and challenges

4. Structure of the TRPA1 ion channel suggests regulatory mechanisms

5. Nociceptor and Hair Cell Transducer Properties of TRPA1, a Channel for Pain and Hearing

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