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 Article Swipe
Jack A. Terrett
,
Huifen Chen
,
Daniel G. Shore
,
Elisia Villemure
,
Robin Larouche‐Gauthier
,
Martin Déry
,
Francis Beaumier
,
Léa Constantineau-Forget
,
Chantal Grand‐Maître
,
Luce Lépissier
,
Stéphane Ciblat
,
Claudio F. Sturino
,
Yong Chen
,
Baihua Hu
,
Aijun Lu
,
Yunli Wang
,
Andrew P. Cridland
,
Stuart I. Ward
,
David H. Hackos
,
Rebecca M. Reese
,
Shannon D. Shields
,
Jun Chen
,
Alessia Balestrini
,
Lorena Riol‐Blanco
,
Wyne P. Lee
,
John Liu
,
Eric Suto
,
Xiumin Wu
,
Juan Zhang
,
Justin Q. Ly
,
Hank La
,
Kevin M. Johnson
,
Matt Baumgardner
,
Kang-Jye Chou
,
Alexis Rohou
,
Lionel Rougé
,
Brian S. Safina
,
Steven Magnuson
,
Matthew Volgraf
·
YOU?
·
· 2021
· Open Access
·
· DOI: https://doi.org/10.1021/acs.jmedchem.0c02023
YOU?
·
· 2021
· Open Access
·
· DOI: https://doi.org/10.1021/acs.jmedchem.0c02023
Transient receptor potential ankyrin 1 (TRPA1) is a nonselective calcium-permeable ion channel highly expressed in the primary sensory neurons functioning as a polymodal sensor for exogenous and endogenous stimuli and has generated widespread interest as a target for inhibition due to its implication in neuropathic pain and respiratory disease. Herein, we describe the optimization of a series of potent, selective, and orally bioavailable TRPA1 small molecule antagonists, leading to the discovery of a novel tetrahydrofuran-based linker. Given the balance of physicochemical properties and strong in vivo target engagement in a rat AITC-induced pain assay, compound 20 was progressed into a guinea pig ovalbumin asthma model where it exhibited significant dose-dependent reduction of inflammatory response. Furthermore, the structure of the TRPA1 channel bound to compound 21 was determined via cryogenic electron microscopy to a resolution of 3 Å, revealing the binding site and mechanism of action for this class of antagonists.
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Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.1021/acs.jmedchem.0c02023
- OA Status
- green
- Cited By
- 45
- References
- 54
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W3139057296
All OpenAlex metadata
Raw OpenAlex JSON
- OpenAlex ID
-
https://openalex.org/W3139057296Canonical identifier for this work in OpenAlex
- DOI
-
https://doi.org/10.1021/acs.jmedchem.0c02023Digital Object Identifier
- Title
-
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 MicroscopyWork title
- Type
-
articleOpenAlex work type
- Language
-
enPrimary language
- Publication year
-
2021Year of publication
- Publication date
-
2021-03-22Full publication date if available
- Authors
-
Jack A. Terrett, Huifen Chen, Daniel G. Shore, Elisia Villemure, Robin Larouche‐Gauthier, Martin Déry, Francis Beaumier, Léa Constantineau-Forget, Chantal Grand‐Maître, Luce Lépissier, Stéphane Ciblat, Claudio F. Sturino, Yong Chen, Baihua Hu, Aijun Lu, Yunli Wang, Andrew P. Cridland, Stuart I. Ward, David H. Hackos, Rebecca M. Reese, Shannon D. Shields, Jun Chen, Alessia Balestrini, Lorena Riol‐Blanco, Wyne P. Lee, John Liu, Eric Suto, Xiumin Wu, Juan Zhang, Justin Q. Ly, Hank La, Kevin M. Johnson, Matt Baumgardner, Kang-Jye Chou, Alexis Rohou, Lionel Rougé, Brian S. Safina, Steven Magnuson, Matthew VolgrafList of authors in order
- Landing page
-
https://doi.org/10.1021/acs.jmedchem.0c02023Publisher landing page
- Open access
-
YesWhether a free full text is available
- OA status
-
greenOpen access status per OpenAlex
- OA URL
-
https://doi.org/10.7270/q2hq43vgDirect OA link when available
- Concepts
-
Chemistry, Transient receptor potential channel, Ankyrin, Biophysics, Mechanism of action, Ion channel, In vivo, Receptor, TRPV1, Pharmacology, Capsazepine, Biochemistry, In vitro, Biology, Biotechnology, Gene, MedicineTop concepts (fields/topics) attached by OpenAlex
- Cited by
-
45Total citation count in OpenAlex
- Citations by year (recent)
-
2025: 10, 2024: 17, 2023: 10, 2022: 5, 2021: 3Per-year citation counts (last 5 years)
- References (count)
-
54Number of works referenced by this work
- Related works (count)
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10Other works algorithmically related by OpenAlex
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| title | 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 |
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