Article

TRPV1 antagonism occurs through diverse structural mechanisms

2026-04-29

Abstract excerpt

Transient receptor potential vanilloid 1 (TRPV1) ion channel mediates thermosensation and pain and is a target for non-addictive analgesics; however, clinical candidates have failed due to thermoregulatory side effects. Limited structural data for human TRPV1 (hTRPV1) bound to clinically relevant antagonists has constrained mechanistic insight. Using chemoinformatics-informed cryo-EM and BRET assays, we define the...

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Literature Corpus work: f8040a5e-737d-511d-93b5-5ef9e6e3b892
DOI: 10.64898/2026.04.27.721197

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