Understanding TRPV1 activation by ligands: Insights from the binding modes of capsaicin and resiniferatoxin.

ABSTRACT: The transient receptor potential cation channel subfamily V member 1 (TRPV1) or vanilloid receptor 1 is a nonselective cation channel that is involved in the detection and transduction of nociceptive stimuli. Inflammation and nerve damage result in the up-regulation of TRPV1 transcription, and, therefore, modulators of TRPV1 channels are potentially useful in the treatment of inflammatory and neuropathic pain. Understanding the binding modes of known ligands would significantly contribute to the success of TRPV1 modulator drug design programs. The recent cryo-electron microscopy structure of TRPV1 only provides a coarse characterization of the location of capsaicin (CAPS) and resiniferatoxin (RTX). Herein, we use the information contained in the experimental electron density maps to accura

SUBMITTER: Elokely K 

PROVIDER: S-EPMC4720335 | biostudies-literature | 2016 Jan

REPOSITORIES: biostudies-literature