Structural pharmacology of TRPV channels.

Abstract

Transient Receptor Potential channels from the vanilloid subfamily (TRPV) are a group of cation channels that play a critical role in a variety of physiological and pathophysiological processes. They are modulated by a variety of endogenous stimuli as well as a range of natural and synthetic compounds. Their roles in human health make them of keen interest, particularly from a pharmacological perspective. However, despite this interest, the complexity of these channels has made it difficult to obtain high resolution structures until recently. With the cryo electron microscopy (cryo-EM) resolution revolution, our laboratory produced several TRPV channels structures and determine mechanisms of TRPV channels activation, inhibition and desensitization. This newly obtained information could guide us towards the design of novel TRPV channels specific therapeutic molecules.