TRPA1 ankyrin repeat six interacts with a small molecule inhibitor chemotype.

ABSTRACT: TRPA1, a member of the transient receptor potential channel (TRP) family, is genetically linked to pain in humans, and small molecule inhibitors are efficacious in preclinical animal models of inflammatory pain. These findings have driven significant interest in development of selective TRPA1 inhibitors as potential analgesics. The majority of TRPA1 inhibitors characterized to date have been reported to interact with the S5 transmembrane helices forming part of the pore region of the channel. However, the development of many of these inhibitors as clinical drug candidates has been prevented by high lipophilicity, low solubility, and poor pharmacokinetic profiles. Identification of alternate compound interacting sites on TRPA1 provides the opportunity to develop structurally distinct modula

SUBMITTER: Tseng WC 

PROVIDER: S-EPMC6275487 | biostudies-literature | 2018 Nov

REPOSITORIES: biostudies-literature