Structural mechanisms underlying activation of TRPV1 channels by pungent compounds in gingers.

ABSTRACT:

Background and purpose

Like chili peppers, gingers produce pungent stimuli by a group of vanilloid compounds that activate the nociceptive transient receptor potential vanilloid 1 (TRPV1) ion channel. How these compounds interact with TRPV1 remains unclear.

Experimental approach

We used computational structural modelling, functional tests (electrophysiology and calcium imaging), and mutagenesis to investigate the structural mechanisms underlying ligand-channel interactions.

Key results

The potency of three principal pungent compounds from ginger -shogaol, gingerol, and zingerone-depends on the same two residues in the TRPV1 channel that form a hydrogen bond with the chili pepper pungent compound, capsaicin. Computational modelling revealed binding poses of these ginge

SUBMITTER: Yin Y 

PROVIDER: S-EPMC6692589 | biostudies-literature | 2019 Sep

REPOSITORIES: biostudies-literature