Mammalian class I odorant receptors exhibit a conserved vestibular-binding pocket.

ABSTRACT: Odorant receptors represent the largest family of mammalian G protein-coupled receptors. Phylogenetically, they are split into two classes (I and II). By analyzing the entire subclass I odorant receptors sequences, we identified two class I-specific and highly conserved motifs. These are predicted to face each other at the extra-cellular portion of the transmembrane domain, forming a vestibular site at the entrance to the orthosteric-binding cavity. Molecular dynamics simulation combined with site-directed mutagenesis and in vitro functional assays confirm the functional role of this vestibular site in ligand-driven activation. Mutations at this part of the receptor differentially affect the receptor response to four agonists. Since this vestibular site is involved in ligand recognition, i

SUBMITTER: Bushdid C 

PROVIDER: S-EPMC7313674 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature