Ligand binding modes from low resolution GPCR models and mutagenesis: chicken bitter taste receptor as a test-case.

ABSTRACT: Bitter taste is one of the basic taste modalities, warning against consuming potential poisons. Bitter compounds activate members of the bitter taste receptor (Tas2r) subfamily of G protein-coupled receptors (GPCRs). The number of functional Tas2rs is species-dependent. Chickens represent an intriguing minimalistic model, because they detect the bitter taste of structurally different molecules with merely three bitter taste receptor subtypes. We investigated the binding modes of several known agonists of a representative chicken bitter taste receptor, ggTas2r1. Because of low sequence similarity between ggTas2r1 and crystallized GPCRs (~10% identity, ~30% similarity at most), the combination of computational approaches with site-directed mutagenesis was used to characterize the agonist-bou

SUBMITTER: Di Pizio A 

PROVIDER: S-EPMC5557796 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature