Nucleic acid ligands act as a PAM and agonist depending on the intrinsic ligand binding state of P2RY2.

ABSTRACT: G protein-coupled receptors (GPCRs) play diverse roles in physiological processes, and hence the ligands to modulate GPCRs have served as important molecules in biological and pharmacological approaches. However, the exploration of novel ligands for GPCR still remains an arduous challenge. In this study, we report a method for the discovery of nucleic acid ligands against GPCRs by an advanced RNA aptamer screening technology that employs a virus-like particle (VLP), exposing the GPCR of interest. An array of biochemical analyses coupled with a cell-based assay revealed that one of the aptamers raised against purinergic receptor P2Y2 (P2RY2), a GPCR, exhibits an activation potency to unliganded receptor and prohibits a further receptor activation by endogenous ligand, behaving like a partia

SUBMITTER: Takahashi M 

PROVIDER: S-EPMC8106294 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature