Direct Selection of DNA-Encoded Libraries for Biased Agonists of GPCRs on Live Cells.

ABSTRACT: G protein-coupled receptors (GPCRs) are the largest superfamily of human membrane target proteins for approved drugs. GPCR ligands can have a complex array of pharmacological activities. Among these activities, biased agonists have potential to serve as both chemical probes to understand specific aspects of receptor signaling and therapeutic leads with more specific, desired activity. Challenges exist, however, in the development of new biased activators due, in part, to the low throughput of traditional screening approaches. DNA-encoded chemical libraries (DELs) dramatically improve the throughput of drug discovery by allowing a collective selection, rather than discrete screening, of large compound libraries. The use of DELs has been largely limited to affinity-based selections against p

SUBMITTER: Cai B 

PROVIDER: S-EPMC10131204 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature