title: The identification of high-affinity G protein-coupled receptor ligands from large combinatorial libraries using multicolor quantum dot-labeled cell-based screening.
abstract: G protein-coupled receptors (GPCRs), which are involved in virtually every biological process, constitute the largest family of transmembrane receptors. Many top-selling and newly approved drugs target GPCRs. In this review, we aim to recapitulate efforts and progress in combinatorial library-assisted GPCR ligand discovery, particularly focusing on one-bead-one-compound library synthesis and quantum dot-labeled cell-based assays, which both effectively enhance the rapid identification of GPCR ligands with higher affinity and specificity.
authors.affiliation: Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL, 32610, USA.
authors.forename: Junjie
authors.initials: J
authors.lastname: Fu
authors.forename: Timothy
authors.initials: T
authors.lastname: Lee
authors.forename: Xin
authors.initials: X
authors.lastname: Qi
mesh_terms: D000818:Animals; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D008024:Ligands; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology; D045663:Quantum Dots / Q000032:analysis; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000378:metabolism*; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D008024:Ligands; D010455:Peptides; D043562:Receptors, G-Protein-Coupled; D054852:Small Molecule Libraries