Over one hundred peptide-activated G protein-coupled receptors recognize ligands with turn structure.

摘要: G protein-coupled receptors (GPCRs) constitute the largest family of cellular involved in signal transduction. A review is given voluminous structural and/or activity evidence support a ligand turn shape being likely recognition domain GPCR-binding domains all these ligands. In absence structurally defined GPCR-ligand complexes, solution or solid-state structures are analyzed for variety ligands alone, including (i) peptide and protein hormone ligands, (ii) bioactive fragments, (iii) cyclic peptides, often analogous segments, (iv) peptidomimetic antagonists with conformational bias enforced by presence turn-inducing constraints. Examples small peptidomimetics naturally occurring peptides also covered, including, somatosatin (14 residues), melanocyte-stimulating (13), oxytocin (9), vasopressin substance P (11), bradykinin opiod fragments proteins.