Structural diversity of G protein-coupled receptors and significance for drug discovery

作者: Malin C. Lagerström , Helgi B. Schiöth

DOI: 10.1038/NRD2518

关键词: ReceptorStructural diversityG protein-coupled receptorBioinformaticsHuman genomeFrizzledBiologyComputational biologyDrug discoveryGlutamate receptorProtein structure

摘要: G protein-coupled receptors (GPCRs) are the largest family of membrane-bound and also targets many drugs. Understanding functional significance wide structural diversity GPCRs has been aided considerably in recent years by sequencing human genome studies, important implications for future therapeutic potential targeting this receptor family. This article aims to provide a comprehensive overview five main GPCR families--Rhodopsin, Secretin, Adhesion, Glutamate Frizzled/Taste2--with focus on gene repertoire, general ligand preference, common unique features, drug discovery.

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