Abstract
G protein coupled receptors (GPCRs) conduct the majority of cellular responses to hormones and neurotransmitters, and are therefore the largest group of pharmaceutical targets for a broad spectrum of diseases. Identification of genes for GPCRs, initially through cloning and subsequently through database mining, raised hopes for the rapid discovery of new therapeutics. However, the number of new approved drugs for GPCR targets over the past two decades has fallen short of expectations. I will discuss challenges in GPCR drug discovery and the potential impact of structural biology and other scientific advances on future drug discovery efforts.
