Allostery: A GPCR’s back door

July 18th, 2014 by Klaus Mohr

Nature Chemical Biology 10, 609 (2014). doi:10.1038/nchembio.1583

Authors: Klaus Mohr & Evi Kostenis

Conventional allosteric modulators of G protein–coupled receptors (GPCRs) bind their target from the extracellular site. A new study shows that a GPCR's intracellular face can likewise be exploited. In particular, they sensitize a class B GPCR for activation by a hardly active peptide-hormone metabolite.