Engineering a minimal G protein to facilitate crystallisation of G protein-coupled receptors in their active conformation.

ABSTRACT: G protein-coupled receptors (GPCRs) modulate cytoplasmic signalling in response to extracellular stimuli, and are important therapeutic targets in a wide range of diseases. Structure determination of GPCRs in all activation states is important to elucidate the precise mechanism of signal transduction and to facilitate optimal drug design. However, due to their inherent instability, crystallisation of GPCRs in complex with cytoplasmic signalling proteins, such as heterotrimeric G proteins and β-arrestins, has proved challenging. Here, we describe the design of a minimal G protein, mini-G_s, which is composed solely of the GTPase domain from the adenylate cyclase stimulating G protein G_s Mini-G_s is a small, soluble protein, which efficiently couples GPCRs in t

SUBMITTER: Carpenter B 

PROVIDER: S-EPMC5181381 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature