Engineering of Challenging G Protein-Coupled Receptors for Structure Determination and Biophysical Studies.

ABSTRACT: Membrane proteins such as G protein-coupled receptors (GPCRs) exert fundamental biological functions and are involved in a multitude of physiological responses, making these receptors ideal drug targets. Drug discovery programs targeting GPCRs have been greatly facilitated by the emergence of high-resolution structures and the resulting opportunities to identify new chemical entities through structure-based drug design. To enable the determination of high-resolution structures of GPCRs, most receptors have to be engineered to overcome intrinsic hurdles such as their poor stability and low expression levels. In recent years, multiple engineering approaches have been developed to specifically address the technical difficulties of working with GPCRs, which are now beginning to make more chall

SUBMITTER: Waltenspuhl Y 

PROVIDER: S-EPMC7962830 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature