Structures of non-rhodopsin GPCRS elucidated through X-ray crystallography

Abstract

During the last decade, more than 130 structures of G Protein-Coupled Receptors were solved mostly using X-ray crystallography, either bound to antagonist, agonist or in complexes with intracellular partners such as G-proteins and arrestin. These structures shed light on molecular mechanisms of GPCR ligand recognition, activation, and allosteric modulation. This is primarily due to tremendous advances in protein engineering and micro-crystallography making GPCRs structure determination more straightforward. This chapter presents an overview of the widely used and successful approaches that led to atomic resolution structures of GPCR. Moreover, we briefly introduce recent technological advancements in the structural biology field that will undoubtedly accelerate solving GPCRs structure in the foreseeable future and provide a more complete understanding of GPCR signaling.