Chapter 1 - Progress in GPCR structure determination

Abstract

G protein-coupled receptors (GPCRs) are widely distributed in the human body and trigger cellular responses to a variety of extracellular stimuli. The diverse functions of GPCRs make these receptors key players in numerous physiological regulations and valuable drug targets for many diseases. The GPCR structures are important for understanding the molecular mechanisms of GPCR signaling and enable structure-based drug discovery. Recent advances in GPCR structure determination have provided valuable insights into ligand recognition, receptor activation, and signaling transduction of these receptors. Here we summarize the recent progress, techniques, and discoveries in GPCR structural studies to elucidate the successful strategies for GPCR structure determination and structural basis of GPCR function.