G-protein coupled receptor structure

摘要: Because of their central role in regulation cellular function, structure/function relationships for G-protein coupled receptors (GPCR) are vital importance, yet only recently have sufficient data been obtained to begin mapping those relationships. GPCRs regulate a wide range processes, including the senses taste, smell, and vision, control myriad intracellular signaling systems response external stimuli. Many diseases linked GPCRs. A critical need exists structural information inform studies on mechanism receptor action regulation. X-ray crystal structures one GPCR, an inactive state, date. However considerable variety has using non-crystallographic approaches. This review begins with very earliest GPCR information, mostly derived from rhodopsin. difficulty crystallizing crystallography, extensive published work utilizing alternative approaches structure is reviewed, determination three-dimensional sparse constraints. The available crystallographic analyses bovine rhodopsin reviewed as high-resolution any GPCR. Structural ligand binding several included. limited excited states also reviewed. It concluded that while basic obtained, more needed describe molecular activation