β2肾上腺素受体结构研究进展精选.pdf

Hans Journal of Medicinal Chemistry 药物化学, 2015, 3, 1-10 Published Online February 2015 in Hans. /journal/hjmce /10.12677/hjmce.2015.31001 Current Progress of Structural Studies on β2 Adrenergic Receptor Lingli Tang, Peng Zhang, Xianlong Wang* Key Laboratory for NeuroInformation of Ministry of Education, School of Life Science and Technology, University of Electronic Science and Technology of China, Chengdu Sichuan * Email: WangXianlong@ th th th Received: Mar. 5 , 2015; accepted: Mar. 18 , 2015; published: Mar. 24 , 2015 Copyright © 2015 by authors and Hans Publishers Inc. This work is licensed under the Creative Commons Attribution International License (CC BY). /licenses/by/4.0/ Abstract Beta-2 adrenergic receptor is an important member among G protein-coupled receptors superfa- mily. As a membrane protein, it is difficult to crystalize and its three-dimensional structure is not known until recent years. Thanks to the development of the crystal engineering techniques and the breakthroughs in the free electron X-ray laser crystallography, many crystal structures of β2 adrenergic receptor at different states become available now. The discovery of the crystal struc- ture β2 adrenergic receptor has enriched our understanding on many life phenomena and its im- pact to the structure-based drug design cannot be overestimated. We review the discovery history of β2 adrenergic receptor crystal structures, the structural characteristics of the receptor, the in- teractions between the receptor and different subtypes of the ligands (agonist, inverse agonist and antagonist) and clinical applications. Keywords β Adrenergic Receptor, G Protein-Coupled Receptor, Crystal Struct