GPCR Conformations: Implications for Rational Drug Design
GPCR Conformations: Implications for Rational Drug Design
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DOI：
10.3390/ph4010007
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发表时间：
2010-12-23
期刊：
影响因子：
4.6
通讯作者：
Bautista DL
中科院分区：
文献类型：
--
作者：
Parrill AL;Bautista DL
G蛋白偶联受体（GPCR）包括在正常生理学和病理生理学中起关键作用的一大类跨膜蛋白。这些关键作用为治疗干预提供了靶点，如靶向该家族成员的当前药剂的大部分所例示的。间接和直接的结构表征技术对我们理解气相化学还原反应的结构和动力学做出了巨大贡献。来自这两种类型的表征技术的GPCR构象的主要特点进行了审查。
G protein-coupled receptors (GPCRs) comprise a large class of transmembrane proteins that play critical roles in both normal physiology and pathophysiology. These critical roles offer targets for therapeutic intervention, as exemplified by the substantial fraction of current pharmaceutical agents that target members of this family. Tremendous contributions to our understanding of GPCR structure and dynamics have come from both indirect and direct structural characterization techniques. Key features of GPCR conformations derived from both types of characterization techniques are reviewed.