| 阮嫔1 赵菡1 薛礼1 蒋明1 黄思罗1△.C 族GPCRs 的半胱氨酸富集区的研究进展及药学意义[J].,2012,12(9):1755-1759 |
| C 族GPCRs 的半胱氨酸富集区的研究进展及药学意义 |
| Recent Research and its Pharmacologic Significance on Cysteine-RichDomain of Class C GPCRs |
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| DOI： |
| 中文关键词: C 族G 蛋白偶联受体 CRD 激活机制 构象变化 |
| 英文关键词: Class C GPCRs CRD Activation mechanism Allosteric change |
| 基金项目:第47 批中国博士后面上基金(20100471184)；国家自然科学面上基金（30973514,31100548） |
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| 中文摘要: |
| C 族GPCRs 是体内重要的受体，参与众多重要的生理和病理进程，并具有复杂的结构和激活机制。在体内该族受体形成组
成性的二聚体并具有七螺旋跨膜结构（heptahelical transmembrane domain，HD）、捕蝇草模块（venus flytrap domain，VFT）和半胱氨
酸富集区（cysteine-rich domain，CRD）。本文系统介绍了近年来CRD 单体的序列和结构解析，以及参与受体激活过程的机制研究
的历程和进展。同时也展望了这些基础研究成果对于开发新的更具有成药性的以C 族GPCRs 为靶点的变构剂的指导意义。 |
| 英文摘要: |
| Class C GPCRs are important receptors in vivo and involved in many physiologic and pathologic process. These
receptors have complex structure and active mechanism. They are constitutive dimer and each monomer is composed of transmembrane
HD (heptahelical transmembrane domain), extracellular VFT (venus flytrap domain) and CRD (cysteine-rich domain) which between in
VFT and CRD. Although there are many results in the activation mechanism of these receptors, but until recently the role of CRD in the
activation process is largely unknown. So we reviewed the course and advance of the research in the sequence, structure, function, and
their conformation change in the activation process of these receptor dimmers. And lastly we also point the significance and new insights
of the Class C GPCR based-drug discovery to gain the new allosteric modulators which have better clinic implication.. |
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