| Baloucoune Guillaume Antoine 肖胜杰蒋明皮振钧黄思罗△.GPCRs 组成性活性的研究进展及意义[J].,2012,12(19):3784-3788 |
| GPCRs 组成性活性的研究进展及意义 |
| Recent Research and its Significance of the Constitutive Activity of GPCRs |
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| DOI： |
| 中文关键词: G 蛋白偶联受体 组成性活性 组成性活性突变体 激活机制 反向激动剂 |
| 英文关键词: GPCRs Constitutive activity CAM Activation mechanism Reverse Agonist |
| 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） |
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| 中文摘要: |
| GPCRs 是体内最大的蛋白质亚家族，其活性涉及体内绝大部分重要的生理和病理进程。研究表明，GPCRs 或其突变体能在
无配体结合的情况下自发产生部分甚至完全活性程度的生理活性，称之为组成性活性。据此研究者提出了GPCRs 激活过程中存
在多个中间激活态的观点，从而丰富了配体受体相互作用的经典模型，并使组成性活性突变体（constitutive active mutant, CAM）
成为研究GPCRs 的新方法。本文系统介绍了组成性活性的研究历程，以及近年来利用CAM 的方法研究GPCRs 的结构、激活机
制和活性调节的历程和进展，和体内组成性活性突变的成因和与疾病的关系，以及CAM 在研究药物作用机理和新药研发中的意
义。 |
| 英文摘要: |
| GPCRs are the largest protein subfamily in human genome, and its activity is involved in the most physiological and
pathological processes in vivo. Studies have shown that, GPCRs or its mutants spontaneously exhibit partly and even full activity in the
absence of ligand which named as constitutive activity. Therefore researchers proposed there exists many active states in the middle of
the activation process in GPCRs to enrich the classical ligand-receptor interaction model. And constitutively active mutant (CAM) is also
to be a new useful method to study GPCRs. This paper systematically describes the course and progress of CAM in recent years, included
the researches of GPCRs structure, activation mechanism and activity regulation illustrated by using CAM, the researches upon the
produce mechanism of CAM in vivo and its role in different disease, as well as the significance of CAM in pharmacology and new drugs
development. |
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