文章摘要

腺苷酸环化酶的研究进展

作者: 1杨 琰茗, 1杨 雅清, 1宋 杲, 1杨 为民, 1翁 稚颖
1 昆明医科大学药学院暨云南省天然药物药理重点实验室,昆明 650500
通讯: 翁 稚颖 Email: weng_zy@sina.com
DOI: 10.3978/j.issn.2095-6959.2019.02.026
基金: 国家自然科学基金 (81860012);云南省科学基金 (2017FE467-023);滇美分子药物联合研究中心 (2015ID001)。

摘要

腺苷酸环化酶(adenyl cyclase,AC)是G蛋白偶联受体(G protein-coupled receptor,GPCR)下游的关键信号分子,通过调节环腺苷-3',5'-一磷酸(cAMP)的合成调控多种细胞功能,从而参与机体的多种病理生理过程。哺乳动物细胞表达了9个跨膜AC亚型(AC1~9,mACs)和1个可溶性AC(sAC,也称为AC10),各亚型在不同组织细胞膜微筏(脂筏)中存在差异性表达,由于不同亚型间具有非特异的交叉协同性或拮抗性,各亚型的非选择性激活/抑制会带来很多潜在的不良反应,因此目前还缺乏特异性的激动剂和抑制剂。认识和了解AC各亚型的研究现状,对进一步研究各亚型特异性激动剂/抑制剂及未来靶向药物的研究具有重要意义。
关键词: 腺苷酸环化酶;亚型;特异性

Research progress of adenylate cyclase

Authors: 1YANG Yanming, 1YANG Yaqing, 1SONG Gao, 1YANG Weimin, 1WENG Zhiying
1 School of Pharmaceutical Science & Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming 650500, China

CorrespondingAuthor:WENG Zhiying Email: weng_zy@sina.com

Foundation: This work was supported by the National Natural Science Foundation (81860012), Yunnan Provincial Science and Technology Department (2017FE467-023)

Abstract

Adenyl cyclase (AC), as a key downstream signaling factor of G protein -coupled receptor (GPCR), is involved in a variety of potential physiological and pathological processes by adjusting the cyclic adenosine-3', 5'-monophosphate (cAMP). So far, nine membrane isoforms (AC1–9) and a soluble adenyl cyclase (sAC) have been cloned. They are expressed in different organs, and have different physiological functions. Non-selective activation/inhibition has many potential side effects. In this article we will summarize the current research of AC isoforms. Research on specific agonists/inhibitors and potential targeted drugs is of great significance.
Keywords: adenyl cyclase; isoforms; specificity