Structure of the adenylyl cyclase catalytic core

Structure of the adenylyl cyclase catalytic core
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腺苷酸环化酶催化核心的结构

DOI:
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发表时间:
1997
期刊:
影响因子:
64.8
通讯作者:
J. Hurley
J. Hurley
中科院分区:
综合性期刊1区
文献类型:
--
作者:
Gongyi Zhang;Yu Liu;A. Ruoho;J. Hurley

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哺乳动物腺苷酸环化酶含有两个保守区域,C1和C2,它们负责毛喉素和G蛋白刺激的催化。II型大鼠腺苷酸环化酶C2催化区的结构具有α/β类折叠的环状二聚体,其具有中央裂缝。两个毛喉素分子结合在裂缝末端的疏水口袋中。裂缝的中心部分排列着与ATP结合有关的带电残基。毛喉素似乎通过促进活性二聚体的组装和催化裂缝内的直接相互作用来激活腺苷酸环化酶。其他腺苷酸环化酶调节剂作用于二聚体界面或柔性C末端区域。
Mammalian adenylyl cyclases contain two conserved regions, C1 and C2, which are responsible for forskolin- and G-protein-stimulated catalysis. The structure of the C2 catalytic region of type II rat adenylyl cyclase has an α/β class fold in a wreath-like dimer, which has a central cleft. Two forskolin molecules bind in hydrophobic pockets at the ends of cleft. The central part of the cleft is lined by charged residues implicated in ATP binding. Forskolin appears to activate adenylyl cyclase by promoting the assembly of the active dimer and by direct interaction within the catalytic cleft. Other adenylyl cyclase regulators act at the dimer interface or on a flexible C-terminal region.
DOI: 10.1126/science.2011744
发表时间: 1991-04-05
期刊: SCIENCE
影响因子: 56.9
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