催化作用
立体化学
DNA
化学
激活剂(遗传学)
部分
细胞生物学
辅因子
胞浆
生物化学
生物
受体
酶
作者
Zhen Zhao,Zhixing Ma,Bo Wang,Yukun Guan,Xiao‐Dong Su,Zhengfan Jiang
出处
期刊:Cell Reports
[Cell Press]
日期:2020-08-01
卷期号:32 (7): 108053-108053
被引量:295
标识
DOI:10.1016/j.celrep.2020.108053
摘要
DNA binding allosterically activates the cytosolic DNA sensor cGAS (cyclic GMP-AMP [cGAMP] synthase) to synthesize 2'3'-cGAMP, using Mg2+ as the metal cofactor that catalyzes two nucleotidyl-transferring reactions. We previously found that Mn2+ potentiates cGAS activation, but the underlying mechanism remains unclear. Here, we report that Mn2+ directly activates cGAS. Structural analysis reveals that Mn2+-activated cGAS undergoes globally similar conformational changes to DNA-activated cGAS but forms a unique η1 helix to widen the catalytic pocket, allowing substrate entry and cGAMP synthesis. Strikingly, in Mn2+-activated cGAS, the linear intermediates pppGpG and pGpA take an inverted orientation in the active pocket, suggesting a noncanonical but accelerated cGAMP cyclization without substrate flip-over. Moreover, unlike the octahedral coordination around Mg2+, the two catalytic Mn2+ are coordinated by triphosphate moiety of the inverted substrate, independent of the catalytic triad residues. Our findings thus uncover Mn2+ as a cGAS activator that initiates noncanonical 2'3'-cGAMP synthesis.
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