期刊
ACS CENTRAL SCIENCE
卷 2, 期 5, 页码 325-331出版社
AMER CHEMICAL SOC
DOI: 10.1021/acscentsci.6b00024
关键词
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Selective manipulation of protein kinases under living conditions is highly desirable yet extremely challenging, particularly in a gain-of-function fashion. Here we employ our recently developed bioorthogonal cleavage reaction as a general strategy for intracellular activation of individual kinases. Site-specific incorporation of trans-cyclooctene-caged lysine in place of the conserved catalytic lysine, in conjunction with the cleavage partner dimethyl-tetrazine, allowed efficient lysine decaging with the kinase activity chemically rescued in living systems.
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