Open AccessBioorthogonal Chemical Activation of Kinases in Living Systems
Author(s) -
Gong Zhang,
Jie Li,
Ran Xie,
Xinyuan Fan,
Yanjun Liu,
Siqi Zheng,
Yun Ge,
Peng R. Chen
Publication year - 2016
Publication title -
acs central science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 4.893
H-Index - 76
eISSN - 2374-7951
pISSN - 2374-7943
DOI - 10.1021/acscentsci.6b00024
Subject(s) - bioorthogonal chemistry , kinase , lysine , biochemistry , cleavage (geology) , chemistry , phosphorylation , microbiology and biotechnology , tetrazine , biology , combinatorial chemistry , click chemistry , amino acid , organic chemistry , paleontology , fracture (geology)
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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