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Bioorthogonal Chemical Activation of Kinases in Living Systems.

ABSTRACT: 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.

SUBMITTER: Zhang G

PROVIDER: S-EPMC4882735 | biostudies-literature | 2016 May

REPOSITORIES: biostudies-literature

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Bioorthogonal Chemical Activation of Kinases in Living Systems.

Zhang Gong G Li Jie J Xie Ran R Fan Xinyuan X Liu Yanjun Y Zheng Siqi S Ge Yun Y Chen Peng R PR

ACS central science 20160427 5

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 decagin ...[more]

PMID: 27280167

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