作者: Yu-Hsuan Tsai , Sebastian Essig , John R. James , Kathrin Lang , Jason W. Chin
DOI: 10.1038/NCHEM.2253
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摘要: The rapid and selective regulation of a target protein within living cells that contain closely related family members is an outstanding challenge. Here we introduce genetically directed bioorthogonal ligand tethering (BOLT) demonstrate inhibition (iBOLT) function. In iBOLT, inhibitor-conjugate/target pairs are created where the contains encoded unnatural amino acid with reactivity inhibitor conjugate complementary group. iBOLT enables first specific MEK isozymes, introducing photoisomerizable linkers in reversible, optical activity (photo-BOLT) live mammalian cells. We pan kinase allows lymphocyte kinase, indicating modularity scalability BOLT. anticipate BOLT will enable diverse proteins for which no small molecule ligands exist.