title: Diels-Alder reaction-triggered bioorthogonal protein decaging in living cells.
abstract: Small molecules that specifically activate an intracellular protein of interest are highly desirable. A generally applicable strategy, however, remains elusive. Herein we describe a small molecule-triggered bioorthogonal protein decaging technique that relies on the inverse electron-demand Diels-Alder reaction for eliminating a chemically caged protein side chain within living cells. This method permits the efficient activation of a given protein (for example, an enzyme) in its native cellular context within minutes.
authors.affiliation: Synthetic and Functional Biomolecules Center, Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Li
authors.affiliation: Synthetic and Functional Biomolecules Center, Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing, China.
authors.forename: Shang
authors.initials: S
authors.lastname: Jia
authors.affiliation: 1] Synthetic and Functional Biomolecules Center, Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing, China. [2] Peking-Tsinghua Center for Life Sciences, Beijing, China.
authors.forename: Peng R
authors.initials: PR
authors.lastname: Chen
mesh_terms: D061565:Cycloaddition Reaction; D004583:Electrons; D004789:Enzyme Activation; D004926:Escherichia coli / Q000235:genetics / Q000378:metabolism; D015870:Gene Expression; D017930:Genes, Reporter; D057809:HEK293 Cells; D006801:Humans; D008156:Luciferases / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism; D008163:Luminescent Measurements; D008239:Lysine / Q000737:chemistry*; D008968:Molecular Conformation; D010957:Plasmids; D011994:Recombinant Proteins / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D054852:Small Molecule Libraries / Q000737:chemistry*; D013194:Staining and Labeling / Q000379:methods; D013777:Tetrazoles / Q000737:chemistry*
chemical_list: D011994:Recombinant Proteins; D054852:Small Molecule Libraries; D013777:Tetrazoles; D008156:Luciferases; D008239:Lysine