Journal
CHINESE CHEMICAL LETTERS
Volume 32, Issue 11, Pages 3623-3626Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.cclet.2021.04.015
Keywords
Amino-yne reaction; Progargylated sulfonium; Proximity-induced; MDM4
Categories
Funding
- National Key Research and Development Program Synthetic Biology Key Special Project of China [2018YFA0902504]
- Natural Science Foundation of China [21778009, 21977010]
- Natural Science Foundation of GuangdongProvince [2020A1515010766, 2020A1515010522, 2019A1515111184, 2019A1515110489]
- Shenzhen Science and Technology Innovation Committee [JCYJ20180507181527112, JCYJ20180508152213145, JCYJ20170817172023838]
- Beijing National Laboratory of Molecular Science Open Grant [BNLMS20160112]
- Shenzhen-Hong Kong Institute of Brain Science-Shenzhen Fundamental Research Institutions [2019SHIBS0004]
- Proteomic Platform of Pingshan Translational Medicine Center of Peking University
- Shenzhen Bay Laboratory of Peking University
- Peking University
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This study presents a novel bioorthogonal reaction that occurs at lysine residues through proximity-induced reactivity, providing a viable approach for lysine-targeted covalent inhibition in proteins.
Whilst most bioorthogonal reactions focus on targeting binding-site cysteine residues, proximity-induced reactivity effect ensures that reaction also occurs at nucleophilic lysine residues. We report one example here that the propargylated-sulfonium center undergoes a nucleophilic reaction with lysine residue via proximity-induced conjugation. This propargylated-sulfonium tethered peptide resulting from a facile propargylation of thiolethers, enables amino-yne reaction at the selected lysine on MDM4 protein. This strategy represents a viable approach of lysine-targeted covalent inhibition in proximity. (C) 2021 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.
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