2. Academic Validation
  3. 2 H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells

2 H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells

  • J Am Chem Soc. 2020 Apr 1;142(13):6051-6059. doi: 10.1021/jacs.9b12116.
Nan Ma 1,  Jun Hu 1,  Zhi-Min Zhang 1,  Wenyan Liu 1,  Minhao Huang 1,  Youlong Fan 1,  Xingfeng Yin 2,  Jigang Wang 3 4,  Ke Ding 1,  Wencai Ye 1,  Zhengqiu Li 1
Affiliations

Affiliations

  • 1 School of Pharmacy, Jinan University, International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development, Ministry of Education (MOE) of China, 601 Huangpu Avenue West, Guangzhou 510632, China.
  • 2 Institute of Life and Health Engineering, College of Life Science and Technology, Jinan University, Guangdong 510632, China.
  • 3 The Second Clinical Medical College of Jinan University, Shenzhen People's Hospital, Shenzhen 518020, China.
  • 4 Artemisinin Research Center and Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
PMID: 32159959 DOI: 10.1021/jacs.9b12116
Abstract

Protein modification by chemical reagents has played an essential role in the treatment of human diseases. However, the reagents currently used are limited to the covalent modification of cysteine and lysine residues. It is thus desirable to develop novel methods that can covalently modify Other residues. Despite the fact that the carboxyl residues are crucial for maintaining the protein function, few selective labeling reactions are currently available. Here, we describe a novel reactive probe, 3-phenyl-2H-azirine, that enables chemoselective modification of carboxyl groups in proteins under both in vitro and in situ conditions with excellent efficiency. Furthermore, proteome-wide profiling of reactive carboxyl residues was performed with a quantitative chemoproteomic platform.

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