1641547-33-2Relevant academic research and scientific papers
2 H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells
Ding, Ke,Fan, Youlong,Hu, Jun,Huang, Minhao,Li, Zhengqiu,Liu, Wenyan,Ma, Nan,Wang, Jigang,Ye, Wencai,Yin, Xingfeng,Zhang, Zhi-Min
, p. 6051 - 6059 (2020)
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.
Azacyclopropene compound, and preparation method and application thereof
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Paragraph 0103; 0106; 0113-0114; 0116, (2020/11/01)
The invention relates to an azacyclopropene compound with a structure as shown in a formula I, and a preparation method and application thereof. The azacyclopropene compound has high selectivity and high efficiency in labeling (modifying) protein amino acid residues, can selectively modify acidic amino acid residues, has a good labeling effect, can be used for researching the activity of proteins,and is crucial to chemical proteomics application and development of covalent inhibitors.
Gold-catalyzed synthesis of functionalized pyridines by using 2H-azirines as synthetic equivalents of alkenyl nitrenes
Prechter, Agnes,Henrion, Guilhem,Faudot Dit Bel, Pierre,Gagosz, Fabien
, p. 4959 - 4963 (2014/05/20)
2H-Azirines are easily synthesized from the corresponding ketones and, despite possessing a C=N bond embedded in a strained three-membered cycle, they are sufficiently stable to be isolated, stored, and manipulated. 2H-Azirines can be regarded as valuable
