Design and synthesis of a novel photoaffinity probe for labelling EGF receptor tyrosine kinases

Abstract

The epidermal growth factor receptor (EGFR) and HER2 are two important tyrosine kinases that play crucial roles in signal transduction pathways that regulate numerous cellular functions including proliferation, differentiation, migration, and angiogenesis. In the past 20 years, many proteomic methods have emerged as powerful methods to evaluate proteins in biological processes and human disease states. Among them, activity-based protein profiling (ABPP) is one useful approach for the functional analysis of proteins. In this study, a novel photoaffinity probe 11 was designed and synthesised to assess the target profiling of the reactive group in the photoaffinity probe 11. Biological evaluation was performed, and the results showed that the novel photoaffinity probe binds to EGFR and HER2 proteins and it hits targets by the reactive group.

Graphical Abstract

Keywords:

• Epidermal growth factor receptor
• activity-based protein profiling
• photoaffinity probe

Acknowledgements

The authors are grateful for the financial support by National Natural Science Foundation of China (81602951); Natural Science Foundation of Jiangsu Province (BK20130216, BK20140225); Six talent peaks project in Jiangsu Province (2016-SWYY-062); Science and technology project of Xuzhou City (KC16SG255); Jiangsu Key Laboratory of Brain Disease Bioinformation in Xuzhou Medical College (Jsbl11103).

Disclosure statement

The authors declare no conflict of interest.

Additional information

Funding

The authors are grateful for the financial support by National Natural Science Foundation of China (81602951); Natural Science Foundation of Jiangsu Province (BK20130216, BK20140225); Six talent peaks project in Jiangsu Province(2016-SWYY-062); Science and technology project of Xuzhou City (KC16SG255); Jiangsu Key Laboratory of Brain Disease Bioinformation in Xuzhou Medical College (Jsbl11103).