The Resurgence of Covalent Drug

 

Reporter: Xuedong Li

CAS Key laboratory of Molecular Recognition and Function, Institute of Chemistry, CAS

2017年9月1日（星期五）  下午16:00，5号楼0100室

Small molecule drugs exert their pharmacological effects through binding to biomolecular targets, thereby modulating their activity (in the enzymes) or downstream signaling (in the case of receptors) with biological consequences that are relevant to the disease state being treated. In the history of therapeutics, covalent drugs occupy a very distinct category. While representing a significant fraction of the drugs on the market, very few have been deliberately designed to interact covalently with their biological target. The prevalence and pharmacological advantage of covalent drugs will be briefly covered, followed by an introduction to their mechanism of action and more detailed discussions of their discovery and the development of safe and efficient covalent enzyme inhibitors.

References

[1] J. Singh et al., Nat. Rev. Drug Discov., 2011, 11, 307-317.

[2] N. Moitessier et al. Eur. J. Med. Chem., 2017, 138, 96-114.

[3] A. S. Kalgutkar et al. Expert. Opin. Drug Discov., 2012, 7, 561-581.

[4] Y. Aye et al. Cell Chem. Bio., 2017, 24, 787-800.

 

CURRICULUM VITE

EDUCATION

2010-2014        HeBei North University

2014-present   Institute of Chemistry, CAS  Ph.D. (Supervisor. Prof. Liang Cheng)