材化部讲座教授(诺贝尔化学奖获得者)受聘仪式暨学术报告

报告题目:Biological applications of SuFEX click chemistry

报告人:诺贝尔化学奖获得者--- K. Barry Sharpless (The Scripps Research Institute, La Jolla, USA,Email: sharples@scripps.edu

报告时间:2017年9月18日下午,14:00-15:30

报告地点:独墅湖校区图书馆学术报告厅

K Barry Sharpless

                

Personal Introduction:  

 

Among a newer generation of scientists representing the entire chemical spectrum, from chemical engineering and materials to chemical biology, K. Barry Sharpless is known for click chemistry, a term he coined in 1998. Inspired by the complexity nature achieves from a handful of building blocks, Sharpless started actively looking in the mid-90s for a way to discover new chemical connectivity and reactivity. Click chemistry did not gain momentum until his group's discovery of CuAAC (the copper-catalyzed azide-alkyne cycloaddition), a near-perfect reaction (2002).  Recently the Sharpless group discovered SuFEx, also near-perfect for click chemistry. In concert with the thiol-ene reaction, these three make click chemistry a far-reaching method for drug discovery, chemical biology and materials science.

 

In 1963, K. Barry Sharpless graduated from Dartmouth College, where he was introduced, most fortuitously, to the wonders of chemistry by T. A. Spencer. Following graduate research with E. E. van Tamelen at Stanford University, Sharpless completed postdoctoral studies with J. P. Collman, also at Stanford, and at Harvard University with Konrad Bloch.

 

Sharpless set up his own laboratory in 1970 at the Massachusetts Institute of Technology.  Except for several years in the 1970s when he was a member of Stanford’s chemistry faculty, Sharpless remained at MIT until moving to the Scripps Research Institute (TSRI) in 1990. At TSRI he is W. M. Keck Professor of Chemistry and a member of the Skaggs Institute for Chemical Biology.

 

 

Abstract:

SuFEx, a new family of click chemistry reactions developed in my laboratory in 2014, relies on commercially available Vikane (sulfuryl fluoride, SO2F2) and ethenesulfonyl fluoride (ESF) to build diverse chemical structures bearing the SVI-F motif, such as -OSO2F (fluorosulfate) and -SO2F (sulfonyl fluoride). Since its development, SuFEx has found applications in materials science, chemical biology and drug discovery.

Arylfluorosulfates can be easily synthesized from phenol precursors and SO2F2 in the presence of an organic base via SuFEx. Arylfluorosulfates are usually stable in a biological environment, but become activated upon encountering a specific protein partner that possesses amino acid residues which can either react with fluorosulfate or facilitate the fluoride departure. This interaction leads to the formation of a covalent linkage between the protein partner and the probe. In this talk, I will discuss our recent efforts using this new approach to discover small molecules with anti-viral and anti-cancer activities. 



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