Synlett 2017; 28(15): 1934-1938
DOI: 10.1055/s-0036-1590974
cluster
© Georg Thieme Verlag Stuttgart · New York

Polyfluorophenyl Ester-Terminated Homobifunctional Cross-Linkers for Protein Conjugation

Jian Wang ◊, Ru-Yan Zhang ◊, Ya-Cong Wang, Xiang-Zhao Chen, Xu-Guang Yin, Jing-Jing Du, Ze Lei, Ling-Ming Xin, Xiao-Fei Gao, Zheng Liu*, Jun Guo*
  • Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, CCNU-uOttawa Joint Research Centre, Hubei International Scientific and Technological Cooperation Base of Pesticide and Green Synthesis, College of Chemistry, Central China Normal University, Wuhan, Hubei 430079, P. R. China   Email: liuz1118@mail.ccnu.edu.cn   Email: jguo@mail.ccnu.edu.cn
We are grateful to the National Key Research and Development Program of China (2017YFA0505200), the National Natural Science Foundation of China (21402058 and 21272084), and the self-determined research funds of CCNU from the college’s basic research and operation of MOE (CCNU16A02001) for support of this research. Assistance from the Program of Introducing Talents of Discipline to Universities of China (111 program, B17019) is also acknowledged
Further Information

Publication History

Received: 30 April 2017

Accepted after revision: 03 July 2017

Publication Date:
08 August 2017 (eFirst)

Equal contributions from these authors

Published as part of the Cluster Recent Advances in Peptide and Protein Synthesis

Abstract

Along with N-hydroxysuccinimidyl, p-nitrophenyl, and phenylseleno esters, tetra- and penta-fluorophenyl esters were comparatively evaluated in term of their reactivity and hydrolytic stability. Their homobifunctional cross-linkers were prepared to conjugate proteins with small molecules, including carbohydrates, fluorescent dyes, and poly(ethylene glycol) monomethyl ether. The conjugations proceeded under mild conditions, affording the corresponding protein conjugates with good efficiency.

Supporting Information