Polyfluorophenyl Ester-Terminated Homobifunctional Cross-Linkers for Protein ConjugationWe 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
Received: 30 April 2017
Accepted after revision: 03 July 2017
08 August 2017 (eFirst)
◊Equal contributions from these authors
Published as part of the Cluster Recent Advances in Peptide and Protein Synthesis
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.