Department of Chemistry, University of Cambridge, Cambridge, CB2 1EW, UK.
Org Biomol Chem. 2020 Jul 1;18(25):4739-4743. doi: 10.1039/d0ob01002b.
A highly efficient disulfide rebridging strategy for the modification of monoclonal antibodies with substituted divinyltriazine linkers is reported. The reaction proceeds efficiently under mild conditions with near stoichiometric quantities of linker. This method of conjugation yields serum stable antibody conjugates with a controlled payload loading of 4.
报道了一种用于用取代的二乙烯三嗪连接物修饰单克隆抗体的高效二硫键重桥连策略。该反应在温和条件下以近乎化学计量的连接物高效进行。这种缀合方法得到的抗体缀合物在血清中稳定,载药量为 4。