Chinese Journal of Nature ›› 2021, Vol. 43 ›› Issue (5): 323-334.doi: 10.3969/j.issn.0253-9608.2021.05.002

• Special Issue for Advanced Immunochemical Studies • Previous Articles     Next Articles

Disulfide re-bridging for the construction of homogeneous antibody-drug conjugates

HUANG Rong①②, CHEN Hongli, JIANG Biao   

  1. ①Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, Shanghai 201210, China; ②School of Physical Science and Technology, ShanghaiTech University, Shanghai 201210, China
  • Received:2021-05-19 Online:2021-10-22 Published:2021-10-22

Abstract: Antibody-drug conjugates (ADCs) combine an antibody with highly potent drugs by chemical linkers, allowing to have both the efficacy of payloads and the targeting ability of antibodies for targeted and precise therapeutics. Currently, 10 ADCs have been approved by FDA. It is very important to develop site-specific conjugation method to obtain homogeneous ADCs with controllable drug-antibody ratio (DAR) for the next generation of ADCs. Recently, the “ThioBridge” method that is based on the reduction and re-bridging of the disulfides in an antibody has demonstrated its advantages: a direct chemical method to site-specific modify native antibody, wide applicability, controllable DAR and high homogeneity. Here, we briefly introduce the recent development and progress of disulfide re-bridging methods to construct homogeneous ADCs.

Key words:  , antibody-drug conjugate, site-specific conjugation, disulfide re-bridging, homogeneity