Synthesis and evaluation of highly releasable and structurally stable antibody-SN-38-conjugates

Lianqi Liu, Fei Xie, Dian Xiao, Xin Xu, Zheng Su, Yanming Wang, Shiyong Fan, Xinbo Zhou & Song Li
Camptothecins, traditional chemotherapy drugs, have been clinically used in antibody-drug conjugates (ADCs), which refreshes the recognition that ADCs preferably incorporate highly potent payloads. However, SN-38, active metabolite of irinotecan from camptothecins, tended to be incorporated into ADCs with an unstable acid sensitive bond, not with the widely used Cathepsin B (CTSB) sensitive bond, which may pose the risk of off-target. Herein, we reported a novel strategy to construct highly releasable and structurally stable SN-38-conjugates, in...
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