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Updated: Feb 1, 2026

Synthesis of Protein Bioconjugates via Cysteine-maleimide Chemistry
Published on: July 20, 2016
Cysteine-Directed Bioconjugation of a Platinum(II)-Acridine Anticancer Agent
Xiyuan Yao1, Christopher M Tracy1, Ulrich Bierbach1
1Department of Chemistry , Wake Forest University , Wake Downtown Campus , Winston-Salem , North Carolina 27101 , United States.
Abstract:
Classical maleimide Michael addition chemistry in conjunction with copper-free click chemistry was investigated as a synthetic strategy to attach cytotoxic platinum-acridine hybrid agents to carrier proteins. The structural integrity and selectivity of the model payloads, which were validated in human serum albumin (HSA) using mass spectrometric analysis and heteronuclear 2D 1H-15N HSQC NMR experiments, may have broad utility for the targeted delivery of highly cytotoxic platinum acridines and other nonclassical platinum containing anticancer agents.
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