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N-Methyl- N-phenylvinylsulfonamides for Cysteine-Selective Conjugation.

Rong Huang, Zhihong Li, Yao Sheng, Jianghui Yu, Yue Wu, Yuexiong Zhan, Hongli Chen, Biao Jiang
Organic Letters 2018 October 5
Use of N-methyl- N-phenylvinylsulfonamides to perform chemoselective modification of cysteine-containing peptides and proteins is reported. Probes linked to the drug were applicable to prepare antibody-drug conjugates (ADCs). The drug-antibody ratio for ADCs was controlled by rationally tuning the electron deficiency and linker hydrophilicity of the probes.

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