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Org Lett. 2018 Oct 19;20(20):6526-6529. doi: 10.1021/acs.orglett.8b02849. Epub 2018 Oct 4.

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

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1
Shanghai Institute for Advanced Immunochemical Studies , ShanghaiTech University , 393 Middle Huaxia Road , Pudong , Shanghai 201210 , China.

Abstract

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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