Chemical site-selective modification of proteins is a key strategy for accessing and studying post-translational modifications (PTMs). Modified proteins have also gained prominence in many therapeutic approaches, including vaccine design and armed antibodies.Reaction engineering at cysteine: From disulfides to thioethers, a range of novel reactions and methods that enable controlled, specific modification of proteins at cysteine were developed. These methods are efficient strategies to access post-translational modifications such as phosphorylation, glycosylation, prenylation, or acetylation and methylation of lysine residues on proteins in a controllable, defined manner.Vascular targeting ADC: A novel strategy for the development of armed antibodies, chemically programmed for the amplified release of a potent cytotoxic drug in the tumor surroundings will be presented. Site-selective mixed disulfide formation directly at cysteine yielded an homogeneous, traceless ADC. When administered intravenously in a syngeneic immunocompetent model of murine cancer that is not cured by conventional cytotoxic agents alone, this vascular targeting ADC potently inhibits tumor growth.

Chemical site-selective protein modification: Development of a traceless vascular targeting ADC for cancer therapy

243rd National Meeting (2012)

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