NOVEL THIOL & AMINO MODIFYING REAGENTS FOR PROTEIN CHEMISTRY AND METHODS OF USE THEREOF

摘要

Provided herein are aryl and heteroaryl sulfone and sulfoxide modifying agents for facile and selective chemical alteration of proteins at thiol in cysteine residues, thiol- and selenol-containing moieties. Also provided herein are TAK242 derivatives for selective reaction with amino-containing compounds. The modifying agents disclosed herein can be used under mild reaction conditions for a variety of conjugation applications in molecules that possess amino, thiol or selenol functionalities. Also provided herein are methods of chemoselectively modifying a moiety containing the amino acids cysteine or lysine. Provided herein are CCR5 and CXCR antagonist derivatives modified for bioconjugation to macromolecules.