A Chemoselective Strategy for Late-Stage Functionalization of Complex Small Molecules with Polypeptides and Proteins

Bradley Pentelute and Daniel Cohen use polypeptides and proteins in late-stage functionalization of small molecules.

The conjugation of small molecules to biopolymers has gained tremendous interest over the last several decades. These hybrid molecules can potentially harness the strengths of the small molecules and proteins to deliver new classes of therapeutics that were previously inaccessible with each component independently. Antibody drug conjugates (ADCs) for targeted cancer treatment highlight the promise of con-jugate therapies in modern medicine. Methods to construct these classes of molecules typically rely on the reaction of the nucleophilic residue within the biopolymer in combination with a preinstalled electrophilic handle on the small molecule of interest.
The groups of Professor Bradley Pentelute from the Massachusetts Institute of Technology (MIT, USA) and Dr. Daniel Cohen from AbbVie, Inc. (North Chicago, USA) found a new approach to prepare small-molecule–biopolymer conjugates using selenocysteine (Sec) as a bioconjugation handle.

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