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Updated: May 2, 2026

Genetic Encoding of a Non-Canonical Amino Acid for the Generation of Antibody-Drug Conjugates Through a Fast Bioorthogonal Reaction
Published on: September 14, 2018
Chemically programmed antibodies
1Department of Cancer Biology, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #2C1, Jupiter, FL 33458, USA; Department of Molecular Therapeutics, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #2C1, Jupiter, FL 33458, USA.
Abstract:
Due to their unlimited chemical diversity, small molecules can rival monoclonal antibodies (mAbs) with respect to specificity and affinity for target molecules. However, key pharmacological properties of mAbs remain unmatched by small molecules. Chemical programming strategies have been developed for site-specific and covalent conjugation of small molecules to mAbs with unique reactivity centers. In addition to blending favorable features of small molecules and mAbs, chemically programmed antibodies (cpAbs) are economically attractive because they utilize the same mAb for an almost unlimited number of target molecule specificities, reducing manufacturing costs and shortening drug discovery and development time. Preclinical studies and clinical trials have begun to demonstrate the broad utility of cpAbs for the treatment and prevention of human diseases.
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