Article
Antibody-directed enzyme prodrug therapy with the T268G mutant of human carboxypeptidase A1: in vitro and in vivo studies with prodrugs of methotrexate and the thymidylate synthase inhibitors GW1031 and GW1843.
Bioconjugate chemistry - 1 Jan 2000
Wolfe L A, Mullin R J, Laethem R, Blumenkopf T A, Cory M, Miller J F, Keith B R, Humphreys J, Smith G K
Abstract excerpt
Antibody-directed enzyme prodrug therapy (ADEPT) is a technique to increase antitumor selectivity in cancer chemotherapy. Our approach to this technology has been to design a mutant of human carboxypeptidase A (hCPA1-T268G) which is capable of hydrolyzing in vivo stable prodrugs of MTX and target...
Topics
- Adenocarcinoma
- Animals
- Antibodies
- Antimetabolites, Antineoplastic
- Carboxypeptidases
- Carboxypeptidases A
- Chromatography, High Pressure Liquid
- Colonic Neoplasms
- Drug Stability
- Enzyme Inhibitors
- Female
- Folic Acid Antagonists
- Glutamic Acid