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 targeting this enzyme to tumors on an Ep-CAM1-specific antibody, ING1. Through the use of this >99% human enzyme which is...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.