• J. Med. Chem. · Mar 1999

    Novel inhibitors of carboxypeptidase G2 (CPG2): potential use in antibody-directed enzyme prodrug therapy.

    • T H Khan, E A Eno-Amooquaye, F Searle, P J Browne, H M Osborn, and P J Burke.
    • Imperial College of Science, Technology and Medicine, Charing Cross Site, Medical Oncology, St. Dunstan's Road, London W6 8RF, UK.
    • J. Med. Chem. 1999 Mar 25; 42 (6): 951-6.

    AbstractThe design and synthesis of potent thiocarbamate inhibitors for carboxypeptidase G2 are described. The best thiocarbamate inhibitor N-(p-methoxybenzenethiocarbonyl)amino-L-glutamic acid 6d, chosen for preliminary investigations of in vitro antibody-directed enzyme prodrug therapy (ADEPT), abrogated the cytotoxicity of a combination of A5B7-carboxypeptidase G2 conjugate and prodrug PGP (N-p-{N,N-bis (2-chloroethyl)amino}phenoxycarbonyl-L-glutamate) toward LS174T cells. This is the first report of a small-molecule enzyme inhibitor proposed for use in conjunction with the ADEPT approach.

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