| Literature DB >> 10090777 |
T H Khan1, E A Eno-Amooquaye, F Searle, P J Browne, H M Osborn, P J Burke.
Abstract
The 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.Entities:
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Year: 1999 PMID： 10090777 DOI： 10.1021/jm990004i
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446