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Peptidyl hydroxamic acids as methionine aminopeptidase inhibitors
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Jan2004, Vol. 14 Issue 1, p77-79. 3p. - Publication Year :
- 2004
-
Abstract
- A new class of methionine aminopeptidase (MetAP) inhibitors, which contain an internal hydroxamate (N-acyl-N-alkylhydroxylamine) core as the metal-chelating group, has been designed, synthesized, and tested. The compounds exhibited reversible, competitive inhibition against Escherichia coli MetAP as well as human MetAP-1 and MetAP-2. The most potent inhibitor had a Ki value of 2.5 μM and >20-fold selectivity toward E. coli MAP. [Copyright &y& Elsevier]
- Subjects :
- *ESCHERICHIA coli
*ENTEROBACTERIACEAE
*ORGANIC acids
*AMINOPEPTIDASES
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 14
- Issue :
- 1
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 22237765
- Full Text :
- https://doi.org/10.1016/j.bmcl.2003.10.031