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Peptidyl hydroxamic acids as methionine aminopeptidase inhibitors

Authors :
Hu, Xubo
Zhu, Jinge
Srivathsan, Sumant
Pei, Dehua
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]

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