Format

Send to

Choose Destination
See comment in PubMed Commons below
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2129-32. doi: 10.1016/j.bmcl.2010.02.052. Epub 2010 Feb 16.

A cell-based assay that targets methionine aminopeptidase in a physiologically relevant environment.

Author information

1
Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA.

Abstract

Methionine aminopeptidase (MetAP) is a promising target for the development of novel antibiotics. However, many potent inhibitors of the purified enzyme failed to show significant antibacterial activity. It is uncertain which divalent metal MetAP uses as its native cofactor in bacterial cells. Herein, we describe a cell-based assay that monitors the hydrolysis of a fluorogenic substrate by overexpressed MetAP in permeabilized Escherichia coli cells and its validation with a set of MetAP inhibitors. This cell-based assay is applicable to those cellular targets with poorly defined native cofactor, increasing the chances of identifying inhibitors that can inhibit the cellular target.

PMID:
20207144
PMCID:
PMC2844763
DOI:
10.1016/j.bmcl.2010.02.052
[Indexed for MEDLINE]
Free PMC Article
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science Icon for PubMed Central
    Loading ...
    Support Center