Send to:

Choose Destination
See comment in PubMed Commons below
Biochem Biophys Res Commun. 2013 Jul 19;437(1):162-7. doi: 10.1016/j.bbrc.2013.06.060. Epub 2013 Jun 24.

Screening-based discovery of the first novel ATP competitive inhibitors of the Staphylococcus aureus essential enzyme UMP kinase.

Author information

  • 1Discovery Sciences, AstraZeneca R&D Boston, Waltham, MA 02451, United States.


UMP kinase (PyrH) is an essential enzyme found only in bacteria, making it ideal as a target for the discovery of antibacterials. To identify inhibitors of PyrH, an assay employing Staphylococcus aureus PyrH coupled to pyruvate kinase/lactate dehydrogenase was developed and was used to perform a high throughput screen. A validated aminopyrimidine series was identified from screening. Kinetic characterization of this aminopyrimidine indicated it was a competitive inhibitor of ATP. We have shown that HTS can be used to identify potential leads for this novel target, the first ATP competitive inhibitor of PyrH reported.

Copyright © 2013 Elsevier Inc. All rights reserved.


Antibacterial targets; HTS; Inhibitor; PyrH; Screening; UMP kinase

[PubMed - indexed for MEDLINE]
PubMed Commons home

PubMed Commons

How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Write to the Help Desk