Issue 19, 2009
From the journal:

Organic & Biomolecular Chemistry

Nucleoside triphosphate mimicry: a sugar triazolyl nucleoside as an ATP-competitive inhibitor of B. anthracispantothenate kinase†

Andrew S. Rowan,a   Nathan I. Nicely,‡b   Nicola Cochrane,a   Wjatschesslaw A. Wlassoff,a   Al Claiborneb  and  Chris J. Hamilton*c  

* Corresponding authors

a School of Chemistry and Chemical Engineering, David Keir Building, Stranmillis Road, Queen's University Belfast, Belfast

b Centre for Structural Biology, Wake Forest University School of Medicine, Winston-Salem, North Carolina, USA

c School of Chemical Sciences and Pharmacy, University of East Anglia, Norwich, Norfolk

Abstract

The synthesis of a library of nucleoside triphoshate mimetics is described where the Mg2+ chelated triphosphate sidechain is replaced by an uncharged methylene-triazole linked monosaccharide sidechain. The compounds have been evaluated as inhibitors of Bacillus anthracispantothenate kinase and a competitive inhibitor has been identified with a Ki that is 3-fold lower than the Km value of ATP.

Graphical abstract: Nucleoside triphosphate mimicry: a sugar triazolyl nucleoside as an ATP-competitive inhibitor of B. anthracispantothenate kinase

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Article information

DOI
https://doi.org/10.1039/B909729E
Article type
Paper
Submitted
18 May 2009
Accepted
29 Jun 2009
First published
27 Jul 2009

Org. Biomol. Chem., 2009,7, 4029-4036

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Nucleoside triphosphate mimicry: a sugar triazolyl nucleoside as an ATP-competitive inhibitor of B. anthracispantothenate kinase

A. S. Rowan, N. I. Nicely, N. Cochrane, W. A. Wlassoff, A. Claiborne and C. J. Hamilton, Org. Biomol. Chem., 2009, 7, 4029 DOI: 10.1039/B909729E

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