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© Marie Prévost, Institut Pasteur
Image of a portion of a Xenopus oocyte expressing a channel receptor.
Publication : Chemistry (Weinheim an der Bergstrasse, Germany)

Synthesis and biochemical evaluation of selective inhibitors of class II fructose bisphosphate aldolases: towards new synthetic antibiotics

Team: Channel Receptors
Member: Brigitte Gicquel
Member: Nathalie Barilone
Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Chemistry (Weinheim an der Bergstrasse, Germany) - 01 Jan 2008

Fonvielle M, Coinçon M, Daher R, Desbenoit N, Kosieradzka K, Barilone N, Gicquel B, Sygusch J, Jackson M, Therisod M

Link to Pubmed [PMID] – 18688832

Chemistry 2008;14(28):8521-9

We report the synthesis and biochemical evaluation of selective inhibitors of class II (zinc-dependent) fructose bisphosphate aldolases. The most active compound is a simplified analogue of fructose bisphosphate, bearing a well-positioned metal chelating group. It is a powerful and highly selective competitive inhibitor of isolated class II aldolases. We report crystallographic studies of this inhibitor bound in the active site of the Helicobacter pylori enzyme. The compound also shows activity against Mycobacterium tuberculosis isolates.