3C56

Class II fructose-1,6-bisphosphate aldolase from helicobacter pylori in complex with N-(3-Hydroxypropyl)-glycolohydroxamic acid bisphosphate, a competitive inhibitor

Summary for 3C56

• Entry DOI: 10.2210/pdb3c56/pdb
• Related: 3C4U 3C52
• Descriptor: Fructose-bisphosphate aldolase, ZINC ION, 3-{hydroxy[(phosphonooxy)acetyl]amino}propyl dihydrogen phosphate, ... (4 entities in total)
• Functional Keywords: class ii, fbp, aldolase, glycolysis, inhibitor, lyase, metal-binding, zinc
• Biological source: Helicobacter pylori
• Total number of polymer chains: 2
• Total formula weight: 68350.65

Authors

Coincon, M.,Sygusch, J.,Potvin-Dulude, P. (deposition date: 2008-01-30, release date: 2008-08-26, Last modification date: 2024-04-03)

Primary citation

Fonvielle, M.,Coincon, M.,Daher, R.,Desbenoit, N.,Kosieradzka, K.,Barilone, N.,Gicquel, B.,Sygusch, J.,Jackson, M.,Therisod, M.
Synthesis and Biochemical Evaluation of Selective Inhibitors of Class II Fructose Bisphosphate Aldolases: Towards New Synthetic Antibiotics.
Chemistry, 14:8521-8529, 2008

PubMed Abstract: 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.

PubMed: 18688832
DOI: 10.1002/chem.200800857

Experimental method

X-RAY DIFFRACTION (2.3 Å)