3C52

Class II fructose-1,6-bisphosphate aldolase from helicobacter pylori in complex with phosphoglycolohydroxamic acid, a competitive inhibitor

Summary for 3C52

• Entry DOI: 10.2210/pdb3c52/pdb
• Related: 3C3S 3C56
• Descriptor: Fructose-bisphosphate aldolase, ZINC ION, CALCIUM ION, ... (6 entities in total)
• Functional Keywords: class ii, fbp, aldolase, glycolysis, inhibitor, phosphoglycolohydroxamic acid, lyase, metal-binding
• Biological source: Helicobacter pylori
• Total number of polymer chains: 2
• Total formula weight: 68200.67

Authors

Coincon, M.,Sygusch, J. (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)