PMID:12210989

Citation	Cox, RJ, Gibson, JS and Mayo Martín, MB (2002) Aspartyl phosphonates and phosphoramidates: the first synthetic inhibitors of bacterial aspartate-semialdehyde dehydrogenase. Chembiochem 3:874-86
Abstract	The synthesis of methylene phosphonate, difluoromethylene phosphonate and phosphoramidate analogues of aspartyl phosphate, together with reduced analogues, is described. These compounds were shown to be effective inhibitors of aspartate-semialdehyde dehydrogenase (ASA-DH) from Escherichia coli. However, despite the structural similarity of the compounds, different patterns of inhibition were observed, indicative of two phases of recognition and binding. Correlation between measured inhibition constants with pK(a) values supports the theory that binding at the phosphate binding site is optimised for singly ionised phosphate analogues.
Links	PubMed Online version:<874::AID-CBIC874>3.0.CO;2-V 10.1002/1439-7633(20020902)3:9<874::AID-CBIC874>3.0.CO;2-V
Keywords	Amides/chemical synthesis; Amides/pharmacology; Aspartate-Semialdehyde Dehydrogenase/antagonists & inhibitors; Aspartic Acid/analogs & derivatives; Aspartic Acid/chemical synthesis; Aspartic Acid/chemistry; Aspartic Acid/pharmacology; Bacterial Proteins/antagonists & inhibitors; Binding Sites; Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/pharmacology; Escherichia coli/enzymology; Kinetics; Organophosphonates/chemical synthesis; Organophosphonates/pharmacology; Phosphoric Acids/chemical synthesis; Phosphoric Acids/pharmacology; Protein Binding; Structure-Activity Relationship
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