title: Synthesis and evaluation of a new inhibitor of phosphoglucose isomerases: the enediolate analogue 5-phospho-D-arabinohydroxamate.
abstract: Designed as a high energy intermediate analogue inhibitor of the potent chemotherapeutic target phosphoglucose isomerases, 5-phospho-D-arabinohydroxamate was efficiently synthesized in a two steps procedure. To date, it proved to be the strongest competitive inhibitor with respect to substrate D-fructose-6-phosphate (Ki down to 98 nM and Km/Ki values up to 513). A comparative inhibition study of this compound and other known strong inhibitors on phosphoglucose isomerases from three different sources is also reported.
authors.affiliation: Laboratoire de Chimie Bioorganique et Bioinorganique, CNRS-URA 1384, ICMO, Université Paris-XI, Orsay, France.
authors.forename: R
authors.initials: R
authors.lastname: Hardré
authors.forename: C
authors.initials: C
authors.lastname: Bonnette
authors.forename: L
authors.initials: L
authors.lastname: Salmon
authors.forename: A
authors.initials: A
authors.lastname: Gaudemer
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D005956:Glucose-6-Phosphate Isomerase / Q000037:antagonists & inhibitors*; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D011817:Rabbits
chemical_list: D004791:Enzyme Inhibitors; D006877:Hydroxamic Acids; D005956:Glucose-6-Phosphate Isomerase