title: Novel bisphosphonate inhibitors of phosphoglycerate kinase.
abstract: A series of novel, conformationally-restrained bisphosphonate analogues of 1,3-bisphosphoglyceric acid 1 have been synthesised and evaluated as inhibitors of 3-PGK. They are competitive inhibitors of the human enzyme and, especially for certain alpha-halophosphonic acid analogues, both Ki and IC50 values extend into the submicromolar range.
authors.affiliation: Krebs Institute, Chemistry Department, Sheffield University, UK.
authors.forename: N A
authors.initials: NA
authors.lastname: Caplan
authors.forename: C I
authors.initials: CI
authors.lastname: Pogson
authors.forename: D J
authors.initials: DJ
authors.lastname: Hayes
authors.forename: G M
authors.initials: GM
authors.lastname: Blackburn
mesh_terms: D004164:Diphosphonates / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D010735:Phosphoglycerate Kinase / Q000037:antagonists & inhibitors*
chemical_list: D004164:Diphosphonates; D004791:Enzyme Inhibitors; D010735:Phosphoglycerate Kinase