Novel bisphosphonate inhibitors of phosphoglycerate kinase.
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.
Caplan
N A
NA
Krebs Institute, Chemistry Department, Sheffield University, UK.
Pogson
C I
CI
Hayes
D J
DJ
Blackburn
G M
GM
D004164:Diphosphonates / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D010735:Phosphoglycerate Kinase / Q000037:antagonists & inhibitors*
D004164:Diphosphonates; D004791:Enzyme Inhibitors; D010735:Phosphoglycerate Kinase