ChemInform Abstract: Novel Bisphosphonate Inhibitors of Phosphoglycerate Kinase

Autor:	N. A. Caplan, C. I. Pogson, David J. Hayes, G M Blackburn
Rok vydání:	2010
Předmět:	chemistry.chemical_classification Phosphoglycerate kinase Enzyme Chemistry Stereochemistry medicine.medical_treatment medicine Ic50 values General Medicine Bisphosphonate
Zdroj:	ChemInform. 29
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.199824215
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::c2e2475fa7e954d4edca03bdd7b8d9e2 https://doi.org/10.1002/chin.199824215 Zobrazit plný text záznamu Plný text