Novel bisphosphonate inhibitors of phosphoglycerate kinase
| Autor: | C. I. Pogson, N. A. Caplan, G M Blackburn, David J. Hayes |
|---|---|
| Rok vydání: | 1999 |
| Předmět: |
medicine.medical_treatment
Clinical Biochemistry Pharmaceutical Science Biochemistry Chemical synthesis Drug Discovery medicine Ic50 values Humans Enzyme Inhibitors Molecular Biology chemistry.chemical_classification Phosphoglycerate kinase biology Diphosphonates Organic Chemistry Bisphosphonate In vitro Kinetics Phosphoglycerate Kinase Enzyme chemistry Enzyme inhibitor biology.protein Molecular Medicine |
| Zdroj: | Bioorganicmedicinal chemistry letters. 8(5) |
| ISSN: | 0960-894X |
| 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: |
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