From M. tuberculosis thymidine monophosphate kinase (TMPKmt) inhibitors towards mitochondrial thymidine kinase (TK-2) inhibitors
2008pp. 87–93
Serge Van Calenbergh, Ineke Van Daele, Sara Van Poecke, Matheus Froeyen, Hélène Munier‐Lehmann, Jan Balzarini
Abstract
Here, we report on the enzyme structure-aided design of a series of substituted 3'- or 5'-thiourea derivatives of beta- and alpha-thymidine, respectively, as thymidine monophosphate kinase inhibitors of M. tuberculosis. In a recent study, several 3'-thiourea substituted thymidine derivatives were found to be exquisitely potent and specific inhibitors of mitochondrial thymidine kinase (TK-2), with high selectivity when compared with cytosolic TK-1.
Related Papers
- → Thymidine uptake, thymidine incorporation, and thymidine kinase activity in marine bacterium isolates(1990)36 cited
- → Synthesis of N3-Substituted Thymidine Analogues for Measurement of Cellular Kinase Activity(2008)6 cited
- → Salvage pathway of pyrimidine synthesis: Divergence of substrate specificity in two related species of teleostean fish(1996)10 cited
- → Thymidine kinase activity and thymidine salvage in adult Brugia pahangi and Dirofilaria immitis(1982)7 cited
- → Phosphorylation of tritiated thymidine by L929 mouse fibroblasts(1969)68 cited