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© Institut Pasteur
Cristaux de cellulase, enzyme purifiée de Clostridium thermocellum permettant la digestion de la cellulose. Image colorisée.
Publication : ChemMedChem

Exploring acyclic nucleoside analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in ChemMedChem - 01 Jul 2008

Familiar O, Munier-Lehmann H, Negri A, Gago F, Douguet D, Rigouts L, Hernández AI, Camarasa MJ, Pérez-Pérez MJ

Link to Pubmed [PMID] – 18418833

ChemMedChem 2008 Jul;3(7):1083-93

In the search for novel inhibitors of the enzyme thymidine monophosphate kinase of Mycobacterium tuberculosis (TMPKmt), an attractive target for novel antituberculosis agents, we report herein the discovery of the first acyclic nucleoside analogues that potently and selectively inhibit TMPKmt. The most potent compounds in this series are (Z)-butenylthymines carrying a naphtholactam or naphthosultam moiety at position 4, which display K(i) values of 0.42 and 0.27 microM, respectively. Docking studies followed by molecular dynamics simulations performed to rationalize the interaction of this new family of inhibitors with the target enzyme revealed a key interaction between the distal substituent and Arg 95 in the target enzyme. The fact that these inhibitors are more easily synthesizable than previously identified TMPKmt inhibitors, together with their potency against the target enzyme, makes them attractive lead compounds for further optimization.

http://www.ncbi.nlm.nih.gov/pubmed/18418833