Design of Thymidine Analogues Targeting Thymidilate Kinase ofMycobacterium tuberculosis
نویسندگان
چکیده
منابع مشابه
Design of Thymidine Analogues Targeting Thymidilate Kinase of Mycobacterium tuberculosis
We design here new nanomolar antituberculotics, inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase (TMPKmt), by means of structure-based molecular design. 3D models of TMPKmt-inhibitor complexes have been prepared from the crystal structure of TMPKmt cocrystallized with the natural substrate deoxythymidine monophosphate (dTMP) (1GSI) for a training set of 15 thymidine analo...
متن کاملDiscovery of bicyclic thymidine analogues as selective and high-affinity inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase.
Thymidine monophosphate kinase of Mycobacterium tuberculosis (TMPKmt) represents an attractive target for selectively blocking bacterial DNA synthesis. Hereby, we report on the discovery of a novel class of bicyclic nucleosides (10 and 11) and one dinucleoside (12), belonging to the most selective inhibitors of TMPKmt discovered so far.
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Worldwide, the epidemiology of tuberculosis varies widely from an uncommon disease refueled by immigration to highly endemic, with ongoing transmission as the driving force. Countries with the highest incidence rates are found in subSaharan Africa, whereas the highest absolute numbers of cases are recorded in India and China. The latter countries experience intermediate incidence rates, but hav...
متن کاملThymidine analogues for tracking DNA synthesis.
Replicating cells undergo DNA synthesis in the highly regulated, S-phase of the cell cycle. Analogues of the pyrimidine deoxynucleoside thymidine may be inserted into replicating DNA, effectively tagging dividing cells allowing their characterisation. Tritiated thymidine, targeted using autoradiography was technically demanding and superseded by 5-bromo-2-deoxyuridine (BrdU) and related halogen...
متن کاملHuman Thymidine Kinase
Cytosolic thymidine kinase (EC 2.7.1.21) has been purified 5200-fold to apparent homogeneity from normal human placenta. The purification includes sequential affinity chromatography on blue-Sepharose and a thymidine column. The molecular weight of the enzyme determined by gel filtration and sucrose density ultracentrifugation is 92,000. The subunit molecular weight is 44,000, suggesting that t...
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ژورنال
عنوان ژورنال: Tuberculosis Research and Treatment
سال: 2013
ISSN: 2090-150X,2090-1518
DOI: 10.1155/2013/670836