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 Enzymatic Studies of a Malarial Drug Target. Towards Novel Inhibitors of TS-DHFR
Наименование:

Enzymatic Studies of a Malarial Drug Target. Towards Novel Inhibitors of TS-DHFR

автор Tina D. издательство Книга по Требованию Другие общетехнические дисциплины
Cтраниц 112        мягкая обложка       
Аннотация:Also, molecular docking and virtual screening of this enzyme identified a lead compound which inhibits both wildtype and drug-resistant parasites. Our kinetic data show this bifunctional enzyme is regulated by elegant interdomain communication, as well as catalytic contributions from distant structural regions, far from the active sites. Co-crystal structures of enzyme with compound suggest a molecular basis for overcoming drug resistance. Understanding the role of these unique regions may lead to more specific, less toxic therapies. The enzyme thymidylate synthase- dihydrofolate reductase (TS-DHFR) is a major antimalarial drug target, and mutations in this enzyme have caused widespread resistance. This work demonstrates how in-depth kinetic analyses can be used to identify novel intramolecular targets for rational drug design, and should be useful specially to students of enzymology, protein biochemistry and pharmacology. Plasmodium falciparum is the parasite responsible for more than 90% of deaths caused by the global epidemic of malaria. Our work comprises the first systematic, mechanistic characterization of TS-DHFR and its non-active site regions.
Автор: Tina D.
Издательство: Книга по Требованию
Год:2009
Цена:
2007 руб
Нет в наличии
Поиск: Enzymatic Studies of a Malarial Drug Target. Towards Novel Inhibitors of TS-DHFR


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