alexa Kinase Inhibition

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Kinase Inhibition

Malaria caused by parasitic protists of the genus Plasmodium remains a widespread, life-threatening infectious disease in the developing countries of the world Of the five Plasmodium species, P. falciparum is the most virulent and responsible for the most severe form of malaria. There are few known drugs that have been effective in the treatment of malaria, a problem that is complicated further by the development of resistance to existing antimalarials.

Artemisinins have been one of the most effective antimalarials. As a result, artemisininbased combination therapy, which involves the combination of artemisinin and a long acting antimalarial with a varied mechanism of action, has largely replaced monotherapy. Some of the agents used in combination with artemisinin have included amodiaquine, mefloquine and lumifantrine.

In recent years, resistance to artemisinin has also been observed, necessitating the development of novel antimalarials targeting varied processes in the malarial life cycle.The P. falciparum kinases play a role in the sexual and asexual phase of the malarial life cycle and provide novel targets that could be pursued in the development of antimalarials . Interestingly, one of the mechanisms of action for artemisinin involves inhibition of Plasmodium falciparum phosphatidylinositol- 3-kinase (PfPI3K), and an increase in levels of PfPI3K with a C580Y mutation has been observed in resistant strains

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