A new international collaboration reports that the compound called TCMDC-135051 is capable of preventing the synthesis of a protein that is required for growth in Plasmodium falciparum, one of the species of the Plasmodium parasite that causes malaria. The study, reported in the journal Science, could lead to the development of a new antimalarial drug.
The compound inhibits the activity of a parasitic enzyme called protein kinase which regulates RNA splicing, and is fundamental to the activity of almost every process within the cell. At the same time it does not affect the human form of the enzyme, which would preclude its use as a drug.
Malaria takes a heavy toll on human life, with almost 500,000 deaths and over 200 million new cases a year. Many drugs have been devised to deal with the parasitic infection, but resistance develops quickly in most cases. However, in the case of TCMDC-135051, it affects P. falciparum’s cyclin-dependent-like protein kinase PfCLK3 which is a vital enzyme in its lifecycle. It does this without affecting the human protein kinase. The plasmodial parasite goes through both asexual and sexual phases in its lifecycle. With the asexual mode of reproduction it is able to proliferate and spread to other cells within the body. In the sexual phase it forms gametocytes which can get back into other mosquitoes to complete its development and infect other human beings.
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