The study also noted that the compound was effective against other species of Plasmodium.
An
international team of researchers have found that a novel compound
can halt the growth of the parasite Plasmodium falciparum known to
cause malaria
-- the deadly mosquito-borne disease which kills nearly 500,000
people every year across the world.
The
study, published in the journal Science, noted that the compound
called TCMDC-135051 developed by the multinational pharmaceutical
company GlaxoSmithKline can eliminate the mosquito-borne parasite in
all the stages of its lifecycle.
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The
researchers, including those from Brazil's Sao Paulo Research
Foundation (FAPESP), noted that the drug specifically acted on a
protein in the the parasite called the cyclin-dependent-like protein
kinase -- PfCLK3 -- without affecting human proteins.
The
researchers noted that PfCLK3 controlled the activity and production
of other proteins required by the parasite to stay alive, and by
blocking these, killed P. falciparum.
According
to the study, inhibition of PfCLK3 not only affected the parasite's
asexual stage of development -- when it proliferated in human cells,
and caused symptoms -- but also in the sexual stage, when it can be
transmitted back to mosquitoes,
repeating the cycle by infecting other humans.
To
identify compounds that specifically inactivated the PfCLK3 protein,
the researchers conducted a large scale automated chemical analysis
-- through a process called high-throughput screening.
In
the process, they analysed nearly 25,000 compounds, and selected
TCMDC-135051 since it showed the most exclusiveness in binding with
the parasite's protein, and had high potency in this regard.
The
study also noted that the compound was effective against other
species of Plasmodium.
"We
also tested it in mice infected with Plasmodium berghei. The results
of this in vivo trial showed that the parasite was eliminated from
the bloodstream after five days of infection," said Paulo Godoi,
co-author of the study from University of Campinas in Brazil.
Since
both the parasite and humans have proteins similar to PfCLK3
orchestrating the activity of almost all processes in cells, the
researchers performed experiments to confirm that TCMDC-135051 was
safe, and did not act on the human forms of the protein.
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