GNF6702 is the name for a broad-spectrum
antiprotozoal drug invented by researchers working at the Genomics Institute of the
Novartis Research Foundation in 2013,
with activity against
leishmaniasis
Leishmaniasis is a wide array of clinical manifestations caused by parasites of the trypanosome genus ''Leishmania''. It is generally spread through the bite of phlebotomine sandflies, ''Phlebotomus'' and ''Lutzomyia'', and occurs most freq ...
,
Chagas disease
Chagas disease, also known as American trypanosomiasis, is a tropical parasitic disease caused by ''Trypanosoma cruzi''. It is spread mostly by insects in the subfamily ''Triatominae'', known as "kissing bugs". The symptoms change over the cou ...
and
sleeping sickness. These three diseases are caused by related
kinetoplastid
Kinetoplastida (or Kinetoplastea, as a class) is a group of flagellated protists belonging to the phylum Euglenozoa, and characterised by the presence of an organelle with a large massed DNA called kinetoplast (hence the name). The organisms are ...
parasites, which share similar biology. GNF6702 acts as
allosteric
In biochemistry, allosteric regulation (or allosteric control) is the regulation of an enzyme by binding an effector molecule at a site other than the enzyme's active site.
The site to which the effector binds is termed the ''allosteric site ...
proteasome
Proteasomes are protein complexes which degrade unneeded or damaged proteins by proteolysis, a chemical reaction that breaks peptide bonds. Enzymes that help such reactions are called proteases.
Proteasomes are part of a major mechanism by w ...
inhibitor which was effective against infection with any of the three protozoal diseases in mice, while having little evident toxicity to mammalian cells.
See also
*
Proteasome inhibitor
References
Carboxamides
2-Pyridyl compounds
Oxazoles
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