Protein Farnesyltransferase from Trypanosoma brucei
نویسندگان
چکیده
منابع مشابه
Isothiazole dioxides: synthesis and inhibition of Trypanosoma brucei protein farnesyltransferase.
A series of isothiazole dioxides was synthesized and evaluated as inhibitors of protein farnesyltransferase from the parasite that causes African sleeping sickness (Trypanosoma brucei). The most potent compound in the series inhibited the parasite enzyme with an IC(50) of 2 microM and blocked the growth of the bloodstream parasite in vitro with an ED(50) of 10 microM. The same compound inhibite...
متن کاملCloning, heterologous expression, and distinct substrate specificity of protein farnesyltransferase from Trypanosoma brucei.
Protein prenylation occurs in the protozoan that causes African sleeping sickness (Trypanosoma brucei), and the protein farnesyltransferase appears to be a good target for developing drugs. We have cloned the alpha- and beta-subunits of T. brucei protein farnesyltransferase (TB-PFT) using nucleic acid probes designed from partial amino acid sequences obtained from the enzyme purified from insec...
متن کاملProtein isoprenylation in Trypanosoma brucei brucei.
Trypanosoma brucei is a digenetic protozoan parasite presenting a public health hazard in certain areas of Africa; it is transmitted between mammals (bloodstream form (BSF)) by tsetse flies (procyclic form (PCF)). We have an ongoing interest in small GTP proteins in T. brucei, and these are commonly isoprenylated. Many isoprenylated proteins belong to the rab family and include ras; the isopren...
متن کاملDesign and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents.
On the basis of the structure of the CVIM tetrapeptide substrate of mammalian protein farnesyltransferase, a series of imidazole-containing peptidomimetics was designed and synthesized, and their inhibition activity against Trypanosoma brucei protein farnesyltransferase (TbPFT) was evaluated. Peptidomimetics where the 5-position of the imidazole ring was linked to the hydrophobic scaffold showe...
متن کاملProtein farnesyltransferase from Trypanosoma brucei. A heterodimer of 61- and 65-kda subunits as a new target for antiparasite therapeutics.
We have previously shown that protein prenylation occurs in the Trypanosomatids Trypanosoma brucei (T. brucei), Trypanosoma cruzi, and Leishmania mexicana and that protein farnesyltransferase (PFT) activity can be detected in cytosolic extracts of insect (procyclic) form T. brucei. A PFT that transfers the farnesyl group from farnesyl pyrophosphate to a cysteine that is 4 residues upstream of t...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 1998
ISSN: 0021-9258
DOI: 10.1074/jbc.273.41.26497