Mechanism of T. brucei Cell Cytotoxicity by Benzophenone-Derived Bisphophonium Salts

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60077344%3A_____%2F13%3A00488322" target="_blank" >RIV/60077344:_____/13:00488322 - isvavai.cz</a>
Result on the web
<a href="http://www.parazitologie.cz/protozoologie/Protodny2013/JPD_sbornik_2013.pdf" target="_blank" >http://www.parazitologie.cz/protozoologie/Protodny2013/JPD_sbornik_2013.pdf</a>
DOI - Digital Object Identifier
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Result language
angličtina
Original language name
Mechanism of T. brucei Cell Cytotoxicity by Benzophenone-Derived Bisphophonium Salts
Original language description
A recent report claims that succinate dehydrogenase, respiratory complex II (cII), is the target of a subset of benzophenone-derived bisphophonium salts that inhibit Leishmania donovani proliferation in a low micromolar concentration range. However, this was suggested from the interpretation of broad phenotypes in treated cells and indirect evidence. We show that these compounds are also very potent inhibitors of both the insect (PS) and mammalian (BS) life stage of Trypanosoma brucei. Since cII is not essential in either stage of T. brucei, we explored the mechanism of cell death in this very closely related parasite. RNAi knockdown cell lines of a critical subunit of cII was generated in both life stages and analyzed for growth phenotype, mitochondrial membrane potential, cII assembly and cII activity. Furthermore, wild type and cII RNAi induced T. brucei cells were treated with two of these compounds and then monitored for their effects on and cII activity. We propose that while these new trypanocidal drugs can directly inhibit cII, this is most likely not the major cause of cell death.n
Czech name
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Czech description
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Project
<a href="/en/project/LL1205" target="_blank" >LL1205: Exploration of the unique charakters od the Trypanosoma brucei FoF1 ATP synthase complex for future drug development against african sleeping sickness.</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2013
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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