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TitleCyanotriazoles are selective topoisomerase II poisons that rapidly cure trypanosome infections.
Journal, issue, pagesScience, Vol. 380, Issue 6652, Page 1349-1356, Year 2023
Publish dateJun 30, 2023
AuthorsSrinivasa P S Rao / Matthew K Gould / Jonas Noeske / Manuel Saldivia / Rajiv S Jumani / Pearly S Ng / Olivier René / Yen-Liang Chen / Marcel Kaiser / Ryan Ritchie / Amanda Fortes Francisco / Nila Johnson / Debjani Patra / Harry Cheung / Colin Deniston / Andreas D Schenk / Wilian A Cortopassi / Remo S Schmidt / Natalie Wiedemar / Bryanna Thomas / Rima Palkar / Nahdiyah A Ghafar / Vanessa Manoharan / Catherine Luu / Jonathan E Gable / Kah Fei Wan / Elmarie Myburgh / Jeremy C Mottram / Whitney Barnes / John Walker / Charles Wartchow / Natasha Aziz / Colin Osborne / Juergen Wagner / Christopher Sarko / John M Kelly / Ujjini H Manjunatha / Pascal Mäser / Jan Jiricek / Suresh B Lakshminarayana / Michael P Barrett / Thierry T Diagana /
PubMed AbstractMillions who live in Latin America and sub-Saharan Africa are at risk of trypanosomatid infections, which cause Chagas disease and human African trypanosomiasis (HAT). Improved HAT treatments are ...Millions who live in Latin America and sub-Saharan Africa are at risk of trypanosomatid infections, which cause Chagas disease and human African trypanosomiasis (HAT). Improved HAT treatments are available, but Chagas disease therapies rely on two nitroheterocycles, which suffer from lengthy drug regimens and safety concerns that cause frequent treatment discontinuation. We performed phenotypic screening against trypanosomes and identified a class of cyanotriazoles (CTs) with potent trypanocidal activity both in vitro and in mouse models of Chagas disease and HAT. Cryo-electron microscopy approaches confirmed that CT compounds acted through selective, irreversible inhibition of trypanosomal topoisomerase II by stabilizing double-stranded DNA:enzyme cleavage complexes. These findings suggest a potential approach toward successful therapeutics for the treatment of Chagas disease.
External linksScience / PubMed:37384702
MethodsEM (single particle)
Resolution2.94 Å
Structure data

29930

8gcc

EMDB-29930, PDB-8gcc:
T. cruzi topoisomerase II alpha bound to dsDNA and the covalent inhibitor CT1
Method: EM (single particle) / Resolution: 2.94 Å

Chemicals

ChemComp-YWX:
2-{3-[(Z)-iminomethyl]-1H-1,2,4-triazol-1-yl}-1-{(3M)-3-[2-(trifluoromethyl)phenyl]-6H-pyrrolo[3,4-b]pyridin-6-yl}ethan-1-one

Source
  • Trypanosoma cruzi (eukaryote)
  • escherichia coli (E. coli)
  • trypanosoma cruzi strain cl brener (eukaryote)
KeywordsISOMERASE / Topoisomerase / DNA binding protein / Topoisomerase inhibitor

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