Journal ArticleDOI
Oxidosqualene cyclase from Saccharomyces cerevisiae, Trypanosoma cruzi, Pneumocystis carinii and Arabidopsis thaliana expressed in yeast: a model for the development of novel antiparasitic agents.
Gianni Balliano,Henrietta Dehmlow,Simonetta Oliaro-Bosso,Matilde Scaldaferri,Silvia Taramino,Franca Viola,Giulia Caron,Johannes Aebi,Jean Ackermann +8 more
TLDR
The screening identified three derivatives particularly promising for the development of novel anti-Trypanosoma agents and eight derivatives for theDevelopment of novelAnti-Pneumocystis agents.About:
This article is published in Bioorganic & Medicinal Chemistry Letters.The article was published on 2009-02-01. It has received 14 citations till now. The article focuses on the topics: Pneumocystis carinii & Antiparasitic agent.read more
Citations
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Journal ArticleDOI
Trypanosomatid Parasites Causing Neglected Diseases
TL;DR: A comprehensive insight into the treatment of Kala azar, Chagas disease and African sleeping sickness is provided and novel small molecule- based therapeutic approaches are discussed.
Journal ArticleDOI
Cytotoxic Effects of Combination of Oxidosqualene Cyclase Inhibitors with Atorvastatin in Human Cancer Cells
Davide Staedler,Catherine Chapuis-Bernasconi,Henrietta Dehmlow,Holger Fischer,Lucienne Juillerat-Jeanneret,Johannes Aebi +5 more
TL;DR: Not only statins targeting the 3-hydroxy-3-methylglutaryl coenzyme A reductase but also inhibitors of oxidosqualene cyclase decrease tumor growth, suggesting new therapeutic opportunities of combined anti-cholesterol agents for dual treatment of glioblastoma.
Journal ArticleDOI
Functional Expression of Parasite Drug Targets and Their Human Orthologs in Yeast
TL;DR: It is demonstrated that yeast strains expressing yeast expressing DHFR enzymes are insensitive to pyrimethamine treatment, whereas yeast strains producing Plasmodium and PvDHFR DHFRs are hypersensitive.
Journal ArticleDOI
A decade of targets and patented drugs for chemotherapy of Chagas disease.
TL;DR: Advances on antichagasic agents directed to specific parasite targets such as metabolic pathways or specific enzymes, including cysteine proteinase inhibitors and inhibitors capable to block ergosterol biosynthesis, are summarized.
Journal ArticleDOI
Synthesis and biological evaluation of some novel urea and thiourea derivatives of isoxazolo[4,5- d ]pyridazine and structurally related thiazolo[4,5- d ]pyridazine as antimicrobial agents
TL;DR: The results revealed that 25 compounds displayed broad spectrum of antibacterial activity, with greater inhibitory effect on the growth of the tested Gram positive strains compared to Gram negative ones, and 14 compounds were able to produce appreciable growth inhibitory activity against Candida albicans fungus when compared to Clotrimazole.
References
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Current and Emerging Azole Antifungal Agents
TL;DR: Present and future uses of the currently available azole antifungal agents in the treatment of systemic and superficial fungal infections are described and a brief overview of the current status of in vitro susceptibility testing and the growing problem of clinical resistance to the azoles is provided.
Journal ArticleDOI
Chemotherapy of trypanosomiases and leishmaniasis
TL;DR: Financial constraints continue to represent a major hurdle to drug development, however, the appearance of not-for-profit product-development partnerships offers a new paradigm for bringing new drugs to patients.
Journal ArticleDOI
American Trypanosomiasis (Chagas' Disease) -- A Tropical Disease Now in the United States
TL;DR: American trypanosomiasis (Chagas' disease) is a zoonosis caused by the protozoan parasite Trypanosoma cruzi and is a major cause of morbidity and mortality among poor people in developing countries, but health care providers in industrialized nations see it less frequently and know little about it.
Journal ArticleDOI
Insight into steroid scaffold formation from the structure of human oxidosqualene cyclase
Ralf Thoma,Tanja Schulz-Gasch,Brigitte D'Arcy,Jörg Benz,Johannes Aebi,Henrietta Dehmlow,Michael Hennig,Martine Stihle,Armin Ruf +8 more
TL;DR: The target protein with an inhibitor that showed cholesterol lowering in vivo opens the way for the structure-based design of new OSC inhibitors, and the complex with the reaction product lanosterol gives a clear picture of the way in which the enzyme achieves product specificity in this highly exothermic cyclization reaction.
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Ro 48-8.071, a new 2,3-oxidosqualene:lanosterol cyclase inhibitor lowering plasma cholesterol in hamsters, squirrel monkeys, and minipigs: comparison to simvastatin.
Olivier Morand,Johannes Aebi,Henrietta Dehmlow,Yu-Hua Ji,N Gains,Hans Lengsfeld,Jacques Himber +6 more
TL;DR: Findings clearly differentiate the OSC inhibitor Ro 48-8.071 from simvastatin, and support the view that OSC is a distinct key component in the regulation of the cholesterol synthesis pathway.