title: Oxidosqualene cyclase from Saccharomyces cerevisiae, Trypanosoma cruzi, Pneumocystis carinii and Arabidopsis thaliana expressed in yeast: a model for the development of novel antiparasitic agents.
abstract: A series of 25 compounds, some of which previously were described as inhibitors of human liver microsomal oxidosqualene cyclase (OSC), were tested as inhibitors of Saccharomyces cerevisiae, Trypanosoma cruzi, Pneumocystis carinii and Arabidopsis thaliana OSCs expressed in an OSC-defective strain of S. cerevisiae. The screening identified three derivatives particularly promising for the development of novel anti-Trypanosoma agents and eight derivatives for the development of novel anti-Pneumocystis agents.
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco, Università di Torino, via P. Giuria 9, 10125 Torino, Italy. gianni.balliano@unito.it
authors.forename: Gianni
authors.initials: G
authors.lastname: Balliano
authors.forename: Henrietta
authors.initials: H
authors.lastname: Dehmlow
authors.forename: Simonetta
authors.initials: S
authors.lastname: Oliaro-Bosso
authors.forename: Matilde
authors.initials: M
authors.lastname: Scaldaferri
authors.forename: Silvia
authors.initials: S
authors.lastname: Taramino
authors.forename: Franca
authors.initials: F
authors.lastname: Viola
authors.forename: Giulia
authors.initials: G
authors.lastname: Caron
authors.forename: Johannes
authors.initials: J
authors.lastname: Aebi
authors.forename: Jean
authors.initials: J
authors.lastname: Ackermann
mesh_terms: D000818:Animals; D000977:Antiparasitic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D017360:Arabidopsis / Q000201:enzymology*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002855:Chromatography, Thin Layer; D015195:Drug Design; D006801:Humans; D019751:Intramolecular Transferases / Q000737:chemistry* / Q000378:metabolism; D008862:Microsomes, Liver / Q000378:metabolism; D008956:Models, Chemical; D045363:Pneumocystis carinii / Q000201:enzymology*; D012441:Saccharomyces cerevisiae / Q000201:enzymology*; D013261:Sterols / Q000737:chemistry; D014349:Trypanosoma cruzi / Q000201:enzymology*
chemical_list: D000977:Antiparasitic Agents; D013261:Sterols; D019751:Intramolecular Transferases; C021924:lanosterol synthase