Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth.

Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth. Research Abstract Details 

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Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth. Abstract Text:

Galina I Lepesheva,Robert D Ott,Tatiana Y Hargrove,Yuliya Y Kleshchenko,Inge Schuster,W David Nes,George C Hill,Fernando Villalta,Michael R Waterman,Galina I Lepesheva,Robert D Ott,Tatiana Y Hargrove,Yuliya Y Kleshchenko,Inge Schuster,W David Nes,George C Hill,Fernando Villalta,Michael R Waterman,Galina I Lepesheva,Robert D Ott,Tatiana Y Hargrove,Yuliya Y Kleshchenko,Inge Schuster,W David Nes,George C Hill,Fernando Villalta,Michael R Waterman,

Sterol 14alpha-demethylases (CYP51) serve as primary targets for antifungal drugs, and specific inhibition of CYP51s in protozoan parasites Trypanosoma brucei (TB) and Trypanosoma cruzi (TC) might provide an effective treatment strategy for human trypanosomiases. Primary inhibitor selection is based initially on the cytochrome P450 spectral response to ligand binding. Ligands that demonstrate strongest binding parameters were examined as inhibitors of reconstituted TB and TC CYP51 activity in vitro. Direct correlation between potency of the compounds as CYP51 inhibitors and their antiparasitic effect in TB and TC cells implies essential requirements for endogenous sterol production in both trypanosomes and suggests a lead structure with a defined region most promising for further modifications. The approach developed here can be used for further large-scale search for new CYP51 inhibitors.

Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth. Publishing Authors By Initials

GI Lepesheva,RD Ott,TY Hargrove,YY Kleshchenko,I Schuster,WD Nes,GC Hill,F Villalta,MR Waterman,GI Lepesheva,RD Ott,TY Hargrove,YY Kleshchenko,I Schuster,WD Nes,GC Hill,F Villalta,MR Waterman,GI Lepesheva,RD Ott,TY Hargrove,YY Kleshchenko,I Schuster,WD Nes,GC Hill,F Villalta,MR Waterman,

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Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Chemistry & biology

VOLUME: 14

Page Numbers: 1283-93

Journal Abbreviation: Chem. Biol.

ISSN: 1074-5521

DAY: 20

MONTH: Nov

YEAR: 2007

Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth. Information

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LANGUAGE: eng

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Grant and Affiliation Information for Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth.

AFFILIATION: Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232-0146, USA.

Country: England

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MEDLINETA: Chem Biol

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