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Galina Lepesheva

Research Profile

Chemicals & Drugs

Genes & Molecular Sequences

Amino Acid Sequences

Concepts & Ideas

Physiology

Mutagenesis, Site-Directed

Procedures

Sequence Alignment

Living Beings

Disorders

Chagas' Disease

Co-author Network

Publications

TOP 3
Grasiella Andriani; Joel Beatty; Zeke Clements; Brian J Coffey; Gilles Courtemanche; William Devine; Jessey Erath; Cristin E Juda; Galina I Lepesheva; Ana Rodriguez; Zdzislaw Wawrzak; JodiAnne T Wood; Emanuele Amata; Michael P Pollastri
Antitrypanosomal lead discovery: identification of a ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth.
Mark C Dobish; Galina I Lepesheva; Fernando Villalta; Michael R Waterman; Jeffrey N Johnston
Organocatalytic, enantioselective synthesis of VNI: a robust therapeutic development platform for Chagas, a neglected tropical disease.
Frederick S Buckner; Susan A Charman; Eric Chatelain; Naveen Kumar Chennamaneni; Maria Terezinha Bahia; Matthew A Hulverson; Joy U Laydbak; Galina I Lepesheva; Ivan Scandale; David M Shackleford; Praveen Kumar Suryadevara; Christophe L M J Verlinde; Karen L White; Michael H Gelb
Pharmacological characterization, structural studies, and in vivo activities of anti-Chagas disease lead compounds derived from tipifarnib.

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All Publications

2013: Grasiella Andriani; Joel Beatty; Zeke Clements; Brian J Coffey; Gilles Courtemanche; William Devine; Jessey Erath; Cristin E Juda; Galina I Lepesheva; Ana Rodriguez; Zdzislaw Wawrzak; JodiAnne T Wood; Emanuele Amata; Michael P Pollastri
Antitrypanosomal lead discovery: identification of a ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth.
Journal of medicinal chemistry 2013;56(6):2556-67.
2012: Mark C Dobish; Galina I Lepesheva; Fernando Villalta; Michael R Waterman; Jeffrey N Johnston
Organocatalytic, enantioselective synthesis of VNI: a robust therapeutic development platform for Chagas, a neglected tropical disease.
Organic letters 2012;14(24):6322-5.
2012: Frederick S Buckner; Susan A Charman; Eric Chatelain; Naveen Kumar Chennamaneni; Maria Terezinha Bahia; Matthew A Hulverson; Joy U Laydbak; Galina I Lepesheva; Ivan Scandale; David M Shackleford; Praveen Kumar Suryadevara; Christophe L M J Verlinde; Karen L White; Michael H Gelb
Pharmacological characterization, structural studies, and in vivo activities of anti-Chagas disease lead compounds derived from tipifarnib.
Antimicrobial agents and chemotherapy 2012;56(9):4914-21.
2012: Craigen R Nes; Ujjal K Singha; Fernando Villalta; Michael R Waterman; Minu Chaudhuri; kulothungan ganapathy; Galina I Lepesheva; Jialin Liu; W David Nes
Novel sterol metabolic network of Trypanosoma brucei procyclic and bloodstream forms.
The Biochemical journal 2012;443(1):267-77.
2011: Tatiana Y Hargrove; Jialin Liu; W David Nes; Michael R Waterman; Zdzislaw Wawrzak; Galina I Lepesheva
Substrate preferences and catalytic parameters determined by structural characteristics of sterol 14alpha-demethylase (CYP51) from Leishmania infantum.
The Journal of biological chemistry 2011;286(30):26838-48.
2011: Galina I Lepesheva; Fernando Villalta; Michael R Waterman
Targeting Trypanosoma cruzi sterol 14α-demethylase (CYP51).
Advances in parasitology 2011;75():65-87.
2011: Galina I Lepesheva; Michael R Waterman
Sterol 14alpha-demethylase (CYP51) as a therapeutic target for human trypanosomiasis and leishmaniasis.
Current topics in medicinal chemistry 2011;11(16):2060-71.
2011: Galina I Lepesheva; Michael R Waterman
Structural basis for conservation in the CYP51 family.
Biochimica et biophysica acta 2011;1814(1):88-93.
2010: Galina I Lepesheva; Tatiana Y Hargrove; Spencer Anderson; Yuliya Kleshchenko; Vyacheslav Furtak; Zdzislaw Wawrzak; Fernando Villalta; Michael R Waterman
Structural insights into inhibition of sterol 14alpha-demethylase in the human pathogen Trypanosoma cruzi.
The Journal of biological chemistry 2010;285(33):25582-90.
2010: Galina I Lepesheva; Hee-Won Park; Tatiana Y Hargrove; Benoit Vanhollebeke; Zdzislaw Wawrzak; Joel M Harp; Munirathinam Sundaramoorthy; W David Nes; Etienne Pays; Minu Chaudhuri; Fernando Villalta; Michael R Waterman
Crystal structures of Trypanosoma brucei sterol 14alpha-demethylase and implications for selective treatment of human infections.
The Journal of biological chemistry 2010;285(3):1773-80.
2009: David C Lamb; Li Lei; Andrew G S Warrilow; Galina I Lepesheva; Jonathan G L Mullins; Michael R Waterman; Steven L Kelly
The first virally encoded cytochrome p450.
Journal of virology 2009;83(16):8266-9.
2009: Mary E Konkle; Tatiana Y Hargrove; Yuliya Y Kleshchenko; Jens P von Kries; Whitney Ridenour; Md Jashim Uddin; Richard M Caprioli; Lawrence J Marnett; W David Nes; Fernando Villalta; Michael R Waterman; Galina I Lepesheva
Indomethacin amides as a novel molecular scaffold for targeting Trypanosoma cruzi sterol 14alpha-demethylase.
Journal of medicinal chemistry 2009;52(9):2846-53.
2009: James M Kraus; Christophe Verlinde; Mandana Karimi; Galina I Lepesheva; Michael H Gelb; Frederick S Buckner
Rational modification of a candidate cancer drug for use against Chagas disease.
Journal of medicinal chemistry 2009;52(6):1639-47.
2008: Galina I Lepesheva; Tatyana Y Hargrove; Yuliya Kleshchenko; W David Nes; Fernando Villalta; Michael R Waterman
CYP51: A major drug target in the cytochrome P450 superfamily.
Lipids 2008;43(12):1117-25.
2007: 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-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth.
Chemistry & biology 2007;14(11):1283-93.
2007: Galina I Lepesheva; Matej Seliskar; Charles G Knutson; Nina V Stourman; Damjana Rozman; Michael R Waterman
Conformational dynamics in the F/G segment of CYP51 from Mycobacterium tuberculosis monitored by FRET.
Archives of biochemistry and biophysics 2007;464(2):221-7.
2007: Galina I Lepesheva; Michael R Waterman
Sterol 14alpha-demethylase cytochrome P450 (CYP51), a P450 in all biological kingdoms.
Biochimica et biophysica acta 2007;1770(3):467-77.
2006: Galina I Lepesheva; T Y Hargrove; Robert D Ott; W David Nes; Michael R Waterman
Biodiversity of CYP51 in trypanosomes.
Biochemical Society transactions 2006;34(Pt 6):1161-4.
2006: Natalya V Strushkevich; Ivan N Harnastai; Galina I Lepesheva; Sergey A Usanov
Role of C-terminal sequence of cytochrome P450scc in folding and functional activity.
Biochemistry. Biokhimii͡a 2006;71(9):1027-34.
2006: Wenxu Zhou; Galina I Lepesheva; Michael R Waterman; W David Nes
Mechanistic analysis of a multiple product sterol methyltransferase implicated in ergosterol biosynthesis in Trypanosoma brucei.
The Journal of biological chemistry 2006;281(10):6290-6.
2006: Galina I Lepesheva; Natalia G Zaitseva; W David Nes; Wenxu Zhou; Miharu Arase; Jialin Liu; George C Hill; Michael R Waterman
CYP51 from Trypanosoma cruzi: a phyla-specific residue in the B' helix defines substrate preferences of sterol 14alpha-demethylase.
The Journal of biological chemistry 2006;281(6):3577-85.
2006: David C Lamb; Youngchang Kim; Liudmila V Yermalitskaya; Valery N Yermalitsky; Galina I Lepesheva; Steven L Kelly; Michael R Waterman; Larissa M Podust
A second FMN binding site in yeast NADPH-cytochrome P450 reductase suggests a mechanism of electron transfer by diflavin reductases.
Structure (London, England : 1993) 2006;14(1):51-61.
2005: Michael R Waterman; Galina I Lepesheva
Sterol 14 alpha-demethylase, an abundant and essential mixed-function oxidase.
Biochemical and biophysical research communications 2005;338(1):418-22.
2005: Natalya V Strushkevich; Tamara N Azeva; Galina I Lepesheva; Sergey A Usanov
Role of positively charged residues lys267, lys270, and arg411 of cytochrome p450scc (CYP11A1) in interaction with adrenodoxin.
Biochemistry. Biokhimii͡a 2005;70(6):664-71.
2004: Larissa M Podust; Liudmila V Yermalitskaya; Galina I Lepesheva; Vladimir N Podust; Enrique A Dalmasso; Michael R Waterman
Estriol bound and ligand-free structures of sterol 14alpha-demethylase.
Structure (London, England : 1993) 2004;12(11):1937-45.
2004: Aouatef Bellamine; Galina I Lepesheva; Michael R Waterman
Fluconazole binding and sterol demethylation in three CYP51 isoforms indicate differences in active site topology.
Journal of lipid research 2004;45(11):2000-7.
2004: Galina I Lepesheva; W David Nes; Wenxu Zhou; George C Hill; Michael R Waterman
CYP51 from Trypanosoma brucei is obtusifoliol-specific.
Biochemistry 2004;43(33):10789-99.
2004: Galina I Lepesheva; Michael R Waterman
CYP51--the omnipotent P450.
Molecular and cellular endocrinology 2004;215(1-2):165-70.
2003: Galina I Lepesheva; Cornelia Virus; Michael R Waterman
Conservation in the CYP51 family. Role of the B' helix/BC loop and helices F and G in enzymatic function.
Biochemistry 2003;42(30):9091-101.
2002: Sergey A Usanov; Sandra E Graham; Galina I Lepesheva; Tamara N Azeva; Natalya V Strushkevich; Maxim Chudaev; Ronald W Estabrook; Julian A Peterson
Probing the interaction of bovine cytochrome P450scc (CYP11A1) with adrenodoxin: evaluating site-directed mutations by molecular modeling.
Biochemistry 2002;41(26):8310-20.
2001: Galina I Lepesheva; Larissa M Podust; Aouatef Bellamine; Michael R Waterman
Folding requirements are different between sterol 14alpha-demethylase (CYP51) from Mycobacterium tuberculosis and human or fungal orthologs.
The Journal of biological chemistry 2001;276(30):28413-20.
2001: Tamara N Azeva; Maxim Chudaev; Galina I Lepesheva; Natalya V Strushkevich; Sergey A Usanov
Site-directed mutagenesis of cytochrome P450scc. II. Effect of replacement of the Arg425 and Arg426 residues on the structural and functional properties of the cytochrome P450scc.
Biochemistry. Biokhimii͡a 2001;66(5):564-75.
2000: Galina I Lepesheva; Tamara N Azeva; Natalya V Strushkevich; Maxim Chudaev; Sergey A Usanov
Site-directed mutagenesis of cytochrome P450scc (CYP11A1). Effect of lysine residue substitution on its structural and functional properties.
Biochemistry. Biokhimii͡a 2000;65(12):1409-18.
1999: Galina I Lepesheva; Natalya V Strushkevich; Sergey A Usanov
Conformational dynamics and molecular interaction reactions of recombinant cytochrome p450scc (CYP11A1) detected by fluorescence energy transfer.
Biochimica et biophysica acta 1999;1434(1):31-43.
1999: Galina I Lepesheva; Tamara N Azeva; Natalya V Strushkevich; T B Adamovich; T S Cherkesova; Sergey A Usanov
Comparative structural-functional characterization of recombinant and natural adrenodoxin. Interaction with cytochrome P450scc.
Biochemistry. Biokhimii͡a 1999;64(9):1079-88.
1998: Galina I Lepesheva; Sergey A Usanov
Comparative structural and immunochemical characterization of recombinant and natural cytochrome p450scc (CYPXIAI).
Biochemistry. Biokhimii͡a 1998;63(2):224-34.
1997: Galina I Lepesheva; Sergey A Usanov
Dynamics and functional activity of cytochrome P450scc selectively labeled with fluorescein isothiocyanate.
Biochemistry. Biokhimii͡a 1997;62(6):648-56.
1996: Galina I Lepesheva; Sergey A Usanov
[The use of selective chemical modification of cytochrome P450scc (CYPXIA1) with fluorescein isothiocyanate for evaluation of intramolecular distances and conformational changes by fluorescent resonance energy transfer].
Biokhimii͡a (Moscow, Russia) 1996;61(8):1395-407.