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1

Sterol 14α-Demethylase as a Potential Target for Antitrypanosomal Therapy: Enzyme Inhibition and Parasite Cell Growth

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

Journal:

Chemistry & Biology

Year:

2007

Language:

english

File:

PDF, 1.14 MB

english, 2007

2

Sterol 14α-demethylase cytochrome P450 (CYP51), a P450 in all biological kingdoms

Galina I. Lepesheva, Michael R. Waterman

Journal:

Biochimica et Biophysica Acta (BBA) - General Subjects

Year:

2007

Language:

english

File:

PDF, 1.31 MB

english, 2007

3

Direct antigen detection in Langmuir—Blodgett films of immunoglobulin G modified with coproporphyrin-I

Illarion V. Turko, Galina I. Lepesheva, Vadim L. Chashchin

Journal:

Analytica Chimica Acta

Year:

1992

Language:

english

File:

PDF, 409 KB

english, 1992

4

Structural basis for conservation in the CYP51 family

Galina I. Lepesheva, Michael R. Waterman

Journal:

Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics

Year:

2011

Language:

english

File:

PDF, 1.58 MB

english, 2011

5

CYP51: A Major Drug Target in the Cytochrome P450 Superfamily

Galina I. Lepesheva, Tatyana Y. Hargrove, Yuliya Kleshchenko, W. David Nes, Fernando Villalta, Michael R. Waterman

Journal:

Year:

2008

Language:

english

File:

PDF, 506 KB

english, 2008

6

Estriol Bound and Ligand-free Structures of Sterol 14α-Demethylase

Larissa M. Podust, Liudmila V. Yermalitskaya, Galina I. Lepesheva, Vladimir N. Podust, Enrique A. Dalmasso, Michael R. Waterman

Journal:

Year:

2004

Language:

english

File:

PDF, 542 KB

english, 2004

7

A Second FMN Binding Site in Yeast NADPH-Cytochrome P450 Reductase Suggests a Mechanism of Electron Transfer by Diflavin Reductases

David C. Lamb, Youngchang Kim, Liudmila V. Yermalitskaya, Valery N. Yermalitsky, Galina I. Lepesheva, Steven L. Kelly, Michael R. Waterman, Larissa M. Podust

Journal:

Year:

2006

Language:

english

File:

PDF, 902 KB

english, 2006

8

Conformational dynamics and molecular interaction reactions of recombinant cytochrome P450scc (CYP11A1) detected by fluorescence energy transfer

Galina I. Lepesheva, Natalya V. Strushkevich, Sergey A. Usanov

Journal:

Biochimica et Biophysica Acta (BBA) - Protein Structure and Molecular Enzymology

Year:

1999

Language:

english

File:

PDF, 298 KB

english, 1999

9

Conformational dynamics in the F/G segment of CYP51 from Mycobacterium tuberculosis monitored by FRET

Galina I. Lepesheva, Matej Seliskar, Charles G. Knutson, Nina V. Stourman, Damjana Rozman, Michael R. Waterman

Journal:

Archives of Biochemistry and Biophysics

Year:

2007

Language:

english

File:

PDF, 533 KB

english, 2007

10

Sterol 14α-demethylase, an abundant and essential mixed-function oxidase

Michael R. Waterman, Galina I. Lepesheva

Journal:

Biochemical and Biophysical Research Communications

Year:

2005

Language:

english

File:

PDF, 198 KB

english, 2005

11

CYP51—the omnipotent P450

Galina I Lepesheva, Michael R Waterman

Journal:

Molecular and Cellular Endocrinology

Year:

2004

Language:

english

File:

PDF, 248 KB

english, 2004

12

[Advances in Parasitology] Chagas Disease, Part A Volume 75 || Targeting Trypanosoma cruzi Sterol 14α-Demethylase (CYP51)

Lepesheva, Galina I.

Year:

2011

Language:

english

File:

PDF, 1.15 MB

english, 2011

13

Organocatalytic, Enantioselective Synthesis of VNI: A Robust Therapeutic Development Platform for Chagas, a Neglected Tropical Disease

Dobish, Mark C., Villalta, Fernando, Waterman, Michael R., Lepesheva, Galina I., Johnston, Jeffrey N.

Journal:

Organic Letters

Year:

2012

Language:

english

File:

PDF, 503 KB

english, 2012

14

Design or screening of drugs for the treatment of Chagas disease: what shows the most promise?

Lepesheva, Galina I

Journal:

Expert Opinion on Drug Discovery

Year:

2013

Language:

english

File:

PDF, 530 KB

english, 2013

15

Dialkylimidazole inhibitors of Trypanosoma cruzi sterol 14α-demethylase as anti-Chagas disease agents

Suryadevara, Praveen Kumar, Racherla, Kishore Kumar, Olepu, Srinivas, Norcross, Neil R., Tatipaka, Hari Babu, Arif, Jennifer A., Planer, Joseph D., Lepesheva, Galina I., Verlinde, Christophe L.M.J., B

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 1.70 MB

english, 2013

16

Substrate Preferences and Catalytic Parameters Determined by Structural Characteristics of Sterol 14α-Demethylase (CYP51) from Leishmania infantum

Hargrove, Tatiana Y., Wawrzak, Zdzislaw, Liu, Jialin, Nes, W. David, Waterman, Michael R., Lepesheva, Galina I.

Journal:

Journal of Biological Chemistry

Year:

2011

Language:

english

File:

PDF, 2.68 MB

english, 2011

17

Corrections to Rational Modification of a Candidate Cancer Drug for Use against Chagas Disease

Kraus, James M., Verlinde, Christophe L. M. J., Karimi, Mandana, Lepesheva, Galina I., Gelb, Michael H., Buckner, Frederick S.

Journal:

Journal of Medicinal Chemistry

Year:

2009

File:

PDF, 568 KB

2009

18

Probing the Interaction of Bovine Cytochrome P450scc (CYP11A1) with Adrenodoxin: Evaluating Site-Directed Mutations by Molecular Modeling †

Usanov, Sergey A., Graham, Sandra E., Lepesheva, Galina I., Azeva, Tamara N., Strushkevich, Natalya V., Gilep, Andrei A., Estabrook, Ronald W., Peterson, Julian A.

Journal:

Year:

2002

Language:

english

File:

PDF, 526 KB

english, 2002

19

Conservation in the CYP51 Family. Role of the B‘ Helix/BC Loop and Helices F and G in Enzymatic Function †

Lepesheva, Galina I., Virus, Cornelia, Waterman, Michael R.

Journal:

Year:

2003

Language:

english

File:

PDF, 389 KB

english, 2003

20

Corrections to Rational Modification of a Candidate Cancer Drug for Use against Chagas Disease

Kraus, James M., Verlinde, Christophe L. M. J., Karimi, Mandana, Lepesheva, Galina I., Gelb, Michael H., Buckner, Frederick S.

Journal:

Journal of Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 540 KB

english, 2009

21

Rational Modification of a Candidate Cancer Drug for Use Against Chagas Disease

Kraus, James M., Verlinde, Christophe L. M. J., Karimi, Mandana, Lepesheva, Galina I., Gelb, Michael H., Buckner, Frederick S.

Journal:

Journal of Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 458 KB

english, 2009

22

CYP51 from Trypanosoma brucei Is Obtusifoliol-Specific †

Lepesheva, Galina I., Nes, W. David, Zhou, Wenxu, Hill, George C., Waterman, Michael R.

Journal:

Year:

2004

Language:

english

File:

PDF, 314 KB

english, 2004

23

Sequence variation in CYP51A from the Y strain of Trypanosoma cruzi alters its sensitivity to inhibition

Cherkesova, Tatiana S., Hargrove, Tatiana Y., Vanrell, M. Cristina, Ges, Igor, Usanov, Sergey A., Romano, Patricia S., Lepesheva, Galina I.

Journal:

Year:

2014

Language:

english

File:

PDF, 2.58 MB

english, 2014

24

Novel 3-Nitrotriazole-Based Amides and Carbinols as Bifunctional Antichagasic Agents

Papadopoulou, Maria V., Bloomer, William D., Lepesheva, Galina I., Rosenzweig, Howard S., Kaiser, Marcel, Aguilera-Venegas, Benjamín, Wilkinson, Shane R., Chatelain, Eric, Ioset, Jean-Robert

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.38 MB

english, 2015

25

Dynamics of CYP51: implications for function and inhibitor design

Yu, Xiaofeng, Cojocaru, Vlad, Mustafa, Ghulam, Salo-Ahen, Outi M. H., Lepesheva, Galina I., Wade, Rebecca C.

Journal:

Journal of Molecular Recognition

Year:

2015

Language:

english

File:

PDF, 2.32 MB

english, 2015

26

Novel sterol metabolic network of Trypanosoma brucei procyclic and bloodstream forms

Nes, Craigen R., Singha, Ujjal K., Liu, Jialin, Ganapathy, Kulothungan, Villalta, Fernando, Waterman, Michael R., Lepesheva, Galina I., Chaudhuri, Minu, Nes, W. David

Journal:

Biochemical Journal

Year:

2012

Language:

english

File:

PDF, 1.31 MB

english, 2012

27

Structure-Functional Characterization of Cytochrome P450 Sterol 14α-Demethylase (CYP51B) from Aspergillus fumigatus and Molecular Basis for the Development of Antifungal Drugs

Hargrove, Tatiana Y., Wawrzak, Zdzislaw, Lamb, David C., Guengerich, F. Peter, Lepesheva, Galina I.

Journal:

Journal of Biological Chemistry

Year:

2015

Language:

english

File:

PDF, 7.57 MB

english, 2015

28

Ligand tunnels in T. brucei and human CYP51: Insights for parasite-specific drug design

Yu, Xiaofeng, Nandekar, Prajwal, Mustafa, Ghulam, Cojocaru, Vlad, Lepesheva, Galina I., Wade, Rebecca C.

Journal:

Biochimica et Biophysica Acta (BBA) - General Subjects

Year:

2015

Language:

english

File:

PDF, 2.47 MB

english, 2015

29

Sterol 14alpha-Demethylase (CYP51) as a Therapeutic Target for Human Trypanosomiasis and Leishmaniasis

I. Lepesheva, Galina, R. Waterman, Michael

Journal:

Current Topics in Medicinal Chemistry

Year:

2011

Language:

english

File:

PDF, 628 KB

english, 2011

30

SPIE Proceedings [SPIE Wuhan 91 - Wuhan (Wednesday 9 October 1991)] International Conference on Optical Fibre Sensors in China OFS(C) '91 - Direct fluoroimmunoassay in Langmuir-Blodgett films of immunoglobulin G

Turko, Illarion V., Lepesheva, Galina I., Chashchin, Vadim L., Culshaw, Brian, Liao, Yanbiao

Year:

1991

Language:

english

File:

PDF, 350 KB

english, 1991

31

Human sterol 14α-demethylase (CYP51) as a target for anticancer chemotherapy: Towards structure-aided drug design

Hargrove, Tatiana Y., Friggeri, Laura, Wawrzak, Zdzislaw, Sivakumaran, Suneethi, Yazlovitskaya, Eugenia M., Hiebert, Scott W., Guengerich, Frederick Peter, Waterman, Michael R., Lepesheva, Galina I.

Journal:

The Journal of Lipid Research

Year:

2016

Language:

english

File:

PDF, 1.07 MB

english, 2016

32

NIH Public Access

Lepesheva, Galina I, Waterman, Michael R

Year:

2012

Language:

english

File:

PDF, 954 KB

english, 2012

33

Antitrypanosomal and antileishmanial activity of prenyl-1,2,3-triazoles

Porta, Exequiel O. J., Jäger, Sebastián N., Nocito, Isabel, Lepesheva, Galina I., Serra, Esteban C., Tekwani, Babu L., Labadie, Guillermo R.

Journal:

Year:

2017

Language:

english

File:

PDF, 1018 KB

english, 2017

34

Structural analyses of Candida albicans sterol 14α-demethylase complexed with azole drugs address the molecular basis of azole-mediated inhibition of fungal sterol biosynthesis

Hargrove, Tatiana Y., Friggeri, Laura, Wawrzak, Zdzislaw, Qi, Aidong, Hoekstra, William J., Schotzinger, Robert J., York, John D., Guengerich, F. Peter, Lepesheva, Galina I.

Journal:

Journal of Biological Chemistry

Year:

2017

Language:

english

File:

PDF, 1.56 MB

english, 2017

35

Crystal structure of the new investigational drug candidate VT-1598 in complex with Aspergillus fumigatus sterol 14α-demethylase provides insights into its broad-spectrum antifungal activity.

Hargrove, Tatiana Y., Garvey, Edward P., Hoekstra, William J., Yates, Christopher M., Wawrzak, Zdzislaw, Rachakonda, Girish, Villalta, Fernando, Lepesheva, Galina. I.

Journal:

Antimicrobial Agents and Chemotherapy

Year:

2017

Language:

english

File:

PDF, 1.12 MB

english, 2017

36

A convergent, scalable and stereoselective synthesis of azole CYP51 inhibitors

Lepesheva, Galina, Christov, Plamen, Sulikowski, Gary A., Kim, Kwangho

Journal:

Tetrahedron Letters

Year:

2017

Language:

english

File:

PDF, 381 KB

english, 2017

37

CYP51 as drug targets for fungi and protozoan parasites: past, present and future

Lepesheva, Galina I., Friggeri, Laura, Waterman, Michael R.

Journal:

Year:

2018

Language:

english

File:

PDF, 1.32 MB

english, 2018

38

Binding of a physiological substrate causes large-scale conformational reorganization in cytochrome P450 51

Hargrove, Tatiana Y., Wawrzak, Zdzislaw, Fisher, Paxtyn M, Child, Stella A, Nes, W. David, Guengerich, F. Peter, Waterman, Michael R., Lepesheva, Galina I.

Journal:

Journal of Biological Chemistry

Year:

2018

Language:

english

File:

PDF, 1.21 MB

english, 2018

39

Validation of human sterol 14α-demethylase (CYP51) druggability: structure-guided design, synthesis and evaluation of stoichiometric, functionally irreversible inhibitors

Friggeri, Laura, Hargrove, Tatiana Y, Wawrzak, Zdzislaw, Guengerich, F. Peter, Lepesheva, Galina I

Journal:

Journal of Medicinal Chemistry

Year:

2019

Language:

english

File:

PDF, 1.08 MB

english, 2019

40

A new chemotype with promise against Trypanosoma cruzi

Wang, Xiaofang, Cal, Monica, Kaiser, Marcel, Buckner, Frederick S., Lepesheva, Galina I., Sanford, Austin G., Wallick, Alexander I., Davis, Paul H., Vennerstrom, Jonathan L.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2019

Language:

english

File:

PDF, 812 KB

english, 2019

41

A requirement for an active proton delivery network supports a Compound I mediated C-C bond cleavage in CYP51 catalysis

Hargrove, Tatiana Y., Wawrzak, Zdzislaw, Guengerich, F. Peter, Lepesheva, Galina I.

Journal:

Journal of Biological Chemistry

Year:

2020

File:

PDF, 1.58 MB

2020

42

The Clinically Approved Antifungal Drug Posaconazole Inhibits Human Cytomegalovirus Replication

Mercorelli, Beatrice, Luganini, Anna, Celegato, Marta, PalÃ¹, Giorgio, Gribaudo, Giorgio, Lepesheva, Galina I., Loregian, Arianna

Journal:

Antimicrobial Agents and Chemotherapy

Year:

2020

File:

PDF, 1.02 MB

2020

43

Concerning P450 evolution: Structural Analyses Support Bacterial Origin of Sterol 14Î±-Demethylases

Lamb, David C, Hargrove, Tatiana Y, Zhao, Bin, Wawrzak, Zdzislaw, Goldstone, Jared V, Nes, W David, Kelly, Steven L, Waterman, Michael R, Stegeman, John J, Lepesheva, Galina I, Echave, Julian

Journal:

Molecular Biology and Evolution

Year:

2020

File:

PDF, 2.24 MB

2020

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