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

Por Hargrove, Tatiana Y., Wawrzak, Zdzislaw, Lamb, David C., Guengerich, F. Peter, Lepesheva, Galina I.
Publicado no J Biol Chem (2015)

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

Por Hargrove, Tatiana Y., Wawrzak, Zdzislaw, Liu, Jialin, Nes, W. David, Waterman, Michael R., Lepesheva, Galina I.
Publicado em 2011

Structural complex of sterol 14α-demethylase (CYP51) with 14α-methylenecyclopropyl-Δ7-24, 25-dihydrolanosterol

Por Hargrove, Tatiana Y., Wawrzak, Zdzislaw, Liu, Jialin, Waterman, Michael R., Nes, W. David, Lepesheva, Galina I.
Publicado em 2012

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

Por Cherkesova, Tatiana S., Hargrove, Tatiana Y., Vanrell, M. Cristina, Ges, Igor, Usanov, Sergey A., Romano, Patricia S., Lepesheva, Galina I.
Publicado no FEBS Lett (2014)

Structural Insights into Inhibition of Sterol 14α-Demethylase in the Human Pathogen Trypanosoma cruzi

Por Lepesheva, Galina I., Hargrove, Tatiana Y., Anderson, Spencer, Kleshchenko, Yuliya, Furtak, Vyacheslav, Wawrzak, Zdzislaw, Villalta, Fernando, Waterman, Michael R.
Publicado em 2010

Human sterol 14α-demethylase as a target for anticancer chemotherapy: towards structure-aided drug design(1)

Por Hargrove, Tatiana Y., Friggeri, Laura, Wawrzak, Zdzislaw, Sivakumaran, Suneethi, Yazlovitskaya, Eugenia M., Hiebert, Scott W., Guengerich, F. Peter, Waterman, Michael R., Lepesheva, Galina I.
Publicado no J Lipid Res (2016)

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

Por Hargrove, Tatiana Y., Friggeri, Laura, Wawrzak, Zdzislaw, Qi, Aidong, Hoekstra, William J., Schotzinger, Robert J., York, John D., Guengerich, F. Peter, Lepesheva, Galina I.
Publicado no J Biol Chem (2017)

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

Por Lepesheva, Galina I., Ott, Robert D., Hargrove, Tatiana Y., Kleshchenko, Yuliya Y., Schuster, Inge, Nes, W. David, Hill, George C., Villalta, Fernando, Waterman, Michael R.
Publicado em 2007

VNI Cures Acute and Chronic Experimental Chagas Disease

Por Villalta, Fernando, Dobish, Mark C., Nde, Pius N., Kleshchenko, Yulia Y., Hargrove, Tatiana Y., Johnson, Candice A., Waterman, Michael R., Johnston, Jeffrey N., Lepesheva, Galina I.
Publicado em 2013

Complexes of Trypanosoma cruzi Sterol 14α-Demethylase (CYP51) with Two Pyridine-based Drug Candidates for Chagas Disease: STRUCTURAL BASIS FOR PATHOGEN SELECTIVITY

Por Hargrove, Tatiana Y., Wawrzak, Zdzislaw, Alexander, Paul W., Chaplin, Jason H., Keenan, Martine, Charman, Susan A., Perez, Catherine J., Waterman, Michael R., Chatelain, Eric, Lepesheva, Galina I.
Publicado em 2013

Structural Basis for Rational Design of Inhibitors Targeting Trypanosoma cruzi Sterol 14α-Demethylase: Two Regions of the Enzyme Molecule Potentiate Its Inhibition

Por Friggeri, Laura, Hargrove, Tatiana Y., Rachakonda, Girish, Williams, Amanda D., Wawrzak, Zdzislaw, Di Santo, Roberto, De Vita, Daniela, Waterman, Michael R., Tortorella, Silvano, Villalta, Fernando, Lepesheva, Galina I.
Publicado em 2014

Crystal Structures of Trypanosoma brucei Sterol 14α-Demethylase and Implications for Selective Treatment of Human Infections

Por Lepesheva, Galina I., Park, Hee-Won, Hargrove, Tatiana Y., Vanhollebeke, Benoit, Wawrzak, Zdzislaw, Harp, Joel M., Sundaramoorthy, Munirathinam, Nes, W. David, Pays, Etienne, Chaudhuri, Minu, Villalta, Fernando, Waterman, Michael R.
Publicado em 2010

CYP51 structures and structure-based development of novel, pathogen-specific inhibitory scaffolds

Por Hargrove, Tatiana Y., Kim, Kwangho, de Nazaré Correia Soeiro, Maria, da Silva, Cristiane França, da Gama Jaen Batista, Denise, Batista, Marcos Meuser, Yazlovitskaya, Eugenia M., Waterman, Michael R., Sulikowski, Gary A., Lepesheva, Galina I.
Publicado em 2012

Indomethacin Amides as a Novel Molecular Scaffold for Targeting Trypanosoma cruzi Sterol 14α-Demethylase

Por Konkle, Mary E., Hargrove, Tatiana Y., Kleshchenko, Yuliya Y., von Kries, Jens P., Ridenour, Whitney, Uddin, Md. Jashim, Caprioli, Richard M., Marnett, Lawrence J., Nes, W. David, Villalta, Fernando, Waterman, Michael R., Lepesheva, Galina I.
Publicado em 2009

Clinical Candidate VT-1161's Antiparasitic Effect In Vitro, Activity in a Murine Model of Chagas Disease, and Structural Characterization in Complex with the Target Enzyme CYP51 fr...

Por Hoekstra, William J., Hargrove, Tatiana Y., Wawrzak, Zdzislaw, da Gama Jaen Batista, Denise, da Silva, Cristiane F., Nefertiti, Aline S. G., Rachakonda, Girish, Schotzinger, Robert J., Villalta, Fernando, Soeiro, Maria de Nazaré C., Lepesheva, Galina I.
Publicado no Antimicrob Agents Chemother (2016)

VFV as a New Effective CYP51 Structure-Derived Drug Candidate for Chagas Disease and Visceral Leishmaniasis

Por Lepesheva, Galina I., Hargrove, Tatiana Y., Rachakonda, Girish, Wawrzak, Zdzislaw, Pomel, Sébastien, Cojean, Sandrine, Nde, Pius N., Nes, W. David, Locuson, Charles W., Calcutt, M. Wade, Waterman, Michael R., Daniels, J. Scott, Loiseau, Philippe M., Villalta, Fernando
Publicado no J Infect Dis (2015)

In Vitro and In Vivo Studies of the Antiparasitic Activity of Sterol 14α-Demethylase (CYP51) Inhibitor VNI against Drug-Resistant Strains of Trypanosoma cruzi

Por Soeiro, Maria de Nazaré Correia, de Souza, Elen Mello, da Silva, Cristiane França, Batista, Denise da Gama Jaen, Batista, Marcos Meuser, Pavão, Beatriz Philot, Araújo, Julianna Siciliano, Aiub, Claudia Alessandra Fortes, da Silva, Patrícia Bernardino, Lionel, Jessica, Britto, Constança, Kim, Kwangho, Sulikowski, Gary, Hargrove, Tatiana Y., Waterman, Michael R., Lepesheva, Galina I.
Publicado em 2013