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The Tetrazole VT-1161 Is a Potent Inhibitor of Trichophyton rubrum through Its Inhibition of T. rubrum CYP51.

Warrilow AGS, Parker JE, Price CL, Garvey EP, Hoekstra WJ, Schotzinger RJ, Wiederhold NP, Nes WD, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2017 Jun 27;61(7). pii: e00333-17. doi: 10.1128/AAC.00333-17. Print 2017 Jul.


The Investigational Drug VT-1129 Is a Highly Potent Inhibitor of Cryptococcus Species CYP51 but Only Weakly Inhibits the Human Enzyme.

Warrilow AG, Parker JE, Price CL, Nes WD, Garvey EP, Hoekstra WJ, Schotzinger RJ, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2016 Jul 22;60(8):4530-8. doi: 10.1128/AAC.00349-16. Print 2016 Aug.


Azole Antifungal Sensitivity of Sterol 14α-Demethylase (CYP51) and CYP5218 from Malassezia globosa.

Warrilow AG, Price CL, Parker JE, Rolley NJ, Smyrniotis CJ, Hughes DD, Thoss V, Nes WD, Kelly DE, Holman TR, Kelly SL.

Sci Rep. 2016 Jun 13;6:27690. doi: 10.1038/srep27690.


The clinical candidate VT-1161 is a highly potent inhibitor of Candida albicans CYP51 but fails to bind the human enzyme.

Warrilow AG, Hull CM, Parker JE, Garvey EP, Hoekstra WJ, Moore WR, Schotzinger RJ, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2014 Dec;58(12):7121-7. doi: 10.1128/AAC.03707-14. Epub 2014 Sep 15.


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 TY, Garvey EP, Hoekstra WJ, Yates CM, Wawrzak Z, Rachakonda G, Villalta F, Lepesheva GI.

Antimicrob Agents Chemother. 2017 Jun 27;61(7). pii: e00570-17. doi: 10.1128/AAC.00570-17. Print 2017 Jul.


Clotrimazole as a potent agent for treating the oomycete fish pathogen Saprolegnia parasitica through inhibition of sterol 14α-demethylase (CYP51).

Warrilow AG, Hull CM, Rolley NJ, Parker JE, Nes WD, Smith SN, Kelly DE, Kelly SL.

Appl Environ Microbiol. 2014 Oct;80(19):6154-66. doi: 10.1128/AEM.01195-14. Epub 2014 Aug 1.


Azole binding properties of Candida albicans sterol 14-alpha demethylase (CaCYP51).

Warrilow AG, Martel CM, Parker JE, Melo N, Lamb DC, Nes WD, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2010 Oct;54(10):4235-45. doi: 10.1128/AAC.00587-10. Epub 2010 Jul 12.


Azole Antifungal Agents To Treat the Human Pathogens Acanthamoeba castellanii and Acanthamoeba polyphaga through Inhibition of Sterol 14α-Demethylase (CYP51).

Lamb DC, Warrilow AG, Rolley NJ, Parker JE, Nes WD, Smith SN, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2015 Aug;59(8):4707-13. doi: 10.1128/AAC.00476-15. Epub 2015 May 26.


Expression, purification, and characterization of Aspergillus fumigatus sterol 14-alpha demethylase (CYP51) isoenzymes A and B.

Warrilow AG, Melo N, Martel CM, Parker JE, Nes WD, Kelly SL, Kelly DE.

Antimicrob Agents Chemother. 2010 Oct;54(10):4225-34. doi: 10.1128/AAC.00316-10. Epub 2010 Jul 26.


Azole affinity of sterol 14α-demethylase (CYP51) enzymes from Candida albicans and Homo sapiens.

Warrilow AG, Parker JE, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2013 Mar;57(3):1352-60. doi: 10.1128/AAC.02067-12. Epub 2012 Dec 28.


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 TY, Friggeri L, Wawrzak Z, Qi A, Hoekstra WJ, Schotzinger RJ, York JD, Guengerich FP, Lepesheva GI.

J Biol Chem. 2017 Apr 21;292(16):6728-6743. doi: 10.1074/jbc.M117.778308. Epub 2017 Mar 3.


The Investigational Fungal Cyp51 Inhibitor VT-1129 Demonstrates Potent In Vitro Activity against Cryptococcus neoformans and Cryptococcus gattii.

Lockhart SR, Fothergill AW, Iqbal N, Bolden CB, Grossman NT, Garvey EP, Brand SR, Hoekstra WJ, Schotzinger RJ, Ottinger E, Patterson TF, Wiederhold NP.

Antimicrob Agents Chemother. 2016 Mar 25;60(4):2528-31. doi: 10.1128/AAC.02770-15. Print 2016 Apr.


Impact of Homologous Resistance Mutations from Pathogenic Yeast on Saccharomyces cerevisiae Lanosterol 14α-Demethylase.

Sagatova AA, Keniya MV, Tyndall JDA, Monk BC.

Antimicrob Agents Chemother. 2018 Feb 23;62(3). pii: e02242-17. doi: 10.1128/AAC.02242-17. Print 2018 Mar.


Activity of Isavuconazole and Other Azoles against Candida Clinical Isolates and Yeast Model Systems with Known Azole Resistance Mechanisms.

Sanglard D, Coste AT.

Antimicrob Agents Chemother. 2015 Oct 19;60(1):229-38. doi: 10.1128/AAC.02157-15. Print 2016 Jan.


Antifungal susceptibility testing of Trichophyton rubrum by E-test.

da Silva Barros ME, de Assis Santos D, Soares Hamdan J.

Arch Dermatol Res. 2007 May;299(2):107-9. Epub 2007 Feb 28.


S279 point mutations in Candida albicans Sterol 14-α demethylase (CYP51) reduce in vitro inhibition by fluconazole.

Warrilow AG, Mullins JG, Hull CM, Parker JE, Lamb DC, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2012 Apr;56(4):2099-107. doi: 10.1128/AAC.05389-11. Epub 2012 Jan 17.


Activity of VT-1129 against Cryptococcus neoformans clinical isolates with high fluconazole MICs.

Nielsen K, Vedula P, Smith KD, Meya DB, Garvey EP, Hoekstra WJ, Schotzinger RJ, Boulware DR.

Med Mycol. 2017 Jun 1;55(4):453-456. doi: 10.1093/mmy/myw089.


In vitro susceptibility to itraconazole, clotrimazole, ketoconazole and terbinafine of 100 isolates of Trichophyton rubrum.

Fernández-Torres B, Vázquez-Veiga H, Llovo X, Pereiro M Jr, Guarro J.

Chemotherapy. 2000 Nov-Dec;46(6):390-4.


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