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An integrated approach for identification and target validation of antifungal compounds active against Erg11p.

Hoepfner D, Karkare S, Helliwell SB, Pfeifer M, Trunzer M, De Bonnechose S, Zimmerlin A, Tao J, Richie D, Hofmann A, Reinker S, Frederiksen M, Movva NR, Porter JA, Ryder NS, Parker CN.

Antimicrob Agents Chemother. 2012 Aug;56(8):4233-40. doi: 10.1128/AAC.06332-11. Epub 2012 May 21.


Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.

Parker JE, Merkamm M, Manning NJ, Pompon D, Kelly SL, Kelly DE.

Antimicrob Agents Chemother. 2008 Oct;52(10):3597-603. doi: 10.1128/AAC.00517-08. Epub 2008 Aug 11.


Surface-active fungicidal D-peptide inhibitors of the plasma membrane proton pump that block azole resistance.

Monk BC, Niimi K, Lin S, Knight A, Kardos TB, Cannon RD, Parshot R, King A, Lun D, Harding DR.

Antimicrob Agents Chemother. 2005 Jan;49(1):57-70.


Identification and evaluation of novel acetolactate synthase inhibitors as antifungal agents.

Richie DL, Thompson KV, Studer C, Prindle VC, Aust T, Riedl R, Estoppey D, Tao J, Sexton JA, Zabawa T, Drumm J, Cotesta S, Eichenberger J, Schuierer S, Hartmann N, Movva NR, Tallarico JA, Ryder NS, Hoepfner D.

Antimicrob Agents Chemother. 2013 May;57(5):2272-80. doi: 10.1128/AAC.01809-12. Epub 2013 Mar 11.


Use of a yeast-based membrane protein expression technology to overexpress drug resistance efflux pumps.

Lamping E, Cannon RD.

Methods Mol Biol. 2010;666:219-50. doi: 10.1007/978-1-60761-820-1_15.


Improved model of lanosterol 14alpha-demethylase by ligand-supported homology modeling: validation by virtual screening and azole optimization.

Sheng C, Wang W, Che X, Dong G, Wang S, Ji H, Miao Z, Yao J, Zhang W.

ChemMedChem. 2010 Mar 1;5(3):390-7. doi: 10.1002/cmdc.200900468.


Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.

Lamping E, Ranchod A, Nakamura K, Tyndall JD, Niimi K, Holmes AR, Niimi M, Cannon RD.

Antimicrob Agents Chemother. 2009 Feb;53(2):354-69. doi: 10.1128/AAC.01095-08. Epub 2008 Nov 17.


Relationship between antifungal resistance of fluconazole resistant Candida albicans and mutations in ERG11 gene.

Feng LJ, Wan Z, Wang XH, Li RY, Liu W.

Chin Med J (Engl). 2010 Mar 5;123(5):544-8.


[Azole resistance in Candida spp].

Kakeya H, Miyazaki T, Miyazaki Y, Kohno S.

Nihon Ishinkin Gakkai Zasshi. 2003;44(2):87-92. Review. Japanese.


Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans.

Tani N, Rahnasto-Rilla M, Wittekindt C, Salminen KA, Ritvanen A, Ollakka R, Koskiranta J, Raunio H, Juvonen RO.

Eur J Med Chem. 2012 Jan;47(1):270-7. doi: 10.1016/j.ejmech.2011.10.053. Epub 2011 Nov 6.


New azoles with potent antifungal activity: design, synthesis and molecular docking.

Che X, Sheng C, Wang W, Cao Y, Xu Y, Ji H, Dong G, Miao Z, Yao J, Zhang W.

Eur J Med Chem. 2009 Oct;44(10):4218-26. doi: 10.1016/j.ejmech.2009.05.018. Epub 2009 May 24.


Facultative sterol uptake in an ergosterol-deficient clinical isolate of Candida glabrata harboring a missense mutation in ERG11 and exhibiting cross-resistance to azoles and amphotericin B.

Hull CM, Parker JE, Bader O, Weig M, Gross U, Warrilow AG, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2012 Aug;56(8):4223-32. doi: 10.1128/AAC.06253-11. Epub 2012 May 21.


PKC signaling regulates drug resistance of the fungal pathogen Candida albicans via circuitry comprised of Mkc1, calcineurin, and Hsp90.

LaFayette SL, Collins C, Zaas AK, Schell WA, Betancourt-Quiroz M, Gunatilaka AA, Perfect JR, Cowen LE.

PLoS Pathog. 2010 Aug 26;6(8):e1001069. doi: 10.1371/journal.ppat.1001069.


Cytochrome P450 lanosterol 14α-demethylase (CYP51): insights from molecular genetic analysis of the ERG11 gene in Saccharomyces cerevisiae.

Loper JC.

J Steroid Biochem Mol Biol. 1992 Dec;43(8):1107-16. doi: 10.1016/0960-0760(92)90339-K. Review.


Mechanisms of resistance to azole antifungal agents in Candida albicans isolates from AIDS patients involve specific multidrug transporters.

Sanglard D, Kuchler K, Ischer F, Pagani JL, Monod M, Bille J.

Antimicrob Agents Chemother. 1995 Nov;39(11):2378-86.


The yeast Saccharomyces cerevisiae Pdr16p restricts changes in ergosterol biosynthesis caused by the presence of azole antifungals.

Šimová Z, Poloncová K, Tahotná D, Holič R, Hapala I, Smith AR, White TC, Griač P.

Yeast. 2013 Jun;30(6):229-41. doi: 10.1002/yea.2956. Epub 2013 May 20.

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