Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

TTD Target ID: TTDS00359

Target Information
NameFungal Cytochrome P450 51    
Type of targetSuccessful target    
SynonymsCYPL1    
CYPLI    
Cyt P450 14DM    
Cytochrome P-450 lanosterol 14-alpha-demethylase    
Cytochrome P450-dependent lanosterol 14-demethylase    
Erg11p    
LDM    
Lanosterol 14 alpha-demethylase    
Lanosterol 14-alpha demethylase    
P450-14DM    
P450L1    
P450LI    
Sterol 14-alpha demethylase    
Sterol 14alpha-demethylase    
DiseaseOropharyngeal candidiasis    [1][2]
Drug(s)BifonazoleApprovedFungal infections[3][4][5]
ButoconazoleApprovedFungal infections[6]
EconazoleApprovedFungal infections[7]
FluconazoleApprovedFungal infections[8]
ItraconazoleApprovedFungal infections[9][10]
KetoconazoleApprovedFungal infections[11]
MiconazoleApprovedFungal infections[12]
OxiconazoleApprovedFungal infections[13][14]
PosaconazoleApprovedFungal infections[15]
SertaconazoleApprovedFungal infections[16]
TerconazoleApprovedFungal infections[17]
TioconazoleApprovedFungal infections[18]
VoriconazoleApprovedInvasive aspergillosis[7]
BioChemical ClassOxidoreductases acting on paired donors    
EC NumberEC 1.14.13.70
PathwayBiosynthesis of steroids
Metabolic pathways
UniProt IDB3V1X5
P10613
Q16850
Q96W81
FunctionCatalyzes c14-demethylation of lanosterol; it transforms lanosterol into 4,4'-dimethyl cholesta-8,14,24-triene-3-beta-ol.    
SequenceMLLLGLLQAGGSVLGQAMEKVTGGNLLSMLLIACAFTLSLVYLIRLAAGHLVQLPAGVKS PPYIFSPIPFLGHAIAFGKSPIEFLENAYEKYGPVFSFTMVGKTFTYLLGSDAAALLFNS KNEDLNAEDVYSRLTTPVFGKGVAYDVPNPVFLEQKKMLKSGLNIAHFKQHVSIIEKETK EYFESWGESGEKNVFEALSELIILTASHCLHGKEIRSQLNEKVAQLYADLDGGFSHAAWL LPGWLPLPSFRRRDRAHREIKDIFYKAIQKRRQSQEKIDDILQTLLDATYKDGRPLTDDE VAGMLIGLLLAGQHTSSTTSAWMGFFLARDKTLQKKCYLEQKTVCGENLPPLTYDQLKDL NLLDRCIKETLRLRPPIMIMMRMARTPQTVAGYTIPPGHQVCVSPTVNQRLKDSWVERLD FNPDRYLQDNPASGEKFAYVPFGAGRHRCIGENFAYVQIKTIWSTMLRLYEFDLIDGYFP TVNYTTMIHTPENPVIRYKRRSK
Target ValidationClick to Find Target Validation Information.    
InhibitorANALOGUE A[19]
Bifonazole[3][4][5]
Butoconazole[6]
CP-320626[19]
Econazole[7]
Fluconazole[8]
Itraconazole[9][10]
Ketoconazole[11]
Miconazole[12]
Oxiconazole[13][14]
Posaconazole[15]
Sertaconazole[16]
Terconazole[17]
Tioconazole[18]
Voriconazole[7]
BinderFLC[20]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The genetic basis of fluconazole resistance development in Candida albicans. Biochim Biophys Acta. 2002 Jul 18;1587(2-3):240-8. To Reference
Ref 2Multiple molecular mechanisms contribute to a stepwise development of fluconazole resistance in clinical Candida albicans strains. Antimicrob Agents Chemother. 1998 Dec;42(12):3065-72. To Reference
Ref 3Investigation of the role of cytochrome P450 2B4 active site residues in substrate metabolism based on crystal structures of the ligand-bound enzyme. Arch Biochem Biophys. 2006 Nov 1;455(1):61-7. Epub 2006 Sep 25. To Reference
Ref 4Bifonazole, a biochemist's view. Dermatologica. 1984;169 Suppl 1:3-9. To Reference
Ref 5Bifonazole and clotrimazole. Their mode of action and the possible reason for the fungicidal behaviour of bifonazole. Arzneimittelforschung. 1984;34(2):139-46. To Reference
Ref 6Effects of terconazole and other azole antifungal agents on the sterol and carbohydrate composition of Candida albicans. Diagn Microbiol Infect Dis. 1990 Jan-Feb;13(1):31-5. To Reference
Ref 7Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus. Antimicrob Agents Chemother. 2008 Oct;52(10):3597-603. Epub 2008 Aug 11. To Reference
Ref 8Conduit artery constriction mediated by low flow a novel noninvasive method for the assessment of vascular function. J Am Coll Cardiol. 2008 May 20;51(20):1953-8. To Reference
Ref 9Voriconazole increases while itraconazole decreases plasma meloxicam concentrations. Antimicrob Agents Chemother. 2009 Feb;53(2):587-92. Epub 2008 Nov 17. To Reference
Ref 10Isolation of genes mediating resistance to inhibitors of nucleoside and ergosterol metabolism in Leishmania by overexpression/selection. J Biol Chem. 1999 Dec 31;274(53):37723-30. To Reference
Ref 11Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302. doi: 10.2165/00003088-200948050-00001. To Reference
Ref 12Novelties in the multifaceted miconazole effects on skin disorders. Expert Opin Pharmacother. 2008 Aug;9(11):1927-34. To Reference
Ref 13Antifungal agents: mechanisms of action. Trends Microbiol. 2003 Jun;11(6):272-9. To Reference
Ref 14Antifungal agents: mode of action in yeast cells. Rev Esp Quimioter. 2006 Jun;19(2):130-9. To Reference
Ref 15A new, broad-spectrum azole antifungal: posaconazole--mechanisms of action and resistance, spectrum of activity. Mycoses. 2006;49 Suppl 1:2-6. To Reference
Ref 16Sertaconazole: a review of its use in the management of superficial mycoses in dermatology and gynaecology. Drugs. 2009;69(3):339-59. doi: 10.2165/00003495-200969030-00009. To Reference
Ref 17Mode of action of anti-Candida drugs: focus on terconazole and other ergosterol biosynthesis inhibitors. Am J Obstet Gynecol. 1991 Oct;165(4 Pt 2):1193-9. To Reference
Ref 18Biological spectra analysis: Linking biological activity profiles to molecular structure. Proc Natl Acad Sci U S A. 2005 Jan 11;102(2):261-6. Epub 2004 Dec 29. To Reference
Ref 19Drug Metab Dispos. 2007 Mar;35(3):493-500. Epub 2006 Dec 28.Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors. To Reference
Ref 20Chemosensitization of fluconazole resistance in Saccharomyces cerevisiae and pathogenic fungi by a D-octapeptide derivative. Antimicrob Agents Chemother. 2004 Apr;48(4):1256-71. To Reference



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

 
   
           
 
Computer-aided Drug Design
About BIDD | Databases | Software | Teaching | Research |  Links

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543