Target Information
Target General Infomation | |||||
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Target ID |
T73726
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Former ID |
TTDS00359
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Target Name |
Fungal Cytochrome P450 51
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Gene Name |
ERG11
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Synonyms |
CYPL1; 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; ERG11
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Target Type |
Successful
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Disease | Aspergillosis [ICD10: B44] | ||||
Candidiasis infection [ICD9: 001-139, 112; ICD10: B37] | |||||
Chronic pain [ICD9: 338.2,780; ICD10: R52.1-R52.2, G89] | |||||
Dry eye disease [ICD9: 370.33; ICD10: H16.229] | |||||
Dermatological disease [ICD10: L00-L99] | |||||
Fungal infections [ICD9: 110-118; ICD10: B35-B49] | |||||
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78] | |||||
Invasive aspergillosis [ICD9: 117.3; ICD10: B44] | |||||
Onychomycosis [ICD10: B35.1] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Tinea pedis [ICD10: B35.6] | |||||
Tinea pedis; Tinea cruris; Tinea corporis; Cutaneous candidiasis; Tinea versicolor [ICD10: B353] | |||||
Function |
Catalyzes C14-demethylation of lanosterol which is critical for ergosterol biosynthesis. It transforms lanosterol into 4,4'-dimethyl cholesta-8,14,24-triene-3-beta-ol.
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BioChemical Class |
Oxidoreductases acting on paired donors
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Target Validation |
T73726
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UniProt ID | |||||
EC Number |
EC 1.14.13.70
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Sequence |
MAIVETVIDGINYFLSLSVTQQISILLGVPFVYNLVWQYLYSLRKDRAPLVFYWIPWFGS
AASYGQQPYEFFESCRQKYGDVFSFMLLGKIMTVYLGPKGHEFVFNAKLSDVSAEDAYKH LTTPVFGKGVIYDCPNSRLMEQKKFAKFALTTDSFKRYVPKIREEILNYFVTDESFKLKE KTHGVANVMKTQPEITIFTASRSLFGDEMRRIFDRSFAQLYSDLDKGFTPINFVFPNLPL PHYWRRDAAQKKISATYMKEIKSRRERGDIDPNRDLIDSLLIHSTYKDGVKMTDQEIANL LIGILMGGQHTSASTSAWFLLHLGEKPHLQDVIYQEVVELLKEKGGDLNDLTYEDLQKLP SVNNTIKETLRMHMPLHSIFRKVTNPLRIPETNYIVPKGHYVLVSPGYAHTSERYFDNPE DFDPTRWDTAAAKANSVSFNSSDEVDYGFGKVSKGVSSPYLPFGGGRHRCIGEQFAYVQL GTILTTFVYNLRWTIDGYKVPDPDYSSMVVLPTEPAEIIWEKRETCMF |
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Structure |
4LXJ
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Drugs and Mode of Action | |||||
Drug(s) | Bifonazole | Drug Info | Approved | Fungal infections | [550663] |
Butoconazole | Drug Info | Approved | Candidiasis infection | [538547], [551871] | |
Econazole | Drug Info | Approved | Tinea pedis; Tinea cruris; Tinea corporis; Cutaneous candidiasis; Tinea versicolor | [551871] | |
Efinaconazole | Drug Info | Approved | Fungal infections | [533086] | |
Fluconazole | Drug Info | Approved | Fungal infections | [537641] | |
Itraconazole | Drug Info | Approved | Fungal infections | [538311] | |
Ketoconazole | Drug Info | Approved | Fungal infections | [538296], [539659] | |
Luliconazole | Drug Info | Approved | Tinea pedis | [532651], [542388], [551871] | |
Miconazole | Drug Info | Approved | Fungal infections | [538319], [539577] | |
Oxiconazole | Drug Info | Approved | Tinea pedis | [538534], [551871] | |
Posaconazole | Drug Info | Approved | Aspergillosis | [528715], [530959], [538580] | |
Sertaconazole | Drug Info | Approved | Fungal infections | [538564] | |
Terconazole | Drug Info | Approved | Candidiasis infection | [538573], [551871] | |
Tioconazole | Drug Info | Approved | Onychomycosis | [538305], [551871] | |
Voriconazole | Drug Info | Approved | Invasive aspergillosis | [537601] | |
CHLORIDE | Drug Info | Phase 3 | Solid tumours | [533218], [539483] | |
Econazole | Drug Info | Phase 3 | Chronic pain | [532876] | |
Luliconazole 10% | Drug Info | Phase 2/3 | Dry eye disease | [523617], [551740] | |
E-1224 | Drug Info | Phase 2 | Fungal infections | [523720] | |
EcoNail | Drug Info | Phase 2 | Fungal infections | [521897] | |
Pramiconazole | Drug Info | Phase 2 | Dermatological disease | [528869] | |
Embeconazole | Drug Info | Phase 1 | Fungal infections | [547271] | |
Genaconazole | Drug Info | Phase 1 | Fungal infections | [531676] | |
Abafungin | Drug Info | Discontinued in Phase 3 | Fungal infections | [548190] | |
AZALANSTAT | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [545151] | |
Inhibitor | Abafungin | Drug Info | [527740] | ||
ANALOGUE A | Drug Info | [528602] | |||
Bifonazole | Drug Info | [536289], [537801], [537803] | |||
Butoconazole | Drug Info | [537667] | |||
CP-320626 | Drug Info | [528602] | |||
E-1224 | Drug Info | [532173] | |||
EcoNail | Drug Info | [531032] | |||
Econazole | Drug Info | [536809] | |||
Efinaconazole | Drug Info | [533086], [551871] | |||
Embeconazole | Drug Info | [549777] | |||
Ketoconazole | Drug Info | [537556] | |||
Luliconazole | Drug Info | [532651], [551871] | |||
Oxiconazole | Drug Info | [535752], [536275] | |||
Posaconazole | Drug Info | [536273] | |||
Sertaconazole | Drug Info | [537139] | |||
Terconazole | Drug Info | [537454] | |||
Tioconazole | Drug Info | [536031] | |||
Modulator | AZALANSTAT | Drug Info | |||
CHLORIDE | Drug Info | [533218] | |||
Fluconazole | Drug Info | [556264] | |||
Genaconazole | Drug Info | [525976] | |||
Itraconazole | Drug Info | [556264] | |||
Luliconazole 10% | Drug Info | ||||
Miconazole | Drug Info | [556264] | |||
Pramiconazole | Drug Info | [1572591] | |||
Voriconazole | Drug Info | [556264] | |||
Binder | FLC | Drug Info | [535932] | ||
References | |||||
Ref 521897 | ClinicalTrials.gov (NCT00385502) A Trial of the Safety and Efficacy of EcoNail in the Treatment of Fungus Infections of the Great Toenail. U.S. National Institutes of Health. | ||||
Ref 523617 | ClinicalTrials.gov (NCT01431820) Safety and Efficacy of Luliconazole Solution, 10% in Subjects With Mild to Moderate Onychomycosis. U.S. National Institutes of Health. | ||||
Ref 523720 | ClinicalTrials.gov (NCT01489228) Proof-of-Concept Study of E1224 to Treat Adult Patients With Chagas Disease. U.S. National Institutes of Health. | ||||
Ref 528869 | The efficacy of oral treatment with pramiconazole in pityriasis versicolor: a phase II a trial. Br J Dermatol. 2007 Jun;156(6):1385-8. | ||||
Ref 530959 | Structural insights into inhibition of sterol 14alpha-demethylase in the human pathogen Trypanosoma cruzi. J Biol Chem. 2010 Aug 13;285(33):25582-90. | ||||
Ref 531676 | In vivo efficacy of SM-8668 (Sch 39304), a new oral triazole antifungal agent. Antimicrob Agents Chemother. 1990 Jun;34(6):980-4. | ||||
Ref 532876 | Econazole nitrate foam 1% for the treatment of tinea pedis: results from two double-blind, vehicle-controlled, phase 3 clinical trials. J Drugs Dermatol. 2014 Jul;13(7):803-8. | ||||
Ref 533086 | Efinaconazole: Developmental and reproductive toxicity potential of a novel antifungal azole. Reprod Toxicol. 2015 Apr;52:18-25. | ||||
Ref 537601 | Disk diffusion test and E-test with enriched Mueller-Hinton agar for determining susceptibility of Candida species to voriconazole and fluconazole. J Microbiol Immunol Infect. 2009 Apr;42(2):148-53. | ||||
Ref 537641 | Fluconazole use as an important risk factor in the emergence of fluconazole-resistant Candida glabrata fungemia. Arch Intern Med. 2009 Aug 10;169(15):1444-5; author reply 1445. | ||||
Ref 538296 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075273. | ||||
Ref 538305 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075915. | ||||
Ref 538311 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 076104. | ||||
Ref 538319 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 076773. | ||||
Ref 538534 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019828. | ||||
Ref 538547 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020421. | ||||
Ref 538564 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021385. | ||||
Ref 538573 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021735. | ||||
Ref 538580 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022003. | ||||
Ref 539483 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2339). | ||||
Ref 539577 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2449). | ||||
Ref 539659 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2568). | ||||
Ref 542388 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7366). | ||||
Ref 545151 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002302) | ||||
Ref 547271 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014655) | ||||
Ref 525976 | New targets and delivery systems for antifungal therapy. Med Mycol. 2000;38 Suppl 1:335-47. | ||||
Ref 527740 | Upregulation of sterol C14-demethylase expression in Trypanosoma cruzi treated with sterol biosynthesis inhibitors. Mol Biochem Parasitol. 2005 Nov;144(1):68-75. | ||||
Ref 528602 | Drug Metab Dispos. 2007 Mar;35(3):493-500. Epub 2006 Dec 28.Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors. | ||||
Ref 531032 | Azole binding properties of Candida albicans sterol 14-alpha demethylase (CaCYP51). Antimicrob Agents Chemother. 2010 Oct;54(10):4235-45. | ||||
Ref 532173 | Recent Developments in Sterol 14-demethylase Inhibitors for Chagas Disease. Int J Parasitol Drugs Drug Resist. 2012 Dec;2:236-242. | ||||
Ref 533086 | Efinaconazole: Developmental and reproductive toxicity potential of a novel antifungal azole. Reprod Toxicol. 2015 Apr;52:18-25. | ||||
Ref 535932 | Chemosensitization of fluconazole resistance in Saccharomyces cerevisiae and pathogenic fungi by a D-octapeptide derivative. Antimicrob Agents Chemother. 2004 Apr;48(4):1256-71. | ||||
Ref 536031 | Biological 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. | ||||
Ref 536273 | A new, broad-spectrum azole antifungal: posaconazole--mechanisms of action and resistance, spectrum of activity. Mycoses. 2006;49 Suppl 1:2-6. | ||||
Ref 536275 | Antifungal agents: mode of action in yeast cells. Rev Esp Quimioter. 2006 Jun;19(2):130-9. | ||||
Ref 536289 | Investigation 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. | ||||
Ref 536809 | Differential 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. | ||||
Ref 537139 | Sertaconazole: 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. | ||||
Ref 537454 | Mode 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. | ||||
Ref 537556 | Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302. doi: 10.2165/00003088-200948050-00001. | ||||
Ref 537667 | Effects 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. | ||||
Ref 537801 | Bifonazole and clotrimazole. Their mode of action and the possible reason for the fungicidal behaviour of bifonazole. Arzneimittelforschung. 1984;34(2):139-46. |
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