Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T93344
|
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| Former ID |
TTDS00302
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| Target Name |
Squalene monooxygenase
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| Gene Name |
SQLE
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| Synonyms |
ERG1; Oxidosqaulene cyclase; SE; Squalene epoxidase; SQLE
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| Target Type |
Successful
|
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| Disease | Coronary artery disease [ICD9: 410-414, 429.2; ICD10: I20-I25] | ||||
| Dermatomycosis [ICD10: B36.0] | |||||
| Hypercholesterolemia [ICD10: E78] | |||||
| Jock itch; Athlete's foot [ICD9: 110.3, 110.4; ICD10: B35.3, B35.6] | |||||
| Function |
Catalyzes the first oxygenation step in sterol biosynthesis and is suggested to be one of the rate-limiting enzymes in this pathway.
|
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| BioChemical Class |
Oxidoreductases acting on paired donors
|
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| Target Validation |
T93344
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| UniProt ID | |||||
| EC Number |
EC 1.14.99.7
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| Sequence |
MWTFLGIATFTYFYKKFGDFITLANREVLLCVLVFLSLGLVLSYRCRHRNGGLLGRQQSG
SQFALFSDILSGLPFIGFFWAKSPPESENKEQLEARRRRKGTNISETSLIGTAACTSTSS QNDPEVIIVGAGVLGSALAAVLSRDGRKVTVIERDLKEPDRIVGEFLQPGGYHVLKDLGL GDTVEGLDAQVVNGYMIHDQESKSEVQIPYPLSENNQVQSGRAFHHGRFIMSLRKAAMAE PNAKFIEGVVLQLLEEDDVVMGVQYKDKETGDIKELHAPLTVVADGLFSKFRKSLVSNKV SVSSHFVGFLMKNAPQFKANHAELILANPSPVLIYQISSSETRVLVDIRGEMPRNLREYM VEKIYPQIPDHLKEPFLEATDNSHLRSMPASFLPPSSVKKRGVLLLGDAYNMRHPLTGGG MTVAFKDIKLWRKLLKGIPDLYDDAAIFEAKKSFYWARKTSHSFVVNILAQALYELFSAT DDSLHQLRKACFLYFKLGGECVAGPVGLLSVLSPNPLVLIGHFFAVAIYAVYFCFKSEPW ITKPRALLSSGAVLYKACSVIFPLIYSEMKYMVH |
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| Drugs and Mode of Action | |||||
| Drug(s) | Naftifine | Drug Info | Approved | Dermatomycosis | [1], [2] |
| Tolnaftate | Drug Info | Approved | Jock itch; Athlete's foot | [3] | |
| FR-194738 | Drug Info | Terminated | Hypercholesterolemia | [4] | |
| NB-598 | Drug Info | Terminated | Discovery agent | [5], [6] | |
| SDZ-87-469 | Drug Info | Terminated | Coronary artery disease | [7] | |
| Inhibitor | 1(beta)-O-galloylpedunculagin | Drug Info | [8] | ||
| 1,2,3,4,6-penta-O-galloyl-beta-D-glucose | Drug Info | [8] | |||
| 1,2,6-tri-O-galloyl-beta-D-glucose | Drug Info | [8] | |||
| Allylamines | Drug Info | [9] | |||
| Chebulinic acid | Drug Info | [8] | |||
| CORILAGIN | Drug Info | [8] | |||
| ELLAGIC ACID | Drug Info | [8] | |||
| EPIGALOCATECHIN GALLATE | Drug Info | [8] | |||
| ETHYLGALLATE | Drug Info | [8] | |||
| EUGENIIN | Drug Info | [8] | |||
| FUROSIN | Drug Info | [8] | |||
| GERANIIN | Drug Info | [8] | |||
| Green tea | Drug Info | [10] | |||
| Mallotinic acid | Drug Info | [8] | |||
| Mallotusinic acid | Drug Info | [8] | |||
| N-cetylgallate | Drug Info | [8] | |||
| N-dodecylgallate | Drug Info | [8] | |||
| Naftifine | Drug Info | [11], [12] | |||
| NB-598 | Drug Info | [10] | |||
| OCTYL_GALLATE | Drug Info | [8] | |||
| PEDUNCULAGIN | Drug Info | [8] | |||
| Procyanidin B-2 3,3'-di-O-gallate | Drug Info | [8] | |||
| Sanguiin H-6 | Drug Info | [8] | |||
| Tellurium | Drug Info | [10] | |||
| THEASINENSIN A | Drug Info | [8] | |||
| Thiocarbamate | Drug Info | [12] | |||
| Tolnaftate | Drug Info | [13], [12] | |||
| Trisnorsqualene alcohol | Drug Info | [8] | |||
| Trisnorsqualene cyclopropylamine | Drug Info | [8] | |||
| Trisnorsqualene difluoromethylidene | Drug Info | [8] | |||
| Modulator | FR-194738 | Drug Info | [14] | ||
| SDZ-87-469 | Drug Info | [13] | |||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| DRM | DRM Info | ||||
| Pathways | |||||
| KEGG Pathway | Steroid biosynthesis | ||||
| Sesquiterpenoid and triterpenoid biosynthesis | |||||
| Metabolic pathways | |||||
| Biosynthesis of secondary metabolites | |||||
| Biosynthesis of antibiotics | |||||
| PathWhiz Pathway | Steroid Biosynthesis | ||||
| Reactome | Cholesterol biosynthesis | ||||
| Activation of gene expression by SREBF (SREBP) | |||||
| References | |||||
| REF 1 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019356. | ||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| REF 3 | Drug information of Tolnaftate, 2008. eduDrugs. | ||||
| REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009590) | ||||
| REF 5 | (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: 3103). | ||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001234) | ||||
| REF 7 | Chemotherapy of fungal diseases. 1990. Page(525-550). | ||||
| REF 8 | J Nat Prod. 2001 Aug;64(8):1010-4.Ellagitannins and hexahydroxydiphenoyl esters as inhibitors of vertebrate squalene epoxidase. | ||||
| REF 9 | Differential inhibition of fungal amd mammalian squalene epoxidases by the benzylamine SDZ SBA 586 in comparison with the allylamine terbinafine. Arch Biochem Biophys. 1997 Apr 15;340(2):265-9. | ||||
| REF 10 | Squalene epoxidase as hypocholesterolemic drug target revisited. Prog Lipid Res. 2003 Jan;42(1):37-50. | ||||
| REF 11 | 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 12 | Characterization of squalene epoxidase activity from the dermatophyte Trichophyton rubrum and its inhibition by terbinafine and other antimycotic agents. Antimicrob Agents Chemother. 1996 Feb;40(2):443-7. | ||||
| REF 13 | Effects of squalene epoxidase inhibitors on Candida albicans. Antimicrob Agents Chemother. 1992 Aug;36(8):1779-81. | ||||
| REF 14 | Synthesis and biological activity of a novel squalene epoxidase inhibitor, FR194738. Bioorg Med Chem Lett. 2004 Feb 9;14(3):633-7. | ||||
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