Target Information
Target General Infomation | |||||
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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 | [538523], [551871] |
Tolnaftate | Drug Info | Approved | Jock itch; Athlete's foot | [550769] | |
FR-194738 | Drug Info | Terminated | Hypercholesterolemia | [546677] | |
NB-598 | Drug Info | Terminated | Discovery agent | [540107], [544824] | |
SDZ-87-469 | Drug Info | Terminated | Coronary artery disease | [551702] | |
Inhibitor | 1(beta)-O-galloylpedunculagin | Drug Info | [526128] | ||
1,2,3,4,6-penta-O-galloyl-beta-D-glucose | Drug Info | [526128] | |||
1,2,6-tri-O-galloyl-beta-D-glucose | Drug Info | [526128] | |||
Allylamines | Drug Info | [538028] | |||
Chebulinic acid | Drug Info | [526128] | |||
CORILAGIN | Drug Info | [526128] | |||
ELLAGIC ACID | Drug Info | [526128] | |||
EPIGALOCATECHIN GALLATE | Drug Info | [526128] | |||
ETHYLGALLATE | Drug Info | [526128] | |||
EUGENIIN | Drug Info | [526128] | |||
FUROSIN | Drug Info | [526128] | |||
GERANIIN | Drug Info | [526128] | |||
Green tea | Drug Info | [535625] | |||
Mallotinic acid | Drug Info | [526128] | |||
Mallotusinic acid | Drug Info | [526128] | |||
N-cetylgallate | Drug Info | [526128] | |||
N-dodecylgallate | Drug Info | [526128] | |||
Naftifine | Drug Info | [537454], [537992] | |||
NB-598 | Drug Info | [535625] | |||
OCTYL_GALLATE | Drug Info | [526128] | |||
PEDUNCULAGIN | Drug Info | [526128] | |||
Procyanidin B-2 3,3'-di-O-gallate | Drug Info | [526128] | |||
Sanguiin H-6 | Drug Info | [526128] | |||
Tellurium | Drug Info | [535625] | |||
THEASINENSIN A | Drug Info | [526128] | |||
Thiocarbamate | Drug Info | [537992] | |||
Tolnaftate | Drug Info | [535827], [537992] | |||
Trisnorsqualene alcohol | Drug Info | [526128] | |||
Trisnorsqualene cyclopropylamine | Drug Info | [526128] | |||
Trisnorsqualene difluoromethylidene | Drug Info | [526128] | |||
Modulator | FR-194738 | Drug Info | [526940] | ||
SDZ-87-469 | Drug Info | [535827] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
Pathways | |||||
References | |||||
Ref 538523 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019356. | ||||
Ref 540107 | (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 544824 | 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 526128 | J Nat Prod. 2001 Aug;64(8):1010-4.Ellagitannins and hexahydroxydiphenoyl esters as inhibitors of vertebrate squalene epoxidase. | ||||
Ref 526940 | Synthesis and biological activity of a novel squalene epoxidase inhibitor, FR194738. Bioorg Med Chem Lett. 2004 Feb 9;14(3):633-7. | ||||
Ref 535625 | Squalene epoxidase as hypocholesterolemic drug target revisited. Prog Lipid Res. 2003 Jan;42(1):37-50. | ||||
Ref 535827 | Effects of squalene epoxidase inhibitors on Candida albicans. Antimicrob Agents Chemother. 1992 Aug;36(8):1779-81. | ||||
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. |
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