Target Information

Target General Infomation
Target ID
T93344
Former ID
TTDS00302
Target Name
Squalene monooxygenase
Gene Name
SQLE
Synonyms
ERG1; Oxidosqaulene cyclase; SE; Squalene epoxidase; SQLE
Target Type
Successful
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.
BioChemical Class
Oxidoreductases acting on paired donors
Target Validation
T93344
UniProt ID
Q14534
EC Number
EC 1.14.99.7
Sequence
MWTFLGIATFTYFYKKFGDFITLANREVLLCVLVFLSLGLVLSYRCRHRNGGLLGRQQSG
SQFALFSDILSGLPFIGFFWAKSPPESENKEQLEARRRRKGTNISETSLIGTAACTSTSS
QNDPEVIIVGAGVLGSALAAVLSRDGRKVTVIERDLKEPDRIVGEFLQPGGYHVLKDLGL
GDTVEGLDAQVVNGYMIHDQESKSEVQIPYPLSENNQVQSGRAFHHGRFIMSLRKAAMAE
PNAKFIEGVVLQLLEEDDVVMGVQYKDKETGDIKELHAPLTVVADGLFSKFRKSLVSNKV
SVSSHFVGFLMKNAPQFKANHAELILANPSPVLIYQISSSETRVLVDIRGEMPRNLREYM
VEKIYPQIPDHLKEPFLEATDNSHLRSMPASFLPPSSVKKRGVLLLGDAYNMRHPLTGGG
MTVAFKDIKLWRKLLKGIPDLYDDAAIFEAKKSFYWARKTSHSFVVNILAQALYELFSAT
DDSLHQLRKACFLYFKLGGECVAGPVGLLSVLSPNPLVLIGHFFAVAIYAVYFCFKSEPW
ITKPRALLSSGAVLYKACSVIFPLIYSEMKYMVH
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)
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 538523FDA 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 544824Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001234)
Ref 546677Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009590)
Ref 550769Drug information of Tolnaftate, 2008. eduDrugs.
Ref 551702Chemotherapy of fungal diseases. 1990. Page(525-550).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 526128J Nat Prod. 2001 Aug;64(8):1010-4.Ellagitannins and hexahydroxydiphenoyl esters as inhibitors of vertebrate squalene epoxidase.
Ref 526940Synthesis and biological activity of a novel squalene epoxidase inhibitor, FR194738. Bioorg Med Chem Lett. 2004 Feb 9;14(3):633-7.
Ref 535625Squalene epoxidase as hypocholesterolemic drug target revisited. Prog Lipid Res. 2003 Jan;42(1):37-50.
Ref 535827Effects of squalene epoxidase inhibitors on Candida albicans. Antimicrob Agents Chemother. 1992 Aug;36(8):1779-81.
Ref 537454Mode 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 537992Characterization 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 538028Differential 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.

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