Target General Infomation
Target ID
T10897
Former ID
TTDS00516
Target Name
Acyl-CoA desaturase
Gene Name
SCD
Synonyms
9 stearoyl-desaturase; Delta(9)-desaturase; Delta-9-stearoyl desaturase; Des A3; DesA3; Fatty acid desaturase; Membrane-bound 9 desaturase; Stearoyl-CoA desaturase; Stearoyl-coenzyme A (Delta9) desaturase; SCD
Target Type
Successful
Disease Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Lipid metabolism disorder [ICD10: E75-E78]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Function
Desaturates stearoyl-CoA to form oleoyl-CoA.
BioChemical Class
Oxidoreductases acting on paired donors
Target Validation
T10897
UniProt ID
EC Number
EC 1.14.19.1
Sequence
MPAHLLQDDISSSYTTTTTITAPPSRVLQNGGDKLETMPLYLEDDIRPDIKDDIYDPTYK
DKEGPSPKVEYVWRNIILMSLLHLGALYGITLIPTCKFYTWLWGVFYYFVSALGITAGAH
RLWSHRSYKARLPLRLFLIIANTMAFQNDVYEWARDHRAHHKFSETHADPHNSRRGFFFS
HVGWLLVRKHPAVKEKGSTLDLSDLEAEKLVMFQRRYYKPGLLMMCFILPTLVPWYFWGE
TFQNSVFVATFLRYAVVLNATWLVNSAAHLFGYRPYDKNISPRENILVSLGAVGEGFHNY
HHSFPYDYSASEYRWHINFTTFFIDCMAALGLAYDRKKVSKAAILARIKRTGDGNYKSG
Drugs and Mode of Action
Drug(s) Isoxyl Drug Info Approved Bacterial infections [536854]
Aramchol Drug Info Phase 2/3 Lipid metabolism disorder [524975]
MK-8245 Drug Info Phase 2 Type 2 diabetes [522582]
Inhibitor 2-(4-benzoylpiperazin-1-yl)thiazole-5-carboxamide Drug Info [530276]
Aramchol Drug Info [531248], [532774]
CVT-12012 Drug Info [530248]
MF-152 Drug Info [530690]
MK-8245 Drug Info [531508]
Sterculic acid Drug Info [551871]
Thiocarlide Drug Info [535853]
Binder Isoxyl Drug Info [536854]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Metabolic pathways
References
Ref 522582ClinicalTrials.gov (NCT00846391) A Study to Assess the Safety and Efficacy of MK8245 in Patients With Type 2 Diabetes Mellitus and Inadequate Glycemic Control (MK8245-005 AM2). U.S. National Institutes of Health.
Ref 524975ClinicalTrials.gov (NCT02279524) A Clinical Trial to Evaluate the Efficacy and Safety of Two Aramchol Doses Versus Placebo in Patients With NASH. U.S. National Institutes of Health.
Ref 536854Has nature already identified all useful antibacterial targets? Curr Opin Microbiol. 2008 Oct;11(5):387-92. Epub 2008 Oct 6.
Ref 530248Bioorg Med Chem Lett. 2009 Aug 1;19(15):4070-4. Epub 2009 Jun 13.Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors.
Ref 530276Bioorg Med Chem Lett. 2009 Sep 1;19(17):5214-7. Epub 2009 Jul 9.Thiazole analog as stearoyl-CoA desaturase 1 inhibitor.
Ref 530690Bioorg Med Chem Lett. 2010 Mar 1;20(5):1593-7. Epub 2010 Jan 21.SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors.
Ref 531248Fatty acid bile acid conjugate inhibits hepatic stearoyl coenzyme A desaturase and is non-atherogenic. Arch Med Res. 2010 Aug;41(6):397-404.
Ref 531508Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. J Med Chem. 2011 Jul 28;54(14):5082-96.
Ref 532774The fatty acid-bile acid conjugate Aramchol reduces liver fat content in patients with nonalcoholic fatty liver disease. Clin Gastroenterol Hepatol. 2014 Dec;12(12):2085-91.e1.
Ref 535853Unique mechanism of action of the thiourea drug isoxyl on Mycobacterium tuberculosis. J Biol Chem. 2003 Dec 26;278(52):53123-30. Epub 2003 Oct 14.
Ref 536854Has nature already identified all useful antibacterial targets? Curr Opin Microbiol. 2008 Oct;11(5):387-92. Epub 2008 Oct 6.
Ref 549662US patent application no. 7,132,529, Antisense modulation of stearoyl-CoA desaturase expression.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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