Therapeutic Targets Database
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TTD Target ID: TTDS00295

Target Information
NameFatty acid synthase    
Type of targetSuccessful target    
SynonymsFAS    
Fatty acyl-CoA synthetase enzyme    
Fatty-acyl-CoA synthase    
Yeast fatty acid synthase    
DiseaseEndometrial carcinoma
[ICD9: 182.0   ICD10: C54.1]
[1]
Leukemia, unspecified
[ICD9: 208.9   ICD10: C91-C95]
[2]
Malaria
[ICD9: 084   ICD10: B50-B54]
[3]
Mesothelioma
[ICD9: 163   ICD10: C45]
[4]
Metastatic osteosarcoma in the lung
[ICD9: 170   ICD10: C40-C41]
[5]
Obesity
[ICD9: 278   ICD10: E66]
[6][7][8]
Prostate cancer
[ICD9: 185   ICD10: C61]
[9][10][11]
Tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[12][8]
Drug(s)CeruleninApprovedDramatic weight loss[13][2][14]
FAS1PreclinicalFungal diseases[15]
FSA2PreclinicalFungal diseases[15]
BioChemical ClassAcyltransferases    
EC NumberEC 2.3.1.85
EC 2.3.1.86
PathwayFatty acid biosynthesis
Insulin signaling pathway
Metabolic pathways
UniProt IDP49327
PDB Structure1XKT; 2CG5; 2JFD; 2JFK; 2PX6; 3HHD; 3TJM.    
FunctionFatty acid synthetase catalyzes the formation of long- chain fatty acids from acetyl-coa, malonyl-coa and nadph. This multifunctional protein has 7 catalytic activities and an acyl carrier protein.    
SequenceMEEVVIAGMSGKLPESENLQEFWDNLIGGVDMVTDDDRRWKAGLYGLPRRSGKLKDLSRF DASFFGVHPKQAHTMDPQLRLLLEVTYEAIVDGGINPDSLRGTHTGVWVGVSGSETSEAL SRDPETLVGYSMVGCQRAMMANRLSFFFDFRGPSIALDTACSSSLMALQNAYQAIHSGQC PAAIVGGINVLLKPNTSVQFLRLGMLSPEGTCKAFDTAGNGYCRSEGVVAVLLTKKSLAR RVYATILNAGTNTDGFKEQGVTFPSGDIQEQLIRSLYQSAGVAPESFEYIEAHGTGTKVG DPQELNGITRALCATRQEPLLIGSTKSNMGHPEPASGLAALAKVLLSLEHGLWAPNLHFH SPNPEIPALLDGRLQVVDQPLPVRGGNVGINSFGFGGSNVHIILRPNTQPPPAPAPHATL PRLLRASGRTPEAVQKLLEQGLRHSQDLAFLSMLNDIAAVPATAMPFRGYAVLGGERGGP EVQQVPAGERPLWFICSGMGTQWRGMGLSLMRLDRFRDSILRSDEAVKPFGLKVSQLLLS TDESTFDDIVHSFVSLTAIQIGLIDLLSCMGLRPDGIVGHSLGEVACGYADGCLSQEEAV LAAYWRGQCIKEAHLPPGAMAAVGLSWEECKQRCPPGVVPACHNSKDTVTISGPQAPVFE FVEQLRKEGVFAKEVRTGGMAFHSYFMEAIAPPLLQELKKVIREPKPRSARWLSTSIPEA QWHSSLARTSSAEYNVNNLVSPVLFQEALWHVPEHAVVLEIAPHALLQAVLKRGLKPSCT IIPLMKKDHRDNLEFFLAGIGRLHLSGIDANPNALFPPVEFPAPRGTPLISPLIKWDHSL AWDVPAAEDFPNGSGSPSAAIYNIDTSSESPDHYLVDHTLDGRVLFPATGYLSIVWKTLA RALGLGVEQLPVVFEDVVLHQATILPKTGTVSLEVRLLEASRAFEVSENGNLVVSGKVYQ WDDPDPRLFDHPESPTPNPTEPLFLAQAEVYKELRLRGYDYGPHFQGILEASLEGDSGRL LWKDNWVSFMDTMLQMSILGSAKHGLYLPTRVTAIHIDPATHRQKLYTLQDKAQVADVVV SRWLRVTVAGGVHISGLHTESAPRRQQEQQVPILEKFCFTPHTEEGCLSERAALQEELQL CKGLVQALQTTVTQQGLKMVVPGLDGAQIPRDPSQQELPRLLSAACRLQLNGNLQLELAQ VLAQERPKLPEDPLLSGLLDSPALKACLDTAVENMPSLKMKVVEVLAGHGHLYSRIPGLL SPHPLLQLSYTATDRHPQALEAAQAELQQHDVAQGQWDPADPAPSALGSADLLVCNCAVA ALGDPASALSNMVAALREGGFLLLHTLLRGHPLGDIVAFLTSTEPQYGQGILSQDAWESL FSRVSLRLVGLKKSFYGSTLFLCRRPTPQDSPIFLPVDDTSFRWVESLKGILADEDSSRP VWLKAINCATSGVVGLVNCLRREPGGNRLRCVLLSNLSSTSHVPEVDPGSAELQKVLQGD LVMNVYRDGAWGAFRHFLLEEDKPEEPTAHAFVSTLTRGDLSSIRWVCSSLRHAQPTCPG AQLCTVYYASLNFRDIMLATGKLSPDAIPGKWTSQDSLLGMEFSGRDASGKRVMGLVPAK GLATSVLLSPDFLWDVPSNWTLEEAASVPVVYSTAYYALVVRGRVRPGETLLIHSGSGGV GQAAIAIALSLGCRVFTTVGSAEKRAYLQARFPQLDSTSFANSRDTSFEQHVLWHTGGKG VDLVLNSLAEEKLQASVRCLATHGRFLEIGKFDLSQNHPLGMAIFLKNVTFHGVLLDAFF NESSADWREVWALVQAGIRDGVVRPLKCTVFHGAQVEDAFRYMAQGKHIGKVVVQVLAEE PEAVLKGAKPKLMSAISKTFCPAHKSYIIAGGLGGFGLELAQWLIQRGVQKLVLTSRSGI RTGYQAKQVRRWRRQGVQVQVSTSNISSLEGARGLIAEAAQLGPVGGVFNLAVVLRDGLL ENQTPEFFQDVCKPKYSGTLNLDRVTREACPELDYFVVFSSVSCGRGNAGQSNYGFANSA MERICEKRRHEGLPGLAVQWGAIGDVGILVETMSTNDTIVSGTLPQRMASCLEVLDLFLN QPHMVLSSFVLAEKAAAYRDRDSQRDLVEAVAHILGIRDLAAVNLDSSLADLGLDSLMSV EVRQTLERELNLVLSVREVRQLTLRKLQELSSKADEASELACPTPKEDGLAQQQTQLNLR SLLVNPEGPTLMRLNSVQSSERPLFLVHPIEGSTTVFHSLASRLSIPTYGLQCTRAAPLD SIHSLAAYYIDCIRQVQPEGPYRVAGYSYGACVAFEMCSQLQAQQSPAPTHNSLFLFDGS PTYVLAYTQSYRAKLTPGCEAEAETEAICFFVQQFTDMEHNRVLEALLPLKGLEERVAAA VDLIIKSHQGLDRQELSFAARSFYYKLRAAEQYTPKAKYHGNVMLLRAKTGGAYGEDLGA DYNLSQVCDGKVSVHVIEGDHRTLLEGSGLESIISIIHSSLAEPRVSVREG
Target ValidationClick to Find Target Validation Information.    
Inhibitor (-)-CATECHINGALLATE[16]
2-Hexadecynoic acid[17]
4-hydroxy-6-nitro-3-phenylquinolin-2 (1H)-one[18]
4-hydroxy-8-nitro-3-phenylquinolin-2 (1H)-one[18]
BIOCHANIN[16]
C75[19]
C75[20]
Cerulenin[13][2][14]
Cerulenin[21]
EPICATECHIN GALLATE[16]
EPIGALOCATECHIN GALLATE[16]
FAS1[15]
FISETIN[16]
FSA2[15]
GALLOCATECHIN GALLATE[16]
MORIN[16]
PA-824[22]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Inhibition of tumor-associated fatty acid synthase activity antagonizes estradiol- and tamoxifen-induced agonist transactivation of estrogen receptor (ER) in human endometrial adenocarcinoma cells. Oncogene. 2004 Jun 17;23(28):4945-58. To Reference
Ref 2Proliferation inhibition and apoptosis induction of K562 cells by fatty acid synthase inhibitor--cerulenin. Zhonghua Xue Ye Xue Za Zhi. 2000 May;21(5):244-6. To Reference
Ref 3The cloning and expression of Pfacs1, a Plasmodium falciparum fatty acyl coenzyme A synthetase-1 targeted to the host erythrocyte cytoplasm. J Mol Biol. 1999 Aug 6;291(1):59-70. To Reference
Ref 4Increased fatty acid synthase is a therapeutic target in mesothelioma. Clin Cancer Res. 2001 Jan;7(1):153-7. To Reference
Ref 5Fas expression inversely correlates with metastatic potential in osteosarcoma cells. Oncol Rep. 2002 Jul-Aug;9(4):823-7. To Reference
Ref 6Regulation of fatty acid synthase (FAS). Prog Lipid Res. 1997 Mar;36(1):43-53. To Reference
Ref 7Weight reduction by Chinese medicinal herbs may be related to inhibition of fatty acid synthase. Life Sci. 2004 Mar 26;74(19):2389-99. To Reference
Ref 8A fatty acid synthase blockade induces tumor cell-cycle arrest by down-regulating Skp2. J Biol Chem. 2004 Jul 16;279(29):30540-5. Epub 2004 May 11. To Reference
Ref 9Overexpression of fatty acid synthase is an early and common event in the development of prostate cancer. Int J Cancer. 2002 Mar 1;98(1):19-22. To Reference
Ref 10Increased fatty acid synthase expression and activity during progression of prostate cancer in the TRAMP model. Prostate. 2003 Nov 1;57(3):245-54. To Reference
Ref 11Fatty acid synthase: a metabolic oncogene in prostate cancer? J Cell Biochem. 2004 Jan 1;91(1):47-53. To Reference
Ref 12Fatty-acid synthase and human cancer: new perspectives on its role in tumor biology. Nutrition. 2000 Mar;16(3):202-8. To Reference
Ref 13Inhibition of Fatty Acid Biosynthesis Prevents Adipocyte Lipotoxicity on Human Osteoblasts In Vitro. J Cell Mol Med. 2009 Mar 27. [Epub ahead of print] To Reference
Ref 14The antibiotic cerulenin, a novel tool for biochemistry as an inhibitor of fatty acid synthesis. Bacteriol Rev. 1976 Sep;40(3):681-97. To Reference
Ref 15Novel antifungal agents, targets or therapeutic strategies for the treatment of invasive fungal diseases: a review of the literature (2005-2009). Rev Iberoam Micol. 2009 Mar 31;26(1):15-22. Epub 2009 May 7. To Reference
Ref 16J Med Chem. 2006 Jun 1;49(11):3345-53.Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. To Reference
Ref 17Bioorg Med Chem. 2010 Nov 1;18(21):7475-85. Epub 2010 Sep 18.2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections. To Reference
Ref 18Bioorg Med Chem Lett. 2006 Sep 1;16(17):4620-3. Epub 2006 Jun 19.3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors. To Reference
Ref 19C75 increases peripheral energy utilization and fatty acid oxidation in diet-induced obesity. Proc Natl Acad Sci U S A. 2002 Jul 9;99(14):9498-502. Epub 2002 Jun 11. To Reference
Ref 20Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21. To Reference
Ref 2120511185 To Reference
Ref 22Novel agents in the management of Mycobacterium tuberculosis disease. Curr Med Chem. 2007;14(18):2000-8. To Reference



 

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