Property Summary

NCBI Gene PubMed Count 196
Grant Count 56
R01 Count 20
Funding $5,088,756.66
PubMed Score 348.46
PubTator Score 756.41

Knowledge Summary

Patent

No data available

Expression

Synonym

Accession P49327 Q13479 Q16702 Q4LE83 Q6P4U5 Q6SS02 Q969R1 Q96C68 Q96IT0
Symbols FAS
OA-519
SDR27X1

Gene

PANTHER Protein Class (2)

PDB

1XKT   2CG5   2JFD   2JFK   2PX6   3HHD   3TJM   4PIV   4W82   4W9N   4Z49   5C37  

MLP Assay (12)

AID Type Active / Inconclusive / Inactive Description
602261 screening 2430 / 0 / 359958 uHTS identification of small molecule inhibitors of the thioesterase domain of fatty acid synthase via a fluorescence intensity assay
602265 summary 0 / 0 / 0 Summary assay for small molecule inhibitors of the thioesterase domain of fatty acid synthase
624325 screening 1009 / 0 / 1246 Single concentration confirmation of uHTS inhibitor hits of the thioesterase domain of fatty acid synthase via a fluorescence intensity assay
624326 confirmatory 967 / 0 / 44 Dose response confirmation of small molecule inhibitors of the thioesterase domain of fatty acid synthase via a kinetic, fluorescence intensity assay
624327 confirmatory 969 / 0 / 42 Dose response confirmation of uHTS inhibitor hits of the thioesterase domain of fatty acid synthase via a fluorescence intensity assay
651670 confirmatory 8 / 0 / 13 SAR analysis of small molecule inhibitors of the thioesterase domain of fatty acid synthase via a fluorescence intensity assay
651979 other 1 / 0 / 0 Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis in situ
651980 other 1 / 0 / 0 Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis in situ
652164 confirmatory 31 / 0 / 8 SAR confirmation of small molecule inhibitors of the thioesterase domain of fatty acid synthase via a fluorescence intensity assay
652165 confirmatory 32 / 0 / 7 SAR confirmation of small molecule inhibitors of the thioesterase domain of fatty acid synthase via a kinetic, fluorescence intensity assay
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Gene RIF (168)

PMID Text
26663084 Data suggest that thioesterase 2 (TE2) catalytic domain of FASN exhibits novel capping domain insert within the alpha/beta hydrolase core; TE2 (as opposed to TE1 domain) readily releases short chain fatty acids from full-length FASN during turnover.
26514456 Our results suggest that FASN upregulation and PTEN downregualtion may be involved in peritoneal dissemination for gastric cancer progression.
26425687 data demonstrate that selective and potent FASN inhibition with TVB-3166 leads to selective death of tumor cells, without significant effect on normal cells, and inhibits in vivo xenograft tumor growth at well-tolerated doses.
26378037 concluded that EGFR can be activated intracellularly by FASN-dependent palmitoylation
26134042 In the present study it was determined whether three key enzymes for glycolysis, glutaminolysis and de novo synthesis of FAs, hexokinase-2, glutaminase and fatty acid synthase
26109148 Loss of fatty acid synthase suppresses the malignant phenotype of colorectal cancer cells by down-regulating energy metabolism and mTOR signaling pathway.
26107737 FASN and HER2 have roles in breast cancer and are blocked by EGCG with pertuzumab or temsirolimus
26025399 The results suggested that differential levels of P-glycoprotein, Caveolin-1 and Fatty acid synthase except CYP450 play a major role in acquired resistant phenotype in bladder cancer.
25970773 Findings indicate that overexpression of FASN plays a crucial role in maintaining energy homeostasis in CRC via increased oxidation of endogenously synthesized lipids.
25958981 Results showed correlated FASN regulation relative to key signaling genes with tumor invasion and differentiation in primary retinoblastoma (RB) tissues. Its silencing exerted definite anti-cancer effects in RB cells through PI3K/AKT signaling pathway.
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AA Sequence

MEEVVIAGMSGKLPESENLQEFWDNLIGGVDMVTDDDRRWKAGLYGLPRRSGKLKDLSRFDASFFGVHPK      1 - 70
QAHTMDPQLRLLLEVTYEAIVDGGINPDSLRGTHTGVWVGVSGSETSEALSRDPETLVGYSMVGCQRAMM     71 - 140
ANRLSFFFDFRGPSIALDTACSSSLMALQNAYQAIHSGQCPAAIVGGINVLLKPNTSVQFLRLGMLSPEG    141 - 210
TCKAFDTAGNGYCRSEGVVAVLLTKKSLARRVYATILNAGTNTDGFKEQGVTFPSGDIQEQLIRSLYQSA    211 - 280
GVAPESFEYIEAHGTGTKVGDPQELNGITRALCATRQEPLLIGSTKSNMGHPEPASGLAALAKVLLSLEH    281 - 350
GLWAPNLHFHSPNPEIPALLDGRLQVVDQPLPVRGGNVGINSFGFGGSNVHIILRPNTQPPPAPAPHATL    351 - 420
PRLLRASGRTPEAVQKLLEQGLRHSQDLAFLSMLNDIAAVPATAMPFRGYAVLGGERGGPEVQQVPAGER    421 - 490
PLWFICSGMGTQWRGMGLSLMRLDRFRDSILRSDEAVKPFGLKVSQLLLSTDESTFDDIVHSFVSLTAIQ    491 - 560
IGLIDLLSCMGLRPDGIVGHSLGEVACGYADGCLSQEEAVLAAYWRGQCIKEAHLPPGAMAAVGLSWEEC    561 - 630
KQRCPPGVVPACHNSKDTVTISGPQAPVFEFVEQLRKEGVFAKEVRTGGMAFHSYFMEAIAPPLLQELKK    631 - 700
VIREPKPRSARWLSTSIPEAQWHSSLARTSSAEYNVNNLVSPVLFQEALWHVPEHAVVLEIAPHALLQAV    701 - 770
LKRGLKPSCTIIPLMKKDHRDNLEFFLAGIGRLHLSGIDANPNALFPPVEFPAPRGTPLISPLIKWDHSL    771 - 840
AWDVPAAEDFPNGSGSPSAAIYNIDTSSESPDHYLVDHTLDGRVLFPATGYLSIVWKTLARALGLGVEQL    841 - 910
PVVFEDVVLHQATILPKTGTVSLEVRLLEASRAFEVSENGNLVVSGKVYQWDDPDPRLFDHPESPTPNPT    911 - 980
EPLFLAQAEVYKELRLRGYDYGPHFQGILEASLEGDSGRLLWKDNWVSFMDTMLQMSILGSAKHGLYLPT    981 - 1050
RVTAIHIDPATHRQKLYTLQDKAQVADVVVSRWLRVTVAGGVHISGLHTESAPRRQQEQQVPILEKFCFT   1051 - 1120
PHTEEGCLSERAALQEELQLCKGLVQALQTKVTQQGLKMVVPGLDGAQIPRDPSQQELPRLLSAACRLQL   1121 - 1190
NGNLQLELAQVLAQERPKLPEDPLLSGLLDSPALKACLDTAVENMPSLKMKVVEVLAGHGHLYSRIPGLL   1191 - 1260
SPHPLLQLSYTATDRHPQALEAAQAELQQHDVAQGQWDPADPAPSALGSADLLVCNCAVAALGDPASALS   1261 - 1330
NMVAALREGGFLLLHTLLRGHPLGDIVAFLTSTEPQYGQGILSQDAWESLFSRVSLRLVGLKKSFYGSTL   1331 - 1400
FLCRRPTPQDSPIFLPVDDTSFRWVESLKGILADEDSSRPVWLKAINCATSGVVGLVNCLRREPGGNRLR   1401 - 1470
CVLLSNLSSTSHVPEVDPGSAELQKVLQGDLVMNVYRDGAWGAFRHFLLEEDKPEEPTAHAFVSTLTRGD   1471 - 1540
LSSIRWVCSSLRHAQPTCPGAQLCTVYYASLNFRDIMLATGKLSPDAIPGKWTSQDSLLGMEFSGRDASG   1541 - 1610
KRVMGLVPAKGLATSVLLSPDFLWDVPSNWTLEEAASVPVVYSTAYYALVVRGRVRPGETLLIHSGSGGV   1611 - 1680
GQAAIAIALSLGCRVFTTVGSAEKRAYLQARFPQLDSTSFANSRDTSFEQHVLWHTGGKGVDLVLNSLAE   1681 - 1750
EKLQASVRCLATHGRFLEIGKFDLSQNHPLGMAIFLKNVTFHGVLLDAFFNESSADWREVWALVQAGIRD   1751 - 1820
GVVRPLKCTVFHGAQVEDAFRYMAQGKHIGKVVVQVLAEEPEAVLKGAKPKLMSAISKTFCPAHKSYIIA   1821 - 1890
GGLGGFGLELAQWLIQRGVQKLVLTSRSGIRTGYQAKQVRRWRRQGVQVQVSTSNISSLEGARGLIAEAA   1891 - 1960
QLGPVGGVFNLAVVLRDGLLENQTPEFFQDVCKPKYSGTLNLDRVTREACPELDYFVVFSSVSCGRGNAG   1961 - 2030
QSNYGFANSAMERICEKRRHEGLPGLAVQWGAIGDVGILVETMSTNDTIVSGTLPQRMASCLEVLDLFLN   2031 - 2100
QPHMVLSSFVLAEKAAAYRDRDSQRDLVEAVAHILGIRDLAAVNLDSSLADLGLDSLMSVEVRQTLEREL   2101 - 2170
NLVLSVREVRQLTLRKLQELSSKADEASELACPTPKEDGLAQQQTQLNLRSLLVNPEGPTLMRLNSVQSS   2171 - 2240
ERPLFLVHPIEGSTTVFHSLASRLSIPTYGLQCTRAAPLDSIHSLAAYYIDCIRQVQPEGPYRVAGYSYG   2241 - 2310
ACVAFEMCSQLQAQQSPAPTHNSLFLFDGSPTYVLAYTQSYRAKLTPGCEAEAETEAICFFVQQFTDMEH   2311 - 2380
NRVLEALLPLKGLEERVAAAVDLIIKSHQGLDRQELSFAARSFYYKLRAAEQYTPKAKYHGNVMLLRAKT   2381 - 2450
GGAYGEDLGADYNLSQVCDGKVSVHVIEGDHRTLLEGSGLESIISIIHSSLAEPRVSVREG            2451 - 2511
//

Text Mined References (208)

PMID Year Title
27478939 2016 C13orf31 (FAMIN) is a central regulator of immunometabolic function.
26663084 2016 Crystal Structure and Substrate Specificity of Human Thioesterase 2: INSIGHTS INTO THE MOLECULAR BASIS FOR THE MODULATION OF FATTY ACID SYNTHASE.
26514456 2015 Expression of Fatty Acid Synthase Negatively Correlates with PTEN and Predicts Peritoneal Dissemination of Human Gastric Cancer.
26425687 2015 Inhibition of de novo Palmitate Synthesis by Fatty Acid Synthase Induces Apoptosis in Tumor Cells by Remodeling Cell Membranes, Inhibiting Signaling Pathways, and Reprogramming Gene Expression.
26378037 2015 Intracellular activation of EGFR by fatty acid synthase dependent palmitoylation.
26134042 2015 Antitumor effects of a drug combination targeting glycolysis, glutaminolysis and de novo synthesis of fatty acids.
26109148 2016 Loss of fatty acid synthase suppresses the malignant phenotype of colorectal cancer cells by down-regulating energy metabolism and mTOR signaling pathway.
26107737 2015 Dual fatty acid synthase and HER2 signaling blockade shows marked antitumor activity against breast cancer models resistant to anti-HER2 drugs.
26025399 2015 Molecular events are associated with resistance to vinblastine in bladder cancer.
25970773 2015 Increased expression of fatty acid synthase provides a survival advantage to colorectal cancer cells via upregulation of cellular respiration.
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