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2-[(Z)-[2-[4-(3-nitrophenyl)-1,3-thiazol-2-yl]hydrazinylidene]methyl]pyridine
good inhibition activity against two enzyme overexpressing cancer cell lines. IC50 value for MDA-MB-468 cell 0.0083 mM, for SW-480 cell 0.0015 mM
3-hydroxynaphthalen-1-yl 3,4,5-trihydroxybenzoate
analog of (-)-epigallocatechin 3-gallate. Compound displays moderate to high cytotoxicity and significantly blocks FASN activity, diminishes FASN protein expression levels and induces apoptosis
4-hydroxynaphthalen-2-yl 3,4,5-trihydroxybenzoate
analog of (-)-epigallocatechin 3-gallate. Compound displays moderate to high cytotoxicity and significantly blocks FASN activity, diminishes FASN protein expression levels and induces apoptosis
naphthalene-1,3-diyl bis(3,4,5-trihydroxybenzoate)
analog of (-)-epigallocatechin 3-gallate. Compound displays moderate to high cytotoxicity and significantly blocks FASN activity, diminishes FASN protein expression levels
[1,1'-biphenyl]-4,4'-diyl bis(3,4,5-trihydroxybenzoate)
analog of (-)-epigallocatechin 3-gallate. Compound displays moderate to high cytotoxicity and significantly blocks FASN activity
(10E,12Z)-octadec-10,12-dienoic acid
-
more potent inhibitor than (9Z,11E)-octadec-9,11-dienoic acid
(9Z,11E)-octadec-9,11-dienoic acid
-
-
1,2,3,4,6-penta-O-galloyl-beta-D-glucose
-
compound is transported across cancer cell membrane to further down-regulate FAS and activate caspase-3 in MDA-MB-231 cells. Compared with other FAS inhibitors, including catechin gallate and morin, 1,2,3,4,6-penta-O-galloyl-beta-D-glucose involves a higher reversible fast-binding inhibition with an irreversible slow-binding inhibition, i.e. saturation kinetics with a dissociation constant of 0.59 microM and a limiting rate constant of 0.16 per min. The major reacting site of PGG is on the beta-ketoacyl reduction domain of FAS. Compound exhibits different types of inhibitions against the three substrates in the FAS overall reaction
1,3-Dibromo-2-propanone
-
-
adriamycin
-
cytotoxic activity against cancer cells, IC50 value for MCF-7 cell 0.0035 mM, for A-549 cell 0.0018 mM, for HL-60 cell 0.0008 mM
diisopropylfluorophosphate
-
-
dutasteride
-
at clinically relevant levels, inhibits FASN mRNA, protein expression and enzymatic activity in prostate cancer cells
epigallocatechin-3-gallate
-
-
ginkgolic acid C15:1
-
DELTA8 and DELTA10 isomers, at ratio 1:2. Cytotoxic activity against cancer cells, IC50 value for MCF-7 cell 0.146 mM, for A-549 cell 0.066 mM, for HL-60 cell 0.005 mM
ginkgolic acid C17:1
-
double bond positions not specified. Cytotoxic activity against cancer cells, IC50 value for MCF-7 cell 0.093 mM, for A-549 cell 0.050 mM, for HL-60 cell 0.004 mM
ginkgolic acid C17:2
-
double bond positions not specified. Cytotoxic activity against cancer cells, IC50 value for MCF-7 cell 0.108 mM, for A-549 cell 0.056 mM, for HL-60 cell 0.004 mM
iodoacetamide
-
beta-ketoacyl synthetase activity, acetyl-CoA but not malonyl-CoA protects
procyanidin
-
procyanidins isolated from seeds of Hippophae rhamnoides inhibits the activity of FAS and reduces MDA-MB-231 cell viability with an IC50 value of 37.5 microg/ml. Procyanidins induce MDA-MB-231 cell apoptosis
pyridoxal 5'-phosphate
-
enoyl reductase activity, NADPH protects
tetrahydrolipstatin
-
i.e. orlistat
trans-4-carboxy-5-octyl-3-methylenebutyrolactone
-
-
cerulenin
-
-
cerulenin
-
significant reduction of proliferation of cell lines
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Atherosclerosis
Macrophage fatty-acid synthase deficiency decreases diet-induced atherosclerosis.
Breast Neoplasms
Malonyl-coenzyme-A is a potential mediator of cytotoxicity induced by fatty-acid synthase inhibition in human breast cancer cells and xenografts.
Carcinoma, Hepatocellular
Human fatty acid synthase: properties and molecular cloning.
Chronic Periodontitis
Structural characterization of Porphyromonas gingivalis enoyl-ACP reductase II (FabK).
Dehydration
Covalent modification of the Mycobacterium tuberculosis FAS-II dehydratase by Isoxyl and Thiacetazone.
Dehydration
Mechanisms of Resistance Associated with the Inhibition of the Dehydration Step of Type II Fatty Acid Synthase in Mycobacterium tuberculosis.
Dehydration
The missing piece of the type II fatty acid synthase system from Mycobacterium tuberculosis.
fatty-acid synthase system deficiency
Macrophage fatty-acid synthase deficiency decreases diet-induced atherosclerosis.
Infections
A combined transcriptome and proteome survey of malaria parasite liver stages.
Infections
Permissive Fatty Acid Incorporation Promotes Staphylococcal Adaptation to FASII Antibiotics in Host Environments.
Infections
Structural and biological evaluation of a novel series of benzimidazole inhibitors of Francisella tularensis enoyl-ACP reductase (FabI).
Infections
The Staphylococcus aureus FASII bypass escape route from FASII inhibitors.
Insulin Resistance
Antiobesity efficacy of asiatic acid: down-regulation of adipogenic and inflammatory processes in high fat diet induced obese rats.
Insulin Resistance
ChREBP binding and histone modifications modulate hepatic expression of the Fasn gene in a metabolic syndrome rat model.
Insulin Resistance
Effects of extended-release niacin on lipid profile and adipocyte biology in patients with impaired glucose tolerance.
Malaria
2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections.
Malaria
2-Octadecynoic acid as a dual life stage inhibitor of Plasmodium infections and plasmodial FAS-II enzymes.
Malaria
A combined transcriptome and proteome survey of malaria parasite liver stages.
Malaria
Analogues of thiolactomycin as potential antimalarial agents.
Malaria
Characterization of the Plasmodium falciparum and P. berghei glycerol 3-phosphate acyltransferase involved in FASII fatty acid utilization in the malaria parasite apicoplast.
Malaria
Expression, purification and crystallization of the Plasmodium falciparum enoyl reductase.
Malaria
Fatty acid metabolism in the Plasmodium apicoplast: Drugs, doubts and knockouts.
Malaria
Type II fatty acid biosynthesis is essential for Plasmodium falciparum sporozoite development in the midgut of Anopheles mosquitoes.
Neoplasms
4-methylene-2-octyl-5-oxotetrahydrofuran-3-carboxylic acid (C75), an inhibitor of fatty-acid synthase, suppresses the mitochondrial fatty acid synthesis pathway and impairs mitochondrial function.
Neoplasms
Antiobesity efficacy of asiatic acid: down-regulation of adipogenic and inflammatory processes in high fat diet induced obese rats.
Neoplasms
Characterization and inhibition of fatty acid synthase in pediatric tumor cell lines.
Neoplasms
Fatty acid synthase as a tumor marker: its extracellular expression in human breast cancer.
Neoplasms
Fatty-acid synthase and human cancer: new perspectives on its role in tumor biology.
Neoplasms
Inhibition of fatty-acid synthase induces caspase-8-mediated tumor cell apoptosis by up-regulating DDIT4.
Neoplasms
Inhibitive effect of zinc ion on fatty acid synthase from chicken liver.
Neoplasms
Lipid signalling enforces functional specialization of Treg cells in tumours.
Neoplasms
Malonyl-coenzyme-A is a potential mediator of cytotoxicity induced by fatty-acid synthase inhibition in human breast cancer cells and xenografts.
Neoplasms
Proto-oncogene FBI-1 (Pokemon) and SREBP-1 Synergistically Activate Transcription of Fatty-acid Synthase Gene (FASN).
Neoplasms
The galloyl moiety of green tea catechins is the critical structural feature to inhibit fatty-acid synthase.
Neuroblastoma
Characterization and inhibition of fatty acid synthase in pediatric tumor cell lines.
Obesity
Identification and structural characterization of an unusual mycobacterial monomeromycolyl-diacylglycerol.
Polycystic Kidney Diseases
A C. elegans model for mitochondrial fatty acid synthase II: the longevity-associated gene W09H1.5/mecr-1 encodes a 2-trans-enoyl-thioester reductase.
Prostatic Neoplasms
Association of fatty-acid synthase polymorphisms and expression with outcomes after radical prostatectomy.
Retinoblastoma
Characterization and inhibition of fatty acid synthase in pediatric tumor cell lines.
Rhabdoid Tumor
Characterization and inhibition of fatty acid synthase in pediatric tumor cell lines.
Sepsis
Permissive Fatty Acid Incorporation Promotes Staphylococcal Adaptation to FASII Antibiotics in Host Environments.
Starvation
Dietary-induced pre-translational control of rat fatty acid synthase.
Toxoplasmosis
Apicoplast-Localized Lysophosphatidic Acid Precursor Assembly Is Required for Bulk Phospholipid Synthesis in Toxoplasma gondii and Relies on an Algal/Plant-Like Glycerol 3-Phosphate Acyltransferase.
Tuberculosis
A common mechanism of inhibition of the Mycobacterium tuberculosis mycolic acid biosynthetic pathway by isoxyl and thiacetazone.
Tuberculosis
A novel interaction linking the FAS-II and phthiocerol dimycocerosate (PDIM) biosynthetic pathways.
Tuberculosis
AccD6, a key carboxyltransferase essential for mycolic acid synthesis in Mycobacterium tuberculosis, is dispensable in a nonpathogenic strain.
Tuberculosis
AccD6, a member of the Fas II locus, is a functional carboxyltransferase subunit of the acyl-coenzyme A carboxylase in Mycobacterium tuberculosis.
Tuberculosis
AcpM, the meromycolate extension acyl carrier protein of Mycobacterium tuberculosis, is activated by the 4'-phosphopantetheinyl transferase PptT, a potential target of the multistep mycolic acid biosynthesis.
Tuberculosis
Analogs of the antituberculous agent pyrazinamide are competitive inhibitors of NADPH binding to M. tuberculosis fatty acid synthase I.
Tuberculosis
Biochemical characterization of acyl carrier protein (AcpM) and malonyl-CoA:AcpM transacylase (mtFabD), two major components of Mycobacterium tuberculosis fatty acid synthase II.
Tuberculosis
Characterization and site-directed mutagenesis of the putative novel acyl carrier protein Rv0033 and Rv1344 from Mycobacterium tuberculosis.
Tuberculosis
Characterization of Mycobacterium smegmatis expressing the Mycobacterium tuberculosis fatty acid synthase I (fas1) gene.
Tuberculosis
Covalent modification of the Mycobacterium tuberculosis FAS-II dehydratase by Isoxyl and Thiacetazone.
Tuberculosis
Crystal structure of MabA from Mycobacterium tuberculosis, a reductase involved in long-chain fatty acid biosynthesis.
Tuberculosis
Crystal structure of the Mycobacterium tuberculosis enoyl-ACP reductase, InhA, in complex with NAD+ and a C16 fatty acyl substrate.
Tuberculosis
Detection and Confirmation of Alkaloids in Leaves of Justicia adhatoda and Bioinformatics Approach to Elicit Its Anti-tuberculosis Activity.
Tuberculosis
Development of a scintillation proximity assay for the Mycobacterium tuberculosis KasA and KasB enzymes involved in mycolic acid biosynthesis.
Tuberculosis
Expression of a recombinant, 4'-Phosphopantetheinylated, active M. tuberculosis fatty acid synthase I in E. coli.
Tuberculosis
Expression, purification, and characterization of the Mycobacterium tuberculosis acyl carrier protein, AcpM.
Tuberculosis
Flavonoid inhibitors as novel antimycobacterial agents targeting Rv0636, a putative dehydratase enzyme involved in Mycobacterium tuberculosis fatty acid synthase II.
Tuberculosis
Function of heterologous Mycobacterium tuberculosis InhA, a type 2 fatty acid synthase enzyme involved in extending C20 fatty acids to C60-to-C90 mycolic acids, during de novo lipoic acid synthesis in Saccharomyces cerevisiae.
Tuberculosis
Inhibition of isolated Mycobacterium tuberculosis fatty acid synthase I by pyrazinamide analogs.
Tuberculosis
Inhibitory activity of pentacyano(isoniazid)ferrate(II), IQG-607, against promastigotes and amastigotes forms of Leishmania braziliensis.
Tuberculosis
Lack of Specificity of Phenotypic Screens for Inhibitors of the Mycobacterium tuberculosis FAS-II System.
Tuberculosis
Ligand-induced fit in mycobacterial MabA: the sequence-specific C-terminus locks the conformational change.
Tuberculosis
MabA (FabG1), a Mycobacterium tuberculosis protein involved in the long-chain fatty acid elongation system FAS-II.
Tuberculosis
Mechanisms of Resistance Associated with the Inhibition of the Dehydration Step of Type II Fatty Acid Synthase in Mycobacterium tuberculosis.
Tuberculosis
Physiological Function of Mycobacterial mtFabD, an Essential Malonyl-CoA:AcpM Transacylase of Type 2 Fatty Acid Synthase FASII, in Yeast mct1Delta Cells.
Tuberculosis
Point mutations within the fatty acid synthase type II dehydratase components HadA or HadC contribute to isoxyl resistance in Mycobacterium tuberculosis.
Tuberculosis
Probing reactivity and substrate specificity of both subunits of the dimeric Mycobacterium tuberculosis FabH using alkyl-CoA disulfide inhibitors and acyl-CoA substrates.
Tuberculosis
Purification and biochemical characterization of the Mycobacterium tuberculosis beta-ketoacyl-acyl carrier protein synthases KasA and KasB.
Tuberculosis
Pyrazinamide, but not pyrazinoic acid, is a competitive inhibitor of NADPH binding to Mycobacterium tuberculosis fatty acid synthase I.
Tuberculosis
Rv3080c regulates the rate of inhibition of mycobacteria by isoniazid through FabD.
Tuberculosis
The condensing activities of the Mycobacterium tuberculosis type II fatty acid synthase are differentially regulated by phosphorylation.
Tuberculosis
The missing piece of the type II fatty acid synthase system from Mycobacterium tuberculosis.
Tuberculosis
The Mycobacterium tuberculosis FAS-II condensing enzymes: their role in mycolic acid biosynthesis, acid-fastness, pathogenesis and in future drug development.
Tuberculosis
The Mycobacterium tuberculosis FAS-II dehydratases and methyltransferases define the specificity of the mycolic acid elongation complexes.
Tuberculosis
The new tuberculosis drug Perchlozone(®) shows cross-resistance with thiacetazone.
Tuberculosis
Triclosan inhibition of mycobacterial InhA in Saccharomyces cerevisiae: yeast mitochondria as a novel platform for in vivo antimycolate assays.
Tuberculosis
X-ray crystal structure of Mycobacterium tuberculosis beta-ketoacyl acyl carrier protein synthase II (mtKasB).
Urinary Bladder Neoplasms
Inhibition of Fatty-acid Synthase Suppresses P-AKT and Induces Apoptosis in Bladder Cancer.
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Fatty acid synthesis and its regulation
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Cloning and expression of the multifunctional human fatty acid synthase and its subdomains in Escherichia coli
Proc. Natl. Acad. Sci. USA
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Human fatty acid synthase: properties and molecular cloning
Proc. Natl. Acad. Sci. USA
92
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1995
Homo sapiens
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Wagle, S.; Bui, A.; Ballard, P.L.; Shuman, H.; Gonzales, J.; Gonzales, L.W.
Hormonal regulation and cellular localization of fatty acid synthase in human fetal lung
Am. J. Physiol.
277
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1999
Homo sapiens
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Swinnen, J.V.; Van Veldhoven, P.P.; Timmermans, L.; De Schrijver, E.; Brusselmans, K.; Vanderhoydonc, F.; Van de Sande, T.; Heemers, H.; Heyns, W.; Verhoeven, G.
Fatty acid synthase drives the synthesis of phospholipids partitioning into detergent-resistant membrane microdomains
Biochem. Biophys. Res. Commun.
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2003
Homo sapiens
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Agostini, M.; Silva, S.D.; Zecchin, K.G.; Coletta, R.D.; Jorge, J.; Loda, M.; Graner, E.
Fatty acid synthase is required for the proliferation of human oral squamous carcinoma cells
Oral Oncol.
40
728-735
2004
Homo sapiens
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Chakravarty, B.; Gu, Z.; Chirala, S.S.; Wakil, S.J.; Quiocho, F.A.
Human fatty acid synthase: structure and substrate selectivity of the thioesterase domain
Proc. Natl. Acad. Sci. USA
101
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2004
Homo sapiens (P49327)
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Carlisle-Moore, L.; Gordon, C.R.; Machutta, C.A.; Miller, W.T.; Tonge, P.J.
Substrate recognition by the human fatty-acid synthase
J. Biol. Chem.
280
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2005
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Asturias, F.J.
Mammalian fatty acid synthase: X-ray structure of a molecular assembly line
ACS Chem. Biol.
1
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2006
Homo sapiens
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Consolazio, A.; Alo, P.L.; Rivera, M.; Iacopini, F.; Paoluzi, O.A.; Crispino, P.; Pica, R.; Paoluzi, P.
Overexpression of fatty acid synthase in ulcerative colitis
Am. J. Clin. Pathol.
126
113-118
2006
Homo sapiens
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Lupu, R.; Menendez, J.A.
Pharmacological inhibitors of fatty acid synthase (FASN)-catalyzed endogenous fatty acid biogenesis: a new family of anti-cancer agents?
Curr. Pharm. Biotechnol.
7
483-494
2006
Homo sapiens
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van de Sande, T.; Roskams, T.; Lerut, E.; Joniau, S.; Van Poppel, H.; Verhoeven, G.; Swinnen, J.V.
High-level expression of fatty acid synthase in human prostate cancer tissues is linked to activation and nuclear localization of Akt/PKB
J. Pathol.
206
214-219
2005
Homo sapiens
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Wang, H.Q.; Altomare, D.A.; Skele, K.L.; Poulikakos, P.I.; Kuhajda, F.P.; Di Cristofano, A.; Testa, J.R.
Positive feedback regulation between AKT activation and fatty acid synthase expression in ovarian carcinoma cells
Oncogene
24
3574-3582
2005
Homo sapiens
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Schmidt, L.J.; Ballman, K.V.; Tindall, D.J.
Inhibition of fatty acid synthase activity in prostate cancer cells by dutasteride
Prostate
67
1111-1120
2007
Homo sapiens
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Grunt, T.W.; Wagner, R.; Grusch, M.; Berger, W.; Singer, C.F.; Marian, B.; Zielinski, C.C.; Lupu, R.
Interaction between fatty acid synthase- and ErbB-systems in ovarian cancer cells
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Kim, K.J.; Kim, H.Y.; Cho, H.K.; Kim, K.H.; Cheong, J.
The SDF-1alpha/CXCR4 axis induces the expression of fatty acid synthase via sterol regulatory element binding protein-1 activation in cancer cells
Carcinogenesis
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679-686
2010
Homo sapiens
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Lu, S.; Archer, M.C.
Sp1 coordinately regulates de novo lipogenesis and proliferation in cancer cells
Int. J. Cancer
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416-425
2010
Homo sapiens
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Lau, D.S.; Archer, M.C.
The 10t,12c isomer of conjugated linoleic acid inhibits fatty acid synthase expression and enzyme activity in human breast, colon, and prostate cancer cells
Nutr. Cancer
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2010
Homo sapiens
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Chen, Q.; Reimer, R.A.
Dairy protein and leucine alter GLP-1 release and mRNA of genes involved in intestinal lipid metabolism in vitro
Nutrition
25
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2009
Homo sapiens
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Zeng, X.F.; Li, W.W.; Fan, H.J.; Wang, X.Y.; Ji, P.; Wang, Z.R.; Ma, S.; Li, L.L.; Ma, X.F.; Yang, S.Y.
Discovery of novel fatty acid synthase (FAS) inhibitors based on the structure of ketoaceyl synthase (KS) domain
Bioorg. Med. Chem. Lett.
21
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2011
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Oh, J.; Hwang, I.H.; Hong, C.E.; Lyu, S.Y.; Na, M.
Inhibition of fatty acid synthase by ginkgolic acids from the leaves of Ginkgo biloba and their cytotoxic activity
J. Enzyme Inhib. Med. Chem.
28
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2013
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Pappenberger, G.; Benz, J.; Gsell, B.; Hennig, M.; Ruf, A.; Stihle, M.; Thoma, R.; Rudolph, M.G.
Structure of the human fatty acid synthase KS-MAT didomain as a framework for inhibitor design
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2010
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Zhao, W.; Wang, Y.; Hao, W.; Zhao, M.; Peng, S.
In vitro inhibition of fatty acid synthase by 1,2,3,4,6-penta-O-galloyl-beta-D-glucose plays a vital role in anti-tumour activity
Biochem. Biophys. Res. Commun.
445
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2014
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Cui, W.; Liang, Y.; Tian, W.; Ji, M.; Ma, X.
Regulating effect of beta-ketoacyl synthase domain of fatty acid synthase on fatty acyl chain length in de novo fatty acid synthesis
Biochim. Biophys. Acta
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2016
Homo sapiens
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Hopperton, K.E.; Duncan, R.E.; Bazinet, R.P.; Archer, M.C.
Fatty acid synthase plays a role in cancer metabolism beyond providing fatty acids for phospholipid synthesis or sustaining elevations in glycolytic activity
Exp. Cell Res.
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2014
Homo sapiens
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Hopcroft, P.; Fisher, D.
Development of a medium-throughput targeted LCMS assay to detect endogenous cellular levels of malonyl-CoA to screen fatty acid synthase inhibitors
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21
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2016
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Liu, H.; Wu, X.; Dong, Z.; Luo, Z.; Zhao, Z.; Xu, Y.; Zhang, J.T.
Fatty acid synthase causes drug resistance by inhibiting TNF-alpha and ceramide production
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Bollu, L.R.; Katreddy, R.R.; Blessing, A.M.; Pham, N.; Zheng, B.; Wu, X.; Weihua, Z.
Intracellular activation of EGFR by fatty acid synthase dependent palmitoylation
Oncotarget
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34992-35003
2015
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Wang, Y.; Nie, F.; Ouyang, J.; Wang, X.; Ma, X.
Inhibitory effects of sea buckthorn procyanidins on fatty acid synthase and MDA-MB-231 cells
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Crous-Maso, J.; Palomeras, S.; Relat, J.; Camo, C.; Martinez-Garza, U.; Planas, M.; Feliu, L.; Puig, T.
(-)-Epigallocatechin 3-gallate synthetic analogues inhibit fatty acid synthase and show anticancer activity in triple negative breast cancer
Molecules
23
1160
2018
Homo sapiens (P49327)
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