FASN Inhibition and Taxane Treatment Combine to Enhance Anti-tumor Efficacy in Diverse Xenograft Tumor Models through Disruption of Tubulin Palmitoylation and Microtubule Organization and FASN Inhibition-Mediated Effects on Oncogenic Signaling and Gene Expression

Heuer, Timothy S.; Ventura, Richard; Mordec, Kasia; Lai, Julie; Fridlib, Marina; Buckley, Douglas; Kemble, George

doi:10.1016/j.ebiom.2016.12.012

Cited by 137Cancer, Lipids, and MetabolismMicrotubule and mitosis dynamicsCancer Treatment and Pharmacology

FASN Inhibition and Taxane Treatment Combine to Enhance Anti-tumor Efficacy in Diverse Xenograft Tumor Models through Disruption of Tubulin Palmitoylation and Microtubule Organization and FASN Inhibition-Mediated Effects on Oncogenic Signaling and Gene Expression

Open access

Heuer, Timothy S., Ventura, Richard, Mordec, Kasia, Lai, Julie, Fridlib, Marina, Buckley, Douglas, Kemble, George·2017·EBioMedicine

DOI 10.1016/j.ebiom.2016.12.012PMC PMC5474427

Open this paper in CoChat — free account Open PDF

Abstract

Palmitate, the enzymatic product of FASN, and palmitate-derived lipids support cell metabolism, membrane architecture, protein localization, and intracellular signaling. Tubulins are among many proteins that are modified post-translationally by acylation with palmitate. We show that FASN inhibition with TVB-3166 or TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression. Disrupted microtubule organization in tumor cells is an additional consequence of FASN inhibition. FASN inhibition combined with taxane treatment enhances inhibition of in vitro tumor cell growth compared to treatment with either agent alone. In lung, ovarian, prostate, and pancreatic tumor xenograft studies, FASN inhibition and paclitaxel or docetaxel combine to inhibit xenograft tumor growth with significantly enhanced anti-tumor activity. Tumor regression was observed in 3 of 6 tumor xenograft models. FASN inhibition does not affect cellular taxane concentration in vitro. Our data suggest a mechanism of enhanced anti-tumor activity of the FASN and taxane drug combination that includes inhibition of tubulin palmitoylation and disruption of microtubule organization in tumor cells, as well as a sensitization of tumor cells to FASN inhibition-mediated effects that include gene expression changes and inhibition of β-catenin. Together, the results strongly support investigation of combined FASN inhibition and taxane treatment as a therapy for a variety of human cancers.

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Integrity signals

Registry

Crossref · 10.1016/j.ebiom.2016.12.012

Cites

52 of 52 references verified0 citation errors · 0 not checkable

Statistics

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

Targeting FASN reduces tubulin palmitoylation, disrupts microtubule organization, and inhibits tumor cell growth.
“Targeting FASN has been found to reduce palmitoylation of tubulin and disrupt microtubule organization, inhibiting tumor cell growth (Heuer et al., 2017).”
From Targeting Metabolism for Cancer Therapy (2017) · cites this paper as Heuer et al., 2017

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

Understanding the Warburg Effect: The Metabolic Requirements of Cell Proliferation
Vander Heiden, M. G., Cantley, L. C., & Thompson, C. B. (2009) · Science · doi:10.1126/science.1160809 · Cited by 16,197 · see citing works
Lipid rafts as a membrane-organizing principle
Lingwood, D., & Simons, K. (2010) · Science · doi:10.1126/science.1174621 · Cited by 4,417 · see citing works
Evidence for the Formation of Symmetric and Asymmetric DLPC-DAPC Lipid Bilayer Domains
Ritter, M., Schmidt, S., Jakab, M., Paulmichl, M., & Henderson, R. M. (2013) · Cellular Physiology and Biochemistry · doi:10.1159/000350122 · Cited by 3,923 · see citing works
Metabolic Reprogramming: A Cancer Hallmark Even Warburg Did Not Anticipate
Ward, P. S., & Thompson, C. B. (2012) · Cancer Cell · doi:10.1016/j.ccr.2012.02.014 · Cited by 3,233 · see citing works
Fatty acid synthase and the lipogenic phenotype in cancer pathogenesis
Menendez, J. A., & Lupu, R. (2007) · Nature Reviews Cancer · doi:10.1038/nrc2222 · Cited by 2,941 · see citing works
Membrane Organization and Lipid RaftsPreprint
Simons, K., & Sampaio, J. L. (2011) · Cold Spring Harbor Perspectives in Biology · doi:10.1101/cshperspect.a004697 · Cited by 1,068 · see citing works
Acetyl-CoA synthetase 2 promotes acetate utilization and maintains cancer cell growth under metabolic stress
Schug, Z. T., Peck, B., Jones, D. T., Zhang, Q., Grosskurth, S., Alam, I. S., Goodwin, L. M., Smethurst, E., Mason, S., Blyth, K., et al. (2015) · Cancer Cell · doi:10.1016/j.ccell.2014.12.002 · Cited by 820 · see citing works
De novo Lipogenesis Protects Cancer Cells from Free Radicals and Chemotherapeutics by Promoting Membrane Lipid Saturation
Rysman, E., Brusselmans, K., Scheys, K., Timmermans, L., Derua, R., Munck, S., Veldhoven, P. P. V., Waltregny, D., Daniëls, V. W., Machiels, J., et al. (2010) · Cancer Research · doi:10.1158/0008-5472.can-09-3871 · Cited by 723 · see citing works
Orlistat Is a Novel Inhibitor of Fatty Acid Synthase with Antitumor Activity
Kridel, S. J., Axelrod, F. T., Rozenkrantz, N., & Smith, J. W. (2004) · Cancer Research · doi:10.1158/0008-5472.can-03-3645 · Cited by 610 · see citing works
Fatty Acid Synthase As a Potential Therapeutic Target in Cancer
Flavin, R., Peluso, S., Nguyen, P. L., & Loda, M. F. (2010) · Future Oncology · doi:10.2217/fon.10.11 · Cited by 545 · see citing works
Palmitoylation regulates raft affinity for the majority of integral raft proteins
Levental, I., Lingwood, D., Grzybek, M., Coskun, Ü., & Simons, K. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1016184107 · Cited by 541 · see citing works
Large-scale profiling of protein palmitoylation in mammalian cells
Martin, B. R., & Cravatt, B. F. (2009) · Nature Methods · doi:10.1038/nmeth.1293 · Cited by 511 · see citing works
Palmitoylated proteins: purification and identification
Wan, J., Roth, A. F., Bailey, A. O., & Davis, N. G. (2007) · Nature Protocols · doi:10.1038/nprot.2007.225 · Cited by 417 · see citing works
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
Ventura, R., Mordec, K., Waszczuk, J., Wang, Z., Lai, J., Fridlib, M., Buckley, D., Kemble, G., & Heuer, T. S. (2015) · EBioMedicine · doi:10.1016/j.ebiom.2015.06.020 · Cited by 301 · see citing works
Self-citation
Inhibition of fatty acid desaturation is detrimental to cancer cell survival in metabolically compromised environments
Peck, B., Schug, Z. T., Zhang, Q., Dankworth, B., Jones, D. T., Smethurst, E. A., Patel, R., Mason, S. M., Jiang, M., Saunders, R. E., et al. (2016) · Cancer & Metabolism · doi:10.1186/s40170-016-0146-8 · Cited by 254 · see citing works
Inhibition of DHHC20-Mediated EGFR Palmitoylation Creates a Dependence on EGFR Signaling
Runkle, K. B., Kharbanda, A., Stypulkowski, E., Cao, X.-J., Wang, W., Garcia, B. A., & Witze, E. S. (2016) · Molecular Cell · doi:10.1016/j.molcel.2016.04.003 · Cited by 225 · see citing works
Overexpression of fatty acid synthase gene activates HER1/HER2 tyrosine kinase receptors in human breast epithelial cells
Vázquez-Martín, A., Colomer, R., Brunet, J., Lupu, R., & Menendez, J. A. (2008) · Cell Proliferation · doi:10.1111/j.1365-2184.2007.00498.x · Cited by 216 · see citing works
Inhibition of fatty acid synthase attenuates CD44-associated signaling and reduces metastasis in colorectal cancer
Zaytseva, Y. Y., Rychahou, P. G., Gulhati, P., Elliott, V. A., Mustain, W. C., O'Connor, K., Morris, A. J., Sunkara, M., Weiss, H. L., Lee, E. Y., et al. (2012) · Cancer Research · doi:10.1158/0008-5472.can-11-4057 · Cited by 208 · see citing works
Non‐small cell lung cancer is characterized by dramatic changes in phospholipid profiles
Marien, E., Meister, M. A., Muley, T., Fieuws, S., Bordel, S., Derua, R., Spraggins, J. M., de Plas, R. V., Dehairs, J., Wouters, J., et al. (2015) · International Journal of Cancer · doi:10.1002/ijc.29517 · Cited by 193 · see citing works
Overexpression of fatty acid synthase is associated with palmitoylation of Wnt1 and cytoplasmic stabilization of β-catenin in prostate cancer
Fiorentino, M., Zadra, G., Palescandolo, E., Fedele, G., Bailey, D., Fiore, C., Nguyen, P. L., Migita, T., Zamponi, R., Vizio, D. D., et al. (2008) · Laboratory Investigation · doi:10.1038/labinvest.2008.97 · Cited by 136 · see citing works
Fatty Acid Synthase Polymorphisms, Tumor Expression, Body Mass Index, Prostate Cancer Risk, and Survival
Nguyen, P. L., Ma, J., Chavarro, J. E., Freedman, M. L., Lis, R. T., Fedele, G., Fiore, C., Qiu, W., Fiorentino, M., Finn, S. P., et al. (2010) · Journal of Clinical Oncology · doi:10.1200/jco.2009.27.0793 · Cited by 130 · see citing works
Fatty acid synthase gene overexpression and copy number gain in prostate adenocarcinoma☆
SHAH, U., Dhir, R., Gollin, S. M., Chandran, U. R., Lewis, D. A., Acquafondata, M. B., & Pflug, B. R. (2006) · Human Pathology · doi:10.1016/j.humpath.2005.11.022 · Cited by 126 · see citing works
Co-activation of AKT and c-Met triggers rapid hepatocellular carcinoma development via the mTORC1/FASN pathway in mice
Hu, J., Che, L., Li, L., Pilo, M. G., Cigliano, A., Ribback, S., Li, X., Latte, G., Mela, M., Evert, M., et al. (2016) · Scientific Reports · doi:10.1038/srep20484 · Cited by 123 · see citing works
Palmitoylation of the EGFR Ligand Spitz by Rasp Increases Spitz Activity by Restricting Its Diffusion
Miura, G. I., Buglino, J. A., Alvarado, D., Lemmon, M. A., Resh, M. D., & Treisman, J. E. (2006) · Developmental Cell · doi:10.1016/j.devcel.2005.11.017 · Cited by 120 · see citing works
Cancer Cells Differentially Activate and Thrive on De Novo Lipid Synthesis Pathways in a Low-Lipid Environment
Daniëls, V. W., Smans, K. A., Royaux, I. E., Chypre, M., Swinnen, J. V., & Zaidi, N. (2014) · PLoS ONE · doi:10.1371/journal.pone.0106913 · Cited by 119 · see citing works
Fatty acid metabolism in breast cancer cells: differential inhibitory effects of epigallocatechin gallate (EGCG) and C75
Puig, T., Vázquez‐Martín, A., Relat, J., Pétriz, J., Menéndez, J. A., Porta, R., Casals, G., Marrero, P. F., Haro, D., Brunet, J., et al. (2007) · Breast Cancer Research and Treatment · doi:10.1007/s10549-007-9678-5 · Cited by 117 · see citing works
Protein S-palmitoylation and cancer
Yeste‐Velasco, M., Linder, M. E., & Lu, Y. (2015) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2015.06.004 · Cited by 100 · see citing works
A novel inhibitor of fatty acid synthase shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines
Puig, T., Aguilar, H., Cufí, S., Oliveras, G., Turrado, C., Ortega‐Gutiérrez, S., Benhamú, B., López-Rodríguez, M. L., Urruticoechea, A., & Colomer, R. (2011) · Breast Cancer Research · doi:10.1186/bcr3077 · Cited by 98 · see citing works
Novel Inhibitors of Fatty Acid Synthase with Anticancer Activity
Puig, T., Turrado, C., Benhamú, B., Aguilar, H., Relat, J., Ortega‐Gutiérrez, S., Casals, G., Marrero, P. F., Urruticoechea, A., Haro, D., et al. (2009) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-09-0856 · Cited by 95 · see citing works
Antitumor effect of orlistat, a fatty acid synthase inhibitor, is via activation of caspase-3 on human colorectal carcinoma-bearing animal
Chuang, H., Chang, Y.-F., & Hwang, J. (2011) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2011.02.016 · Cited by 83 · see citing works
Posttranslational modification of tubulin by palmitoylation: I. In vivo and cell-free studies.
Caron, J. M. (1997) · Molecular Biology of the Cell · doi:10.1091/mbc.8.4.621 · Cited by 83 · see citing works
Inhibition of Tumor-associated Fatty Acid Synthase Hyperactivity Induces Synergistic Chemosensitization of HER-2/neu-Overexpressing Human Breast Cancer Cells to Docetaxel (taxotere)
Menéndez, J. A., Lupu, R., & Colomer, R. (2004) · Breast Cancer Research and Treatment · doi:10.1023/b:brea.0000018409.59448.60 · Cited by 82 · see citing works
Up-regulation of USP2a and FASN in gliomas correlates strongly with glioma grade
Tao, B., He, H., Shi, X., Wang, C., Li, W., Li, B., Dong, Y., Hu, G., Hou, L., Luo, C., et al. (2013) · Journal of Clinical Neuroscience · doi:10.1016/j.jocn.2012.03.050 · Cited by 79 · see citing works
Expression of Fatty Acid Synthase Depends on NAC1 and Is Associated with Recurrent Ovarian Serous Carcinomas
Ueda, S. M., Yap, K. L., Davidson, B., Tian, Y., Murthy, V. K., Wang, T., Visvanathan, K., Kuhajda, F. P., Bristow, R. E., Zhang, H., et al. (2010) · Journal of Oncology · doi:10.1155/2010/285191 · Cited by 78 · see citing works
Blockade of Fatty Acid Synthase Induces Ubiquitination and Degradation of Phosphoinositide-3-Kinase Signaling Proteins in Ovarian Cancer
Tomek, K., Wagner, R., Varga, F., Singer, C. F., Karlic, H., & Grunt, T. W. (2011) · Molecular Cancer Research · doi:10.1158/1541-7786.mcr-10-0467 · Cited by 74 · see citing works
Co-expression of fatty acid synthase and caveolin-1 in pancreatic ductal adenocarcinoma: Implications for tumor progression and clinical outcome
Witkiewicz, A. K., Nguyen, K., Dasgupta, A., Kennedy, E. P., Yeo, C. J., Lisanti, M. P., & Brody, J. R. (2008) · Cell Cycle · doi:10.4161/cc.7.19.6719 · Cited by 71 · see citing works
Intracellular activation of EGFR by fatty acid synthase dependent palmitoylation
Bollu, L. R., Katreddy, R. R., Blessing, A. M., Pham, N., Zheng, B., Wu, X., & Weihua, Z. (2015) · Oncotarget · doi:10.18632/oncotarget.5252 · Cited by 71 · see citing works
Inhibition of fatty acid synthase by luteolin post-transcriptionally down-regulates c-Met expression independent of proteosomal/lysosomal degradation
Coleman, D. T., Bigelow, R. L. H., & Cardelli, J. A. (2009) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-08-0722 · Cited by 69 · see citing works
The role of palmitoylation in regulating Ras localization and function
Eisenberg, S., Laude, A., Beckett, A. J., Mageean, C. J., Aran, V., Hernandez-Valladares, M., Henis, Y. I., & Prior, I. A. (2013) · Biochemical Society Transactions · doi:10.1042/bst20120268 · Cited by 64 · see citing works
Inhibition of Fatty Acid Synthase Suppresses c-Met Receptor Kinase and Induces Apoptosis in Diffuse Large B-Cell Lymphoma
Shahab Uddin, M. S., Hussain, A. R., Ahmed, M., Bu, R., Ahmed, S. O., Ajarim, D. S., Al‐Dayel, F., Bavi, P. P., & Al-Kuraya, K. S. (2010) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-09-1061 · Cited by 58 · see citing works
Posttranslational modification of tubulin by palmitoylation: II. Identification of sites of palmitoylation.
Ozols, J., & Caron, J. M. (1997) · Molecular Biology of the Cell · doi:10.1091/mbc.8.4.637 · Cited by 55 · see citing works
Suppression of endogenous lipogenesis induces reversion of the malignant phenotype and normalized differentiation in breast cancer
González-Guerrico, A. M., Espinoza, I. C., Schroeder, B., Park, C. H., Chandra Mohan, K. V. P., Khurana, A., Corominas-Faja, B., Cuyàs, E., Alarcón, T., Kleer, C. G., et al. (2016) · Oncotarget · doi:10.18632/oncotarget.9463 · Cited by 48 · see citing works
Preliminary activity in the first in human study of the first-in-class fatty acid synthase (FASN) inhibitor, TVB-2640.
Dean, E. J., Falchook, G. S., Patel, M. R., Brenner, A. J., Infante, J. R., Arkenau, H., Borazanci, E. H., Lopez, J. S., Pant, S., Schmid, P., et al. (2016) · Journal of Clinical Oncology · doi:10.1200/jco.2016.34.15_suppl.2512 · Cited by 45 · see citing works
Self-citation
Serum Levels of Fatty Acid Synthase in Colorectal Cancer Patients Are Associated with Tumor Stage
Notarnicola, M., Tutino, V., Calvani, M., Lorusso, D., Guerra, V., & Caruso, M. G. (2011) · Journal of Gastrointestinal Cancer · doi:10.1007/s12029-011-9300-2 · Cited by 44 · see citing works
Single Site α-Tubulin Mutation Affects Astral Microtubules and Nuclear Positioning during Anaphase inSaccharomyces cerevisiae: Possible Role for Palmitoylation of α-Tubulin
Caron, J. M., Vega, L. R., Fleming, J., Bishop, R., & Solomon, F. (2001) · Molecular Biology of the Cell · doi:10.1091/mbc.12.9.2672 · Cited by 43 · see citing works
Palmitoylation of Tubulin
Zambito, A. M., & Wolff, J. (1997) · Biochemical and Biophysical Research Communications · doi:10.1006/bbrc.1997.7525 · Cited by 34 · see citing works
Nutrient-dependent phosphorylation channels lipid synthesis to regulate PPARα
Jensen-Urstad, A. P. L., Song, H., Lodhi, I. J., Funai, K., Yin, L., Coleman, T., & Semenkovich, C. F. (2013) · Journal of Lipid Research · doi:10.1194/jlr.m036103 · Cited by 31 · see citing works
Ras palmitoylation is necessary for N-Ras activation and signal propagation in growth factor signalling
Song, S.-P., Hennig, A., Schubert, K., Markwart, R., Schmidt, P., Prior, I. A., Böhmer, F.-D., & Rubio, I. (2013) · Biochemical Journal · doi:10.1042/bj20121799 · Cited by 27 · see citing works
Tissue microarray analysis of FAS, Bcl-2, Bcl-x, ER, PgR, Hsp60, p53 and Her2-neu in breast carcinoma.
Sebastiani, V., Botti, C., Tondo, U. D., Visca, P., Pizzuti, L., Santeusanio, G., & Alò, P. L. (2006) · PubMed · Cited by 24 · see citing works
Vinblastine, a Chemotherapeutic Drug, Inhibits Palmitoylation of Tubulin in Human Leukemic Lymphocytes
Caron, J. M., & Herwood, M. (2007) · Chemotherapy · doi:10.1159/000098419 · Cited by 22 · see citing works
You Lose Some, You Win Some: Weight Loss Induces Microbiota and Metabolite Shifts
Bik, E. M. (2015) · EBioMedicine · doi:10.1016/j.ebiom.2015.07.037 · Cited by 14 · see citing works
Abstract 801: Sensitivity of cell lines to Fatty Acid Synthase inhibitors depends on the lipid content in the cellular environment
Smans, K. A., Breucker, S. D., Esser, N., Fraiponts, E., Gilissen, R., Graeser, R., Janssen, B., Meerpoel, L., Peeters, D. C. G., Hecke, G. V., et al. (2014) · Cancer Research · doi:10.1158/1538-7445.am2014-801 · Cited by 2 · see citing works

Flagged first, then by citations

1 of the 53 references couldn’t be matched to a known paper.

Sorted by citations

Targeting cancer metabolism in the era of precision oncology
Stine, Z. E., Schug, Z. T., Salvino, J. M., & Dang, C. V. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00339-6 · Cited by 1,189 · see citing works
Targeting Metabolism for Cancer Therapy
Luengo, A., Gui, D. Y., & Vander Heiden, M. G. (2017) · Cell Chemical Biology · doi:10.1016/j.chembiol.2017.08.028 · Cited by 971 · see citing works
Lipid metabolism in cancer: New perspectives and emerging mechanisms
Broadfield, L. A., Pane, A. A., Talebi, A., Swinnen, J. V., & Fendt, S. (2021) · Developmental Cell · doi:10.1016/j.devcel.2021.04.013 · Cited by 765 · see citing works
Lipids and cancer: Emerging roles in pathogenesis, diagnosis and therapeutic intervention
Butler, L. M., Perone, Y., Dehairs, J., Lupien, L. E., de Laat, V., Talebi, A., Loda, M. F., Kinlaw, W. B., & Swinnen, J. V. (2020) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2020.07.013 · Cited by 617 · see citing works
Metabolic reprogramming in clear cell renal cell carcinoma
Wettersten, H. I., Aboud, O. A., Lara, P. N., & Weiss, R. H. (2017) · Nature Reviews Nephrology · doi:10.1038/nrneph.2017.59 · Cited by 573 · see citing works
Lipid metabolic reprogramming in tumor microenvironment: from mechanisms to therapeutics
Jin, H.-R., Wang, J., Wang, Z., Xi, M., Xia, B., Deng, K., & Yang, J. (2023) · Journal of Hematology & Oncology · doi:10.1186/s13045-023-01498-2 · Cited by 509 · see citing works
First-in-human study of the safety, pharmacokinetics, and pharmacodynamics of first-in-class fatty acid synthase inhibitor TVB-2640 alone and with a taxane in advanced tumors
Falchook, G. S., Infante, J. R., Arkenau, H., Patel, M. R., Dean, E. J., Borazanci, E. H., Brenner, A. J., Cook, N., Lopez, J., Pant, S., et al. (2021) · EClinicalMedicine · doi:10.1016/j.eclinm.2021.100797 · Cited by 302 · see citing works
Self-citation
Inhibition of de novo lipogenesis targets androgen receptor signaling in castration-resistant prostate cancer
Zadra, G., Ribeiro, C. F., Chetta, P., Ho, Y., Cacciatore, S., Gao, X., Syamala, S., Bango, C., Photopoulos, C., Huang, Y., et al. (2018) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1808834116 · Cited by 298 · see citing works
Metabolic reprogramming in renal cancer: Events of a metabolic disease
Chakraborty, S., Balan, M., Sabarwal, A., Choueiri, T. K., & Pal, S. (2021) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2021.188559 · Cited by 208 · see citing works
Fatty acid synthase – Modern tumor cell biology insights into a classical oncology target
BUCKLEY, D. I., Duke, G. M., Heuer, T. S., O’Farrell, M., Wagman, A. S., McCulloch, W. F., & Kemble, G. W. (2017) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2017.02.021 · Cited by 197 · see citing works
Self-citation
Fat and Furious: Lipid Metabolism in Antitumoral Therapy Response and Resistance
Bacci, M., Lorito, N., Smiriglia, A., & Morandi, A. (2020) · Trends in cancer · doi:10.1016/j.trecan.2020.10.004 · Cited by 194 · see citing works
Protein palmitoylation in cancer: molecular functions and therapeutic potential
Zhou, B., Hao, Q., Liang, Y., & Kong, E. (2022) · Molecular Oncology · doi:10.1002/1878-0261.13308 · Cited by 185 · see citing works
Clinical development of metabolic inhibitors for oncology
Lemberg, K. M., Gori, S. S., Tsukamoto, T., Rais, R., & Slusher, B. S. (2022) · Journal of Clinical Investigation · doi:10.1172/jci148550 · Cited by 142 · see citing works
Orlistat as a FASN inhibitor and multitargeted agent for cancer therapy
Schcolnik‐Cabrera, A., Chávez-Blanco, A. D., Domínguez-Gómez, G., Taja‐Chayeb, L., Morales‐Bárcenas, R., Trejo‐Becerril, C., Pérez‐Cárdenas, E., González‐Fierro, A., & Dueñas‐González, A. (2018) · Expert Opinion on Investigational Drugs · doi:10.1080/13543784.2018.1471132 · Cited by 141 · see citing works
Preclinical evaluation of novel fatty acid synthase inhibitors in primary colorectal cancer cells and a patient-derived xenograft model of colorectal cancer
Zaytseva, Y. Y., Rychahou, P. G., Le, A.-T., Scott, T. L., Flight, R. M., Kim, J. T., Harris, J., Liu, J., Wang, C., Morris, A. J., et al. (2018) · Oncotarget · doi:10.18632/oncotarget.25361 · Cited by 123 · see citing works
Self-citation
Therapeutic efficacy of FASN inhibition in preclinical models of HCC
Wang, H., Zhou, Y., Xu, H., Wang, X., Zhang, Y., Shang, R., O’Farrell, M., Roessler, S. K., Sticht, C., Stahl, A., et al. (2022) · Hepatology · doi:10.1002/hep.32359 · Cited by 120 · see citing works
HOXB13 suppresses de novo lipogenesis through HDAC3-mediated epigenetic reprogramming in prostate cancer
Lü, X., Fong, K.-W., Gritsina, G., Wang, F., Baca, S. C., Brea, L. T., Berchuck, J. E., Spisák, S., Ross, J., Morrissey, C. M., et al. (2022) · Nature Genetics · doi:10.1038/s41588-022-01045-8 · Cited by 114 · see citing works
Inhibition of Fatty Acid Synthase Upregulates Expression of CD36 to Sustain Proliferation of Colorectal Cancer Cells
Drury, J., Rychahou, P. G., He, D., Jafari, N., Wang, C., Lee, E. Y., Weiss, H. L., Evers, B. M., & Zaytseva, Y. Y. (2020) · Frontiers in Oncology · doi:10.3389/fonc.2020.01185 · Cited by 111 · see citing works
Lipid-induced S-palmitoylation as a Vital Regulator of Cell Signaling and Disease Development
Qu, M., Zhou, X., Wang, X., & Li, H. (2021) · International Journal of Biological Sciences · doi:10.7150/ijbs.64046 · Cited by 110 · see citing works
FASN inhibition targets multiple drivers of NASH by reducing steatosis, inflammation and fibrosis in preclinical models
O’Farrell, M., Duke, G. M., Crowley, R., BUCKLEY, D. I., Martins, E. B., Bhattacharya, D., Friedman, S. L., & Kemble, G. W. (2022) · Scientific Reports · doi:10.1038/s41598-022-19459-z · Cited by 104 · see citing works
Self-citation
Combinatorial strategies to target RAS-driven cancers
Perurena, N., Situ, L., & Cichowski, K. M. (2024) · Nature reviews. Cancer · doi:10.1038/s41568-024-00679-6 · Cited by 104 · see citing works
Fatty acid synthase (FASN) regulates the mitochondrial priming of cancer cells
Schroeder, B., Steen, T. V., Espinoza, I. C., Venkatapoorna, C. M. K., Hu, Z., Martín, F., Regan, K. M., Cuyàs, E., Meng, X. W., Verdura, S., et al. (2021) · Cell Death and Disease · doi:10.1038/s41419-021-04262-x · Cited by 100 · see citing works
Self-citation
Down‐regulation of PKM2 decreases FASN expression in bladder cancer cells through AKT/mTOR/SREBP‐1c axis
Tao, T., Su, Q., Xu, S., Deng, J., Zhou, S., Yu, Z., Huang, Y., He, C., He, S., Peng, M., et al. (2018) · Journal of Cellular Physiology · doi:10.1002/jcp.27129 · Cited by 95 · see citing works
The Heterogeneity of Lipid Metabolism in Cancer
Park, J. K., Coffey, N. J., Limoges, A., & Le, A. (2018) · Advances in experimental medicine and biology · doi:10.1007/978-3-319-77736-8_3 · Cited by 79 · see citing works
Pathogenetic, Prognostic, and Therapeutic Role of Fatty Acid Synthase in Human Hepatocellular Carcinoma
Che, L., Paliogiannis, P., Cigliano, A., Pilo, M. G., Chen, X., & Calvisi, D. F. (2019) · Frontiers in Oncology · doi:10.3389/fonc.2019.01412 · Cited by 76 · see citing works
Diverse Roles of Protein Palmitoylation in Cancer Progression, Immunity, Stemness, and Beyond
Li, M., Zhang, L., & Chen, C.-W. D. (2023) · Cells · doi:10.3390/cells12182209 · Cited by 73 · see citing works
Selective Enrichment and Direct Analysis of Protein S-Palmitoylation Sites
Thinon, E., Fernandez, J., Molina, H., & Hang, H. C. (2018) · Journal of Proteome Research · doi:10.1021/acs.jproteome.8b00002 · Cited by 74 · see citing works
De Novo Fatty Acid Synthesis-Driven Sphingolipid Metabolism Promotes Metastatic Potential of Colorectal Cancer
Jafari, N., Drury, J., Morris, A. J., Onono, F. O., Stevens, P. D., Gao, T., Liu, J., Wang, C., Lee, E. Y., Weiss, H. L., et al. (2018) · Molecular Cancer Research · doi:10.1158/1541-7786.mcr-18-0199 · Cited by 66 · see citing works
Implications of lipid droplets in lung cancer: Associations with drug resistance (Review)
Jin, C., & Yuan, P. (2020) · Oncology Letters · doi:10.3892/ol.2020.11769 · Cited by 62 · see citing works
Too complex to fail? Targeting fatty acid metabolism for cancer therapy
Munir, R., Lisec, J., Swinnen, J. V., & Zaidi, N. (2021) · Progress in Lipid Research · doi:10.1016/j.plipres.2021.101143 · Cited by 62 · see citing works
The role of lipid metabolism in tumor immune microenvironment and potential therapeutic strategies
Wang, D., Ye, Q., Gu, H., & Chen, Z. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2022.984560 · Cited by 62 · see citing works
Metabolic dependencies and targets in ovarian cancer
Zhang, Y., Wang, Y., Zhao, G., Oršulić, S., & Matei, D. E. (2023) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2023.108413 · Cited by 59 · see citing works
Targeting lipid metabolism for ferroptotic cancer therapy
Luo, M., Yan, J., Hu, X., Li, H., Li, H., Liu, Q., Chen, Y., & Zou, Z. (2022) · APOPTOSIS · doi:10.1007/s10495-022-01795-0 · Cited by 57 · see citing works
Nanovesicles for Lipid Metabolism Reprogram-Enhanced Ferroptosis and Magnetotherapy of Refractory Tumors and Inhibiting Metastasis with Activated Innate Immunity
Cheng, X.-Q., Xu, J., Cui, Y., Liu, J., Chen, Y., He, C., Cui, L., Liu, Y., Song, B., Gong, C., et al. (2025) · ACS Nano · doi:10.1021/acsnano.4c16981 · Cited by 53 · see citing works
Targeting Cell Metabolism as Cancer Therapy
Ngoi, N. Y. L., Eu, J. Q., Hirpara, J. L., Wang, L., Lim, J. S. J., Lee, S. C., Lim, Y., Pervaiz, S., Goh, B. C., & Wong, A. L. A. (2019) · Antioxidants and Redox Signaling · doi:10.1089/ars.2019.7947 · Cited by 51 · see citing works
Cytotoxicity and Radiosensitizing Activity of the Fatty Acid Synthase Inhibitor C75 Is Enhanced by Blocking Fatty Acid Uptake in Prostate Cancer Cells
Rae, C. J., Fragkoulis, G. I., & Chalmers, A. J. (2020) · Advances in Radiation Oncology · doi:10.1016/j.adro.2020.06.022 · Cited by 46 · see citing works
Theoretical framework and emerging challenges of lipid metabolism in cancer
Gu, Q., Wang, Y., Yi, P., & Cheng, C. (2024) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2024.12.002 · Cited by 45 · see citing works
Combination Treatment with Orlistat-Containing Nanoparticles and Taxanes Is Synergistic and Enhances Microtubule Stability in Taxane-Resistant Prostate Cancer Cells
Souchek, J. J., Davis, A. L., Hill, T. K., Holmes, M. B., Qi, B., Singh, P. K., Kridel, S. J., & Mohs, A. M. (2017) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-17-0013 · Cited by 45 · see citing works
FASN inhibition as a potential treatment for endocrine-resistant breast cancer
Gruslova, A., McClellan, B., Balinda, H. U., Viswanadhapalli, S., Alers, V. A., Sareddy, G. R., Huang, T. H. ‐., Garcia, M., deGraffenried, L. A., Vadlamudi, R. K., et al. (2021) · Breast Cancer Research and Treatment · doi:10.1007/s10549-021-06231-6 · Cited by 45 · see citing works
Metabolomics at the tumor microenvironment interface: Decoding cellular conversations
Berrell, N., Sadeghirad, H., Blick, T., Bidgood, C. L., Leggatt, G. R., O'Byrne, K. J., & Kulasinghe, A. (2023) · Medicinal Research Reviews · doi:10.1002/med.22010 · Cited by 42 · see citing works
Fatty Acid Synthase Confers Tamoxifen Resistance to ER+/HER2+ Breast Cancer
Menéndez, J. A., Papadimitropoulou, A., Steen, T. V., Cuyàs, E., Oza-Gajera, B. P., Verdura, S., Espinoza, I. C., Vellón, L., Mehmi, I., & Lupu, R. (2021) · Cancers · doi:10.3390/cancers13051132 · Cited by 41 · see citing works
Anticancer properties of the fatty acid synthase inhibitor TVB-3166 on oral squamous cell carcinoma cell lines
Aquino, I. G., Bastos, D. C., Zelaya, F. J. M. C., Teixeira, I. F., Salo, T. A., Coletta, R. D., & Graner, E. (2020) · Archives of Oral Biology · doi:10.1016/j.archoralbio.2020.104707 · Cited by 38 · see citing works
Lipid droplet turnover at the lysosome inhibits growth of hepatocellular carcinoma in a BNIP3-dependent manner
Berardi, D. E., Bock-Hughes, A., Terry, A. R., Drake, L. E., Bozek, G., & Macleod, K. F. (2022) · Science Advances · doi:10.1126/sciadv.abo2510 · Cited by 37 · see citing works
In Vivo Effectiveness of Orlistat in the Suppression of Human Colorectal Cancer Cell Proliferation
Czumaj, A., Zabielska, J., Pakiet, A., Mika, A., Rostkowska, O. M., Makarewicz, W., Kobiela, J., Śledziński, T., & Stelmańska, E. (2019) · Anticancer Research · doi:10.21873/anticanres.13531 · Cited by 37 · see citing works
The Heterogeneity of Lipid Metabolism in Cancer
Park, J. K., Coffey, N. J., Limoges, A., & Le, A. (2021) · Advances in experimental medicine and biology · doi:10.1007/978-3-030-65768-0_3 · Cited by 37 · see citing works
Fatty acid synthase: a druggable driver of breast cancer brain metastasis
Menéndez, J. A., & Lupu, R. (2022) · Expert Opinion on Therapeutic Targets · doi:10.1080/14728222.2022.2077189 · Cited by 37 · see citing works
Fatty acids in cancer chemoresistance
Qin, J., Ye, L., Wen, X., Zhang, X., Di, Y., Chen, Z., & Wang, Z. (2023) · Cancer Letters · doi:10.1016/j.canlet.2023.216352 · Cited by 36 · see citing works
Acetone immersion enhanced MALDI-MS imaging of small molecule metabolites in biological tissues
Sun, C., Li, Z., Ma, C., Zang, Q., Li, J., Liu, W., Zhao, H., & Wang, X. (2019) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2019.112797 · Cited by 35 · see citing works
Predicting and Overcoming Taxane Chemoresistance
Rodrigues, S., Moindjie, H., Haykal, M. M., & Nahmias, C. (2020) · Trends in Molecular Medicine · doi:10.1016/j.molmed.2020.09.007 · Cited by 35 · see citing works
Orlistat Displays Antitumor Activity and Enhances the Efficacy of Paclitaxel in Human Hepatoma Hep3B Cells
You, B., Chen, L., Hsu, P.-H., Sung, P.-H., Hung, Y.-C., & Lee, H. (2019) · Chemical Research in Toxicology · doi:10.1021/acs.chemrestox.8b00269 · Cited by 33 · see citing works
Anoikis resistance in Cancer: Mechanisms, therapeutic strategies, potential targets, and models for enhanced understanding
Shaw, P., Bhowmik, A. D., Pillai, M. S. G., Robbins, N., Dwivedi, S. K. D., & Rao, G. (2025) · Cancer Letters · doi:10.1016/j.canlet.2025.217750 · Cited by 33 · see citing works
Fatty acid synthase inhibitor orlistat impairs cell growth and down-regulates PD-L1 expression of a human T-cell leukemia line
Cioccoloni, G., Aquino, A., Notarnicola, M., Caruso, M. G., Bonmassar, E., Zonfrillo, M., Caporali, S., Faraoni, I., Villivà, C., Fuggetta, M. P., et al. (2019) · Journal of Chemotherapy · doi:10.1080/1120009x.2019.1694761 · Cited by 32 · see citing works
Fatty acid synthase ( FASN ) signalome: A molecular guide for precision oncology
Menéndez, J. A., Cuyàs, E., Encinar, J. A., Steen, T. V., Verdura, S., Llop‐Hernández, À., López, J., Serrano‐Hervás, E., Osuna, S., Martı́n-Castillo, B., et al. (2023) · Molecular Oncology · doi:10.1002/1878-0261.13582 · Cited by 35 · see citing works
Genetic ablation of FASN attenuates the invasive potential of prostate cancer driven by Pten loss
Bastos, D. C., Ribeiro, C. F., Ahearn, T. U., Nascimento, J., Pakula, H., Clohessy, J. G., Mucci, L. A., Roberts, T. M., Zanata, S. M., Zadra, G., et al. (2020) · The Journal of Pathology · doi:10.1002/path.5587 · Cited by 31 · see citing works
Global Metabolomic and Lipidomic Analysis Reveal the Synergistic Effect of Bufalin in Combination with Cinobufagin against HepG2 Cells
Zhang, J., Hong, Y., Jiang, L.-L., Yi, X., Yang, C., Liu, L., Chen, Z., Wu, Y., & Cai, Z. (2020) · Journal of Proteome Research · doi:10.1021/acs.jproteome.9b00681 · Cited by 29 · see citing works
Palmitoylation as a Signal for Delivery
Wang, Y., Lu, H., Fang, C., & Xu, J. (2020) · Advances in experimental medicine and biology · doi:10.1007/978-981-15-3266-5_16 · Cited by 28 · see citing works
An Inhibitor of Fatty Acid Synthase Thioesterase Domain with Improved Cytotoxicity against Breast Cancer Cells and Stability in Plasma
Lupien, L. E., Dunkley, E. M., Maloy, M. J., Lehner, I. B., Foisey, M. G., Ouellette, M. E., Lewis, L. D., Pooler, D. B., Kinlaw, W. B., & Baures, P. W. (2019) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.119.258947 · Cited by 27 · see citing works
Inhibiting de novo lipogenesis identifies a therapeutic vulnerability in therapy-resistant colorectal cancer
Jog, E., Jainarayanan, A., Ferlita, A. L., Chakraborty, A., Dalwai, A., Yahya, S., Shivashankar, A., Choudhary, B. S., Chandramouli, A., Kazi, M. K., et al. (2024) · Redox Biology · doi:10.1016/j.redox.2024.103458 · Cited by 26 · see citing works
Personalized Medicine for Prostate Cancer: Is Targeting Metabolism a Reality?
Fidelito, G., Watt, M. J., & Taylor, R. A. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2021.778761 · Cited by 27 · see citing works
Metabolic reprogramming based on RNA sequencing of gemcitabine-resistant cells reveals the FASN gene as a therapeutic for bladder cancer
Zhou, L., Du, K., Dai, Y., Zeng, Y., Luo, Y., Ren, M., Pan, W., Liu, Y., Zhang, L., Zhu, R., et al. (2024) · Journal of Translational Medicine · doi:10.1186/s12967-024-04867-8 · Cited by 24 · see citing works
Metabolic Reprogramming of Cancer Cells and Therapeutics Targeting Cancer Metabolism
Punnasseril, J. M. J., Auwal, A., Gopalan, V., Lam, A. K.-Y., & Islam, F. (2025) · Cancer Medicine · doi:10.1002/cam4.71244 · Cited by 27 · see citing works
FASN inhibitor TVB-3166 prevents S-acylation of the spike protein of human coronaviruses
Mekhail, K., Lee, M., Sugiyama, M. G., Astori, A., St‐Germain, J. R., Latreille, E., Khosraviani, N., Wei, K., Li, Z., Rini, J. M., et al. (2022) · Journal of Lipid Research · doi:10.1016/j.jlr.2022.100256 · Cited by 25 · see citing works
Fatty acid metabolism: A new therapeutic target for cervical cancer
Ping, P., Li, J., Lei, H., & Xu, X. (2023) · Frontiers in Oncology · doi:10.3389/fonc.2023.1111778 · Cited by 28 · see citing works
Pharmacological induction of membrane lipid poly-unsaturation sensitizes melanoma to ROS inducers and overcomes acquired resistance to targeted therapy
Talebi, A., de Laat, V., Spotbeen, X., Dehairs, J., Rambow, F., Rogiers, A., Vanderhoydonc, F., Rizzotto, L., Planque, M., Doglioni, G., et al. (2023) · Journal of Experimental & Clinical Cancer Research · doi:10.1186/s13046-023-02664-7 · Cited by 22 · see citing works
Self-citation
FASN inhibition sensitizes metastatic OSCC cells to cisplatin and paclitaxel by downregulating cyclin B1
Almeida, L. Y., MOREIRA, F. D. S., dos Santos, G. A., Zelaya, F. J. M. C., Rojas, C. A. O., Agostini, M., Mariano, F. S., Bastos, D. C., Nicolau, U. R., Kowalski, L. P., et al. (2021) · Oral Diseases · doi:10.1111/odi.14017 · Cited by 21 · see citing works
Targeting ELOVL6 to disrupt c-MYC driven lipid metabolism in pancreatic cancer enhances chemosensitivity
García, A. G., Aporta, M. F., Vallejo-Palma, G., Trujillo, A. G., Castillo‐González, R., Lozano, D. C., Perdiguero, A. M., Velasco, R. M., Castro, M. C., Benito, E. D. S., et al. (2025) · Nature Communications · doi:10.1038/s41467-025-56894-8 · Cited by 20 · see citing works
The role of cancer cell bioenergetics in dormancy and drug resistance
Tau, S. S., & Miller, T. W. (2023) · Cancer and Metastasis Reviews · doi:10.1007/s10555-023-10081-7 · Cited by 20 · see citing works
PSMA-targeted combination brusatol and docetaxel nanotherapeutics for the treatment of prostate cancer
Adekiya, T. A., Hudson, T., Bakare, O., Ameyaw, E. E., Adebayo, A. S., Olajubutu, O., & Adesina, S. K. (2024) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2024.117125 · Cited by 19 · see citing works
The anti-diabetic PPARγ agonist Pioglitazone inhibits cell proliferation and induces metabolic reprogramming in prostate cancer
Atas, E., Berchtold, K., Schlederer, M., Prodinger, S., Sternberg, F., Pucci, P., Steel, C., Matthews, J. D., James, E. R., Philippe, C., et al. (2025) · Molecular Cancer · doi:10.1186/s12943-025-02320-y · Cited by 18 · see citing works
Exploiting metabolic vulnerabilities in cancer: From mechanisms to therapeutic opportunities
Xue, Z.-R., Xin, Y.-Y., & Jin, W. (2025) · Cancer Letters · doi:10.1016/j.canlet.2025.218067 · Cited by 19 · see citing works
Altered lipid metabolism in APC-driven colorectal cancer: the potential for therapeutic intervention
Kelson, C. O., & Zaytseva, Y. Y. (2024) · Frontiers in Oncology · doi:10.3389/fonc.2024.1343061 · Cited by 18 · see citing works
Atorvastatin improves cisplatin sensitivity through modulation of cholesteryl ester homeostasis in breast cancer cells
dos Santos, D. Z., Guimarães, I. D. S., Hakeem-Sanni, M. F., Cochran, B. J., Rye, K., Grewal, T., Hoy, A. J., & Rangel, L. B. A. (2022) · Discover Oncology · doi:10.1007/s12672-022-00598-8 · Cited by 17 · see citing works
Metabolic heterogeneity in tumor microenvironment – A novel landmark for immunotherapy
Chen, C., Han, P., & Qing, Y. (2024) · Autoimmunity Reviews · doi:10.1016/j.autrev.2024.103579 · Cited by 17 · see citing works
The antimetastatic activity of orlistat is accompanied by an antitumoral immune response in mouse melanoma
Almeida, L. Y., Mariano, F. S., Bastos, D. C., Cavassani, K. A., Raphelson, J. R., Mariano, V. S., Agostini, M., Moreira, F. S., Coletta, R. D., Mattos‐Graner, R. O., et al. (2019) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-019-04010-1 · Cited by 17 · see citing works
Cancer dormancy and metabolism: From molecular insights to translational opportunities
Wang, Y., Liu, L., Zhang, X., Liang, T., & Bai, X. (2025) · Cancer Letters · doi:10.1016/j.canlet.2025.218097 · Cited by 16 · see citing works
Fatty acid synthase (FASN) inhibition cooperates with BH3 mimetic drugs to overcome resistance to mitochondrial apoptosis in pancreatic cancer
Steen, T. V., Espinoza, I. C., Duran, C., Casadevall, G., Serrano‐Hervás, E., Cuyàs, E., Verdura, S., Kemble, G. W., Kaufmann, S. H., McWilliams, R. R., et al. (2025) · Neoplasia · doi:10.1016/j.neo.2025.101143 · Cited by 15 · see citing works
Self-citation
Palmitoylome profiling indicates that androgens regulate the palmitoylation of α‑tubulin in prostate cancer‑derived LNCaP cells and supernatants
Li, W., Zhang, J., Zou, L., Cui, J. T., Su, F., Jin, J., Xiao, F., Liu, M., & Zhao, G. (2019) · Oncology Reports · doi:10.3892/or.2019.7333 · Cited by 15 · see citing works
Association between different levels of lipid metabolism‑related enzymes and fatty acid synthase in Wilms' tumor
Wang, X., Du, G., Wu, Y., Zhang, Y., Guo, F., Liu, W., & Wu, R. (2019) · International Journal of Oncology · doi:10.3892/ijo.2019.4948 · Cited by 15 · see citing works
Inhibition of Aberrant Activated Fibroblast‐Like Synoviocytes in Rheumatoid Arthritis by Leishmania Peptide via the Regulation of Fatty Acid Synthesis Metabolism
Su, J., Fan, X., Zou, Y., Fu, G., Feng, S., Wang, X., Yu, Y., Li, L., Bian, Z., Huang, R., et al. (2025) · Advanced Science · doi:10.1002/advs.202409154 · Cited by 14 · see citing works
The Pharmacological or Genetic Blockade of Endogenous De Novo Fatty Acid Synthesis Does Not Increase the Uptake of Exogenous Lipids in Ovarian Cancer Cells
Grunt, T. W., Lemberger, L., Colomer, R., López-Rodríguez, M. L., & Wagner, R. (2021) · Frontiers in Oncology · doi:10.3389/fonc.2021.610885 · Cited by 14 · see citing works
Oncogenic Integration of Nucleotide Metabolism via Fatty Acid Synthase in Non-Hodgkin Lymphoma
Ravi, D., Beheshti, A., Abermil, N., Lansigan, F., Kinlaw, W. B., Matthan, N. R., Mokhtar, M., Passero, F. C., Puliti, P., David, K. A., et al. (2021) · Frontiers in Oncology · doi:10.3389/fonc.2021.725137 · Cited by 14 · see citing works
Activity-based protein profiling of human and plasmodium serine hydrolases and interrogation of potential antimalarial targets
Davison, D., Howell, S. A., Snijders, A. P., & Deu, E. (2022) · iScience · doi:10.1016/j.isci.2022.104996 · Cited by 14 · see citing works
Fatty Acid Synthase Inhibitors Enhance Microtubule-Stabilizing and Microtubule-Destabilizing Drugs in Taxane-Resistant Prostate Cancer Cells
Souchek, J. J., Laliwala, A., Houser, L. J., Muraskin, L., Vu, Q., & Mohs, A. M. (2023) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.3c00182 · Cited by 13 · see citing works
Targeting metabolic reprogramming to overcome drug resistance in advanced bladder cancer: insights from gemcitabine‐ and cisplatin‐resistant models
Kawahara, I., Yoshino, H., Fukumoto, W., Arima, J., Saito, S., Li, G., Fukuda, I., Mitsuke, A., Sakaguchi, T., Inoguchi, S., et al. (2024) · Molecular Oncology · doi:10.1002/1878-0261.13684 · Cited by 13 · see citing works
Role of Aberrant Lipid Metabolism of Cancer Stem Cells in Cancer Progression
Zhou, J., Zhao, J., & Su, C. (2021) · Current Cancer Drug Targets · doi:10.2174/1568009619666210316112333 · Cited by 13 · see citing works
Investigation of the effects of dichlorvos poisoning on AMPK signaling pathway in chicken brain tissues
Xiao, Y., Zheng, X., Li, G., Zhou, C., Wu, C., Xu, Z. Q., Hu, G., Guo, X., Li, L., Cao, H., et al. (2020) · Environmental Pollution · doi:10.1016/j.envpol.2020.114109 · Cited by 13 · see citing works
Lipid Metabolic Reprogramming in Embryonal Neoplasms with MYCN Amplification
Talapatra, J., & Reddy, M. M. (2023) · Cancers · doi:10.3390/cancers15072144 · Cited by 12 · see citing works
Imaging the metabolic reprograming of fatty acid synthesis pathway enables new diagnostic and therapeutic opportunity for breast cancer
Wang, F., Ma, S., Chen, P., Han, Y., Liu, Z., Wang, X., Sun, C., & Yu, Z. (2023) · Cancer Cell International · doi:10.1186/s12935-023-02908-8 · Cited by 12 · see citing works
Regulation of fatty acid synthase on tumor and progress in the development of related therapies
Bai, R., & Cui, J. (2024) · Chinese Medical Journal · doi:10.1097/cm9.0000000000002880 · Cited by 14 · see citing works
The role of novel protein acylations in cancer
Cao, D., Sun, W., Li, X., Jian, L., Zhou, X., Bode, A. M., & Luo, X. (2024) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2024.176841 · Cited by 14 · see citing works
The shadow of cancer therapeutic resistance: Unveiling the role of S-palmitoylation
Yang, X., Xu, M., Deng, Z., & Xu, B. (2025) · Drug Resistance Updates · doi:10.1016/j.drup.2025.101264 · Cited by 13 · see citing works
Druggable Metabolic Vulnerabilities Are Exposed and Masked during Progression to Castration Resistant Prostate Cancer
Choi, S. Y. C., Ribeiro, C. F., Wang, Y. Z., Loda, M. F., Plymate, S. R., & Uo, T. (2022) · Biomolecules · doi:10.3390/biom12111590 · Cited by 12 · see citing works
Upregulation of Fatty Acid Synthase Increases Activity of β-Catenin and Expression of NOTUM to Enhance Stem-like Properties of Colorectal Cancer Cells
Kelson, C. O., Tessmann, J. W., Geisen, M. E., He, D., Wang, C., Gao, T., Evers, B. M., & Zaytseva, Y. Y. (2024) · Cells · doi:10.3390/cells13191663 · Cited by 11 · see citing works
Adipocyte–Tumor Interactions in the Bone Marrow Niche: Implications for Metastasis and Therapy
Dabaliz, A., Hakawati, M. N. A., Alrashdan, N., Alrashdan, S., Bakir, M., & Mohammad, K. S. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms26199781 · Cited by 11 · see citing works
FASN contributes to the pathogenesis of lupus by promoting TLR-mediated activation of macrophages and dendritic cells
Xiao, Y., Gao, Y., Hu, Y., Zhang, X., Wang, L., Li, H., Lu, Y., Ma, Q., Dai, J., Ning, Z., et al. (2024) · International Immunopharmacology · doi:10.1016/j.intimp.2024.113136 · Cited by 10 · see citing works
Targeting Prostate Cancer Metabolism Through Transcriptional and Epigenetic Modulation: A Multi-Target Approach to Therapeutic Innovation
Espitia-Pérez, P., Espitia-Pérez, L., & Negrette-Guzmán, M. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms26136013 · Cited by 10 · see citing works
Targeting fatty acid synthase for cancer drug discovery: Retrospective analyses and outlook
Cui, Q., Josephraj, S., Gu, B., Liu, J., & Zhang, J. (2025) · Pharmacological Reviews · doi:10.1016/j.pharmr.2025.100105 · Cited by 9 · see citing works
When fat goes down, prostate cancer is on the ropes
Zadra, G., & Loda, M. F. (2019) · Molecular & Cellular Oncology · doi:10.1080/23723556.2019.1595308 · Cited by 9 · see citing works
Resistance mechanisms to taxanes and PARP inhibitors in advanced prostate cancer
Lombard, A. P., & Gao, A. C. (2020) · Current Opinion in Endocrine and Metabolic Research · doi:10.1016/j.coemr.2020.02.006 · Cited by 9 · see citing works
Pharmacological fatty acid synthase inhibitors differently affect the malignant phenotype of oral cancer cells.
Boelcke, W. P., Teixeira, I. F., Aquino, I. G., Mazzaro, A. R., Zelaya, F. J. M. C., de Souza, A. P., Salo, T. A., Coletta, R. D., Graner, E., & Bastos, D. C. (2021) · Archives of Oral Biology · doi:10.1016/j.archoralbio.2021.105343 · Cited by 9 · see citing works

Abstract 4743: Preclinical studies characterize tumor type sensitivity to FASN inhibition and the mechanism and efficacy of novel drug combinations with TVB-2640
Heuer, T. S., Ventura, R., Lai, J., Waszczuk, J., Rubio, C., Hammonds, R. G., Farrell, M. O., BUCKLEY, D. I., & Kemble, G. W. (2016) · Cancer Research · doi:10.1158/1538-7445.am2016-4743 · Cited by 3 · see citing works
Self-citation
Abstract 1815: Efficacy of FASN-selective small molecule inhibitors in preclinical tumor models
Heuer, T. S., Ventura, R., Waszczuk, J., Mordec, K., Lai, J., Johnson, R. J. K., Hu, L., Cai, H., Wagman, A. S., BUCKLEY, D. I., et al. (2014) · Cancer Research · doi:10.1158/1538-7445.am2014-1815
Self-citation
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
Ventura, R., Mordec, K., Waszczuk, J., Wang, Z., Lai, J., Fridlib, M., Buckley, D., Kemble, G., & Heuer, T. S. (2015) · EBioMedicine · doi:10.1016/j.ebiom.2015.06.020 · Cited by 301 · see citing works
Self-citation
Fatty Acid Synthase Inhibitors Enhance Microtubule-Stabilizing and Microtubule-Destabilizing Drugs in Taxane-Resistant Prostate Cancer Cells
Souchek, J. J., Laliwala, A., Houser, L. J., Muraskin, L., Vu, Q., & Mohs, A. M. (2023) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.3c00182 · Cited by 13 · see citing works
Abstract C175: FASN inhibition studies in preclinical tumor models identify biomarkers that align with in vitro and in vivo sensitivity to TVB-2640
Heuer, T. S., Ventura, R., Mordec, K., Lai, J., Waszczuk, J., Rubio, C., Farrell, M. O., BUCKLEY, D. I., & Kemble, G. W. (2015) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.targ-15-c175
Self-citation

Authors: Heuer, T. S., Ventura, R., Mordec, K., Lai, J., Fridlib, M., Buckley, D., & Kemble, G.
Corresponding author: Heuer, Timothy S.
ORCID: Ventura, Richard
Kemble, George
Venue: EBioMedicine
Publisher: Elsevier BV
Published: 2017-02
Volume: 16
Pages: 51-62
ISSN: 2352-3964 (ISSN-L)
DOI: 10.1016/j.ebiom.2016.12.012
PMC: PMC5474427
OpenAlex: W2567412474
Cited by: 136
References: 53
Citations by year: 2026: 6 · 2025: 17 · 2024: 20 · 2023: 18 · 2022: 19 · 2021: 17 · 2020: 14 · 2019: 12 · 2018: 8 · 2017: 5
FWCI: 3.47
Type: journal article
Language: en
Open access: gold
doi.org
Licence: cc-by-nc-nd
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
creativecommons.org/licenses/by-nc-nd/4.0/ (vor)
Locations: EBioMedicine (publishedVersion, cc-by-nc-nd)
Europe PMC (PubMed Central) (publishedVersion, cc-by-nc-nd)
PubMed Central (publishedVersion, cc-by-nc-nd)
PubMed (publishedVersion)
DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer, Lipids, and Metabolism
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › Microtubule and mitosis dynamics
Health Sciences › Medicine › Oncology › Cancer Treatment and Pharmacology
Keywords: FASN inhibition, microtubule organization, taxanes, paclitaxel, docetaxel, combination cancer therapy, tumor xenografts, β-catenin signaling, palmitate, lung cancer, ovarian cancer, prostate cancer, pancreatic cancer
MeSH terms: A549 Cells, Animals, Antineoplastic Agents, Azetidines, Bridged-Ring Compounds, Cell Line, Enzyme Inhibitors, Female, Humans, Mice, Inbred BALB C, Mice, Nude, Microtubules, Nitriles, Phosphorylation, Pyrazoles, Tubulin, Blotting, Western, Molecular Structure, Gene Expression Regulation, Neoplastic, Microscopy, Confocal, Reverse Transcriptase Polymerase Chain Reaction, Xenograft Model Antitumor Assays, Taxoids, Cell Line, Tumor, beta Catenin, Mice, Lipoylation, Fatty Acid Synthase, Type I, Carcinogenesis

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

FASN Inhibition and Taxane Treatment Combine to Enhance Anti-tumor Efficacy in Diverse Xenograft Tumor Models through Disruption of Tubulin Palmitoylation and Microtubule Organization and FASN Inhibition-Mediated Effects on Oncogenic Signaling and Gene Expression

Abstract

Integrity signals

Claims the paper makes

Claims other papers make about this one

Self-check

Cites

Cited by

Related

Record

About these checks