Literature DB >> 20373869

Fatty acid synthase as a potential therapeutic target in cancer.

Richard Flavin1, Stephane Peluso, Paul L Nguyen, Massimo Loda.   

Abstract

Fatty acid synthase (FASN) is a key enzyme involved in neoplastic lipogenesis. Overexpression of FASN is common in many cancers, and accumulating evidence suggests that it is a metabolic oncogene with an important role in tumor growth and survival, making it an attractive target for cancer therapy. Early small-molecule FASN inhibitors such as cerulenin, C75 and orlistat have been shown to induce apoptosis in several cancer cell lines and to induce tumor growth delay in several cancer xenograft models but their mechanism is still not well understood. These molecules suffer from pharmacological limitations and weight loss as a side effect that prevent their development as systemic drugs. Several potent inhibitors have recently been reported that may help to unravel and exploit the full potential of FASN as a target for cancer therapy in the near future. Furthermore, novel sources of FASN inhibitors, such as green tea and dietary soy, make both dietary manipulation and chemoprevention potential alternative modes of therapy in the future.

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Year:  2010        PMID: 20373869      PMCID: PMC3197858          DOI: 10.2217/fon.10.11

Source DB:  PubMed          Journal:  Future Oncol        ISSN: 1479-6694            Impact factor:   3.404


  105 in total

1.  Fatty acid synthase inhibition in human breast cancer cells leads to malonyl-CoA-induced inhibition of fatty acid oxidation and cytotoxicity.

Authors:  J N Thupari; M L Pinn; F P Kuhajda
Journal:  Biochem Biophys Res Commun       Date:  2001-07-13       Impact factor: 3.575

2.  Fatty acid synthase gene overexpression and copy number gain in prostate adenocarcinoma.

Authors:  Uzma S Shah; Rajiv Dhir; Susanne M Gollin; Uma R Chandran; Dale Lewis; Marie Acquafondata; Beth R Pflug
Journal:  Hum Pathol       Date:  2006-02-07       Impact factor: 3.466

3.  Platensimycin is a selective FabF inhibitor with potent antibiotic properties.

Authors:  Jun Wang; Stephen M Soisson; Katherine Young; Wesley Shoop; Srinivas Kodali; Andrew Galgoci; Ronald Painter; Gopalakrishnan Parthasarathy; Yui S Tang; Richard Cummings; Sookhee Ha; Karen Dorso; Mary Motyl; Hiranthi Jayasuriya; John Ondeyka; Kithsiri Herath; Chaowei Zhang; Lorraine Hernandez; John Allocco; Angela Basilio; José R Tormo; Olga Genilloud; Francisca Vicente; Fernando Pelaez; Lawrence Colwell; Sang Ho Lee; Bruce Michael; Thomas Felcetto; Charles Gill; Lynn L Silver; Jeffery D Hermes; Ken Bartizal; John Barrett; Dennis Schmatz; Joseph W Becker; Doris Cully; Sheo B Singh
Journal:  Nature       Date:  2006-05-18       Impact factor: 49.962

4.  The expression of fatty acid synthase (FASE) is an early event in the development and progression of squamous cell carcinoma of the lung.

Authors:  C J Piyathilake; A R Frost; U Manne; W C Bell; H Weiss; D C Heimburger; W E Grizzle
Journal:  Hum Pathol       Date:  2000-09       Impact factor: 3.466

5.  Fatty acid synthase inhibitors are chemopreventive for mammary cancer in neu-N transgenic mice.

Authors:  Patricia M Alli; Michael L Pinn; Elizabeth M Jaffee; Jill M McFadden; Francis P Kuhajda
Journal:  Oncogene       Date:  2005-01-06       Impact factor: 9.867

6.  Epigallocatechin-3-gallate is a potent natural inhibitor of fatty acid synthase in intact cells and selectively induces apoptosis in prostate cancer cells.

Authors:  Koen Brusselmans; Ellen De Schrijver; Walter Heyns; Guido Verhoeven; Johannes V Swinnen
Journal:  Int J Cancer       Date:  2003-10-10       Impact factor: 7.396

7.  Novel fatty acid synthase (FAS) inhibitors: design, synthesis, biological evaluation, and molecular docking studies.

Authors:  Xiaokui Wang; Jian Lin; Yao Chen; Wu Zhong; Guoming Zhao; Hongying Liu; Site Li; Lili Wang; Song Li
Journal:  Bioorg Med Chem       Date:  2009-01-29       Impact factor: 3.641

8.  Experimental verification of conformational variation of human fatty acid synthase as predicted by normal mode analysis.

Authors:  Jacob Brink; Steven J Ludtke; Yifei Kong; Salih J Wakil; Jianpeng Ma; Wah Chiu
Journal:  Structure       Date:  2004-02       Impact factor: 5.006

9.  Brain fatty acid synthase activates PPARalpha to maintain energy homeostasis.

Authors:  Manu V Chakravarthy; Yimin Zhu; Miguel López; Li Yin; David F Wozniak; Trey Coleman; Zhiyuan Hu; Michael Wolfgang; Antonio Vidal-Puig; M Daniel Lane; Clay F Semenkovich
Journal:  J Clin Invest       Date:  2007-09       Impact factor: 14.808

10.  Malonyl-CoA decarboxylase inhibition is selectively cytotoxic to human breast cancer cells.

Authors:  W Zhou; Y Tu; P J Simpson; F P Kuhajda
Journal:  Oncogene       Date:  2009-06-22       Impact factor: 9.867

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  206 in total

1.  Colonic mucosal fatty acid synthase as an early biomarker for colorectal neoplasia: modulation by obesity and gender.

Authors:  Mart Dela Cruz; Ramesh K Wali; Laura K Bianchi; Andrew J Radosevich; Susan E Crawford; Lisa Jepeal; Michael J Goldberg; Jaclyn Weinstein; Navneet Momi; Priya Roy; Audrey H Calderwood; Vadim Backman; Hemant K Roy
Journal:  Cancer Epidemiol Biomarkers Prev       Date:  2014-08-25       Impact factor: 4.254

2.  Oncogene KRAS activates fatty acid synthase, resulting in specific ERK and lipid signatures associated with lung adenocarcinoma.

Authors:  Arvin M Gouw; Livia S Eberlin; Katherine Margulis; Delaney K Sullivan; Georgia G Toal; Ling Tong; Richard N Zare; Dean W Felsher
Journal:  Proc Natl Acad Sci U S A       Date:  2017-04-11       Impact factor: 11.205

3.  Differential requirement for de novo lipogenesis in cholangiocarcinoma and hepatocellular carcinoma of mice and humans.

Authors:  Lei Li; Li Che; Kevin M Tharp; Hyo-Min Park; Maria G Pilo; Dan Cao; Antonio Cigliano; Gavinella Latte; Zhong Xu; Silvia Ribback; Frank Dombrowski; Matthias Evert; Gregory J Gores; Andreas Stahl; Diego F Calvisi; Xin Chen
Journal:  Hepatology       Date:  2016-03-25       Impact factor: 17.425

4.  Fatty Acid Synthase Promotes the Palmitoylation of Chikungunya Virus nsP1.

Authors:  Na Zhang; Hongjian Zhao; Leiliang Zhang
Journal:  J Virol       Date:  2019-01-17       Impact factor: 5.103

5.  Active site labeling of fatty acid and polyketide acyl-carrier protein transacylases.

Authors:  Tony D Davis; Jennifer M Michaud; Michael D Burkart
Journal:  Org Biomol Chem       Date:  2019-05-15       Impact factor: 3.876

6.  Targeted metabolomic profiling of low and high grade serous epithelial ovarian cancer tissues: a pilot study.

Authors:  Gunjal Garg; Ali Yilmaz; Praveen Kumar; Onur Turkoglu; David G Mutch; Matthew A Powell; Barry Rosen; Ray O Bahado-Singh; Stewart F Graham
Journal:  Metabolomics       Date:  2018-11-24       Impact factor: 4.290

7.  An Essential Role for the Tumor-Suppressor Merlin in Regulating Fatty Acid Synthesis.

Authors:  Dina S Stepanova; Galina Semenova; Yin-Ming Kuo; Andrew J Andrews; Sylwia Ammoun; C Oliver Hanemann; Jonathan Chernoff
Journal:  Cancer Res       Date:  2017-07-20       Impact factor: 12.701

8.  Involvement of de novo synthesized palmitate and mitochondrial EGFR in EGF induced mitochondrial fusion of cancer cells.

Authors:  Lakshmi Reddy Bollu; Jiangong Ren; Alicia Marie Blessing; Rajasekhara Reddy Katreddy; Guang Gao; Lei Xu; Jinrong Wang; Fei Su; Zhang Weihua
Journal:  Cell Cycle       Date:  2014       Impact factor: 4.534

9.  MNX1 Is Oncogenically Upregulated in African-American Prostate Cancer.

Authors:  Li Zhang; Jianghua Wang; Yongquan Wang; Yiqun Zhang; Patricia Castro; Longjiang Shao; Arun Sreekumar; Nagireddy Putluri; Nilanjan Guha; Saligrama Deepak; Arunkumar Padmanaban; Chad J Creighton; Michael Ittmann
Journal:  Cancer Res       Date:  2016-08-30       Impact factor: 12.701

10.  Destabilization of Fatty Acid Synthase by Acetylation Inhibits De Novo Lipogenesis and Tumor Cell Growth.

Authors:  Huai-Peng Lin; Zhou-Li Cheng; Ruo-Yu He; Lei Song; Meng-Xin Tian; Li-Sha Zhou; Beezly S Groh; Wei-Ren Liu; Min-Biao Ji; Chen Ding; Ying-Hong Shi; Kun-Liang Guan; Dan Ye; Yue Xiong
Journal:  Cancer Res       Date:  2016-10-10       Impact factor: 12.701

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