1
|
Chen JQ and Russo J: Dysregulation of
glucose transport, glycolysis, TCA cycle and glutaminolysis by
oncogenes and tumor suppressors in cancer cells. Biochim Biophys
Acta. 1826:370–384. 2012.PubMed/NCBI
|
2
|
Levine AJ and Puzio-Kuter AM: The control
of the metabolic switch in cancers by oncogenes and tumor
suppressor genes. Science. 330:1340–1344. 2010. View Article : Google Scholar : PubMed/NCBI
|
3
|
Barger JF and Plas DR: Balancing
biosynthesis and bioenergetics: Metabolic programs in oncogenesis.
Endocr Relat Cancer. 17:R287–R304. 2010. View Article : Google Scholar : PubMed/NCBI
|
4
|
Newsholme EA, Crabtree B and Ardawi MS:
The role of high rates of glycolysis and glutamine utilization in
rapidly dividing cells. Biosci Rep. 5:393–400. 1985. View Article : Google Scholar : PubMed/NCBI
|
5
|
McKeehan WL: Glycolysis, glutaminolysis
and cell proliferation. Cell Biol Int Rep. 6:635–650. 1982.
View Article : Google Scholar : PubMed/NCBI
|
6
|
Menendez JA, Ropero S, Mehmi I, Atlas E,
Colomer R and Lupu R: Overexpression and hyperactivity of breast
cancer-associated fatty acid synthase (oncogenic antigen-519) is
insensitive to normal arachidonic fatty acid-induced suppression in
lipogenic tissues but it is selectively inhibited by tumoricidal
α-linolenic and γ-linolenic fatty acids: A novel mechanism by which
dietary fat can alter mammary tumorigenesis. Int J Oncol.
24:1369–1383. 2004.PubMed/NCBI
|
7
|
Wang Y, Jones Voy B, Urs S, Kim S,
Soltani-Bejnood M, Quigley N, Heo YR, Standridge M, Andersen B,
Dhar M, et al: The human fatty acid synthase gene and de novo
lipogenesis are coordinately regulated in human adipose tissue. J
Nutr. 134:1032–1038. 2004.PubMed/NCBI
|
8
|
Little JL and Kridel SJ: Fatty acid
synthase activity in tumor cells. Subcell Biochem. 49:169–194.
2008. View Article : Google Scholar : PubMed/NCBI
|
9
|
Menendez JA and Lupu R: Fatty acid
synthase and the lipogenic phenotype in cancer pathogenesis. Nat
Rev Cancer. 7:763–777. 2007. View
Article : Google Scholar : PubMed/NCBI
|
10
|
Di Cosimo S, Ferretti G, Papaldo P,
Carlini P, Fabi A and Cognetti F: Lonidamine: Efficacy and safety
in clinical trials for the treatment of solid tumors. Drugs Today.
39:157–174. 2003. View Article : Google Scholar : PubMed/NCBI
|
11
|
Kisner DL, Catane R and Muggia FM: The
rediscovery of DON (6-diazo-5-oxo-L-norleucine). Recent Results
Cancer Res. 74:258–263. 1980. View Article : Google Scholar : PubMed/NCBI
|
12
|
Lupu R and Menendez JA: Pharmacological
inhibitors of Fatty Acid Synthase (FASN) - catalyzed endogenous
fatty acid biogenesis: A new family of anti-cancer agents? Curr
Pharm Biotechnol. 7:483–493. 2006. View Article : Google Scholar : PubMed/NCBI
|
13
|
Menendez JA, Vellon L and Lupu R:
Antitumoral actions of the anti-obesity drug orlistat (Xenical™) in
breast cancer cells: Blockade of cell cycle progression, promotion
of apoptotic cell death and PEA3-mediated transcriptional
repression of Her2/neu (erbB-2) oncogene. Ann Oncol. 16:1253–1267.
2005. View Article : Google Scholar : PubMed/NCBI
|
14
|
Yang CS, Matsuura K, Huang NJ, Robeson AC,
Huang B, Zhang L and Kornbluth S: Fatty acid synthase inhibition
engages a novel caspase-2 regulatory mechanism to induce ovarian
cancer cell death. Oncogene. 34:3264–3272. 2015. View Article : Google Scholar
|
15
|
Fujiwara J, Sowa Y, Horinaka M, Koyama M,
Wakada M, Miki T and Sakai T: The anti-obesity drug orlistat
promotes sensitivity to TRAIL by two different pathways in
hormone-refractory prostate cancer cells. Int J Oncol.
40:1483–1491. 2012.PubMed/NCBI
|
16
|
Zecchin KG, Rossato FA, Raposo HF, Melo
DR, Alberici LC, Oliveira HC, Castilho RF, Coletta RD, Vercesi AE
and Graner E: Inhibition of fatty acid synthase in melanoma cells
activates the intrinsic pathway of apoptosis. Lab Invest.
91:232–240. 2011. View Article : Google Scholar
|
17
|
Samudio I, Harmancey R, Fiegl M,
Kantarjian H, Konopleva M, Korchin B, Kaluarachchi K, Bornmann W,
Duvvuri S, Taegtmeyer H, et al: Pharmacologic inhibition of fatty
acid oxidation sensitizes human leukemia cells to apoptosis
induction. J Clin Invest. 120:142–156. 2010. View Article : Google Scholar :
|
18
|
Kant S, Kumar A and Singh SM: Tumor growth
retardation and chemosensitizing action of fatty acid synthase
inhibitor orlistat on T cell lymphoma: Implication of reconstituted
tumor microenvironment and multidrug resistance phenotype. Biochim
Biophys Acta. 1840:294–302. 2014. View Article : Google Scholar
|
19
|
Tirado-Vélez JM, Joumady I, Sáez-Benito A,
Cózar-Castellano I and Perdomo G; Tirado-Vélez JM: Inhibition of
fatty acid metabolism reduces human myeloma cells proliferation.
PLoS One. 7:e464842012. View Article : Google Scholar : PubMed/NCBI
|
20
|
Olsen AM, Eisenberg BL, Kuemmerle NB,
Flanagan AJ, Morganelli PM, Lombardo PS, Swinnen JV and Kinlaw WB:
Fatty acid synthesis is a therapeutic target in human liposarcoma.
Int J Oncol. 36:1309–1314. 2010.PubMed/NCBI
|
21
|
Dowling S, Cox J and Cenedella RJ:
Inhibition of fatty acid synthase by Orlistat accelerates gastric
tumor cell apoptosis in culture and increases survival rates in
gastric tumor bearing mice in vivo. Lipids. 44:489–498. 2009.
View Article : Google Scholar : PubMed/NCBI
|
22
|
Chuang HY, Chang YF and Hwang JJ:
Antitumor effect of orlistat, a fatty acid synthase inhibitor, is
via activation of caspase-3 on human colorectal carcinoma-bearing
animal. Biomed Pharmacother. 65:286–292. 2011. View Article : Google Scholar : PubMed/NCBI
|
23
|
Pardo A, Selman M, Ramírez R, Ramos C,
Montaño M, Stricklin G and Raghu G: Production of collagenase and
tissue inhibitor of metalloproteinases by fibroblasts derived from
normal and fibrotic human lungs. Chest. 102:1085–1089. 1992.
View Article : Google Scholar : PubMed/NCBI
|
24
|
Huang RS and Ratain MJ: Pharmacogenetics
and pharmacogenomics of anticancer agents. CA Cancer J Clin.
59:42–55. 2009. View Article : Google Scholar : PubMed/NCBI
|
25
|
Fernandes DJ, Sur P, Kute TE and Capizzi
RL: Proliferation-dependent cytotoxicity of methotrexate in murine
L5178Y leukemia. Cancer Res. 48:5638–5644. 1988.PubMed/NCBI
|
26
|
Gatto B and Cavalli M: From proteins to
nucleic acid-based drugs: The role of biotech in anti-VEGF therapy.
Anticancer Agents Med Chem. 6:287–301. 2006. View Article : Google Scholar : PubMed/NCBI
|
27
|
Hanahan D and Weinberg RA: Hallmarks of
cancer: The next generation. Cell. 144:646–674. 2011. View Article : Google Scholar : PubMed/NCBI
|
28
|
Zhao Y, Liu H, Riker AI, Fodstad O, Ledoux
SP, Wilson GL and Tan M: Emerging metabolic targets in cancer
therapy. Front Biosci. 16:1844–1860. 2011. View Article : Google Scholar
|
29
|
Ganapathy-Kanniappan S and Geschwind JF:
Tumor glycolysis as a target for cancer therapy: Progress and
prospects. Mol Cancer. 12:1522013. View Article : Google Scholar : PubMed/NCBI
|
30
|
Granchi C and Minutolo F: Anticancer
agents that counteract tumor glycolysis. ChemMedChem. 7:1318–1350.
2012. View Article : Google Scholar : PubMed/NCBI
|
31
|
Dwarakanath BS, Singh D, Banerji AK, Sarin
R, Venkataramana NK, Jalali R, Vishwanath PN, Mohanti BK, Tripathi
RP, Kalia VK, et al: Clinical studies for improving radiotherapy
with 2-deoxy-D-glucose: Present status and future prospects. J
Cancer Res Ther. 5(Suppl 1): S21–S26. 2009. View Article : Google Scholar : PubMed/NCBI
|
32
|
Garon EB, Christofk HR, Hosmer W, Britten
CD, Bahng A, Crabtree MJ, Hong CS, Kamranpour N, Pitts S,
Kabbinavar F, et al: Dichloroacetate should be considered with
platinum-based chemotherapy in hypoxic tumors rather than as a
single agent in advanced non-small cell lung cancer. J Cancer Res
Clin Oncol. 140:443–452. 2014. View Article : Google Scholar : PubMed/NCBI
|
33
|
Catane R, Von Hoff DD, Glaubiger DL and
Muggia FM: Azaserine, DON and azotomycin: Three diazo analogs of
L-glutamine with clinical antitumor activity. Cancer Treat Rep.
63:1033–1038. 1979.PubMed/NCBI
|
34
|
Unger C, Mueller C, Bausch MP, et al: A
phase I schedule optimization study of pegylatedglutaminase
(PEG-PGA) plus 6-diazo-5-oxo-l-norleucine (DON) in patients (pts)
with advanced solid tumors. J Clin Oncol. 29:abs. 3049. 2011.
|
35
|
Strickland DK: Study of the glutaminase
inhibitor CB-839 in solid tumors. Clinical Trials Identifier:
NCT02071862. February. 2014, http://clinicaltrials.gov/ct2/results?term=glutaminasecancer&Search=Search.
Last updated March 9, 2015.
|
36
|
Griffths M, Keast D, Patrick G, Crawford M
and Palmer TN: The role of glutamine and glucose analogues in
metabolic inhibition of human myeloid leukaemia in vitro. Int J
Biochem. 25:1749–1755. 1993. View Article : Google Scholar
|
37
|
Anighoro A, Bajorath J and Rastelli G:
Polypharmacology: Challenges and opportunities in drug discovery. J
Med Chem. 57:7874–7887. 2014. View Article : Google Scholar : PubMed/NCBI
|
38
|
Zhi J, Mulligan TE and Hauptman JB:
Long-term systemic exposure of orlistat, a lipase inhibitor and its
metabolites in obese patients. J Clin Pharmacol. 39:41–46. 1999.
View Article : Google Scholar : PubMed/NCBI
|
39
|
O'Connor MB: An orlistat 'overdose' in a
child. Ir J Med Sci. 179:3152010. View Article : Google Scholar
|
40
|
Young CD and Anderson SM: Sugar and fat -
that's where it's at: Metabolic changes in tumors. Breast Cancer
Res. 10:2022008. View
Article : Google Scholar : PubMed/NCBI
|
41
|
Sankaranarayanapillai M, Zhang N, Baggerly
KA and Gelovani JG: Metabolic shifts induced by fatty acid synthase
inhibitor orlistat in non-small cell lung carcinoma cells provide
novel pharmacodynamic biomarkers for positron emission tomography
and magnetic resonance spectroscopy. Mol Imaging Biol. 15:136–147.
2013. View Article : Google Scholar :
|