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https://www.readbyqxmd.com/read/28615298/combination-treatment-with-orlistat-containing-nanoparticles-and-taxanes-is-synergistic-and-enhances-microtubule-stability-in-taxane-resistant-prostate-cancer-cells
#1
Joshua J Souchek, Amanda L Davis, Tanner K Hill, Megan B Holmes, Bowen Qi, Pankaj K Singh, Steven J Kridel, Aaron M Mohs
Taxane-based therapy provides a survival benefit in patients with metastatic prostate cancer, yet the median survival is less than 20 months in this setting due in part to taxane-associated resistance. Innovative strategies are required to overcome chemoresistance for improved patient survival. Here, NanoOrl, a new experimental nanoparticle formulation of the FDA-approved drug, orlistat, was investigated for its cytotoxicity in taxane-resistant prostate cancer utilizing two established taxane-resistant (TxR) cell lines...
June 14, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28588696/mapk-p53-mediated-fasn-expression-in-bone-tumors
#2
Ye Jiang, Xiaofan Yin, Liang Wu, Qiang Qin, Jun Xu
The correlation between mitogen-activated protein kinase (MAPK)/P53 signaling-dependent fatty acid synthase (FASN) expression and bone tumors was examined in the present study. We established the SH081 bone tumor cell line, which was used to determine the expression of FASN and MAPK/P53 at the mRNA and protein levels in bone tumor cells and normal cells. Compared with the normal cells, the expression of MAPK/P53 and FASN mRNA was significantly elevated, whereas inhibition of MAPK/P53 decreased FASN expression...
June 2017: Oncology Letters
https://www.readbyqxmd.com/read/28576870/role-of-mir-383-and-mir-146b-in-different-propensities-to-obesity-in-male-mice
#3
Shu-Fang Xia, Xiao-Mei Duan, Xiang-Rong Cheng, Li-Mei Chen, Yan-Jun Kang, Peng Wang, Xue Tang, Yong-Hui Shi, Guowei Le
The study was designed to investigate the possible mechanisms of hepatic microRNAs (miRs) in regulating local thyroid hormone (TH) action and ultimately different propensities to high-fat diet (HFD) induced obesity. When obesity-prone (OP) and obesity-resistant (OR) mice were fed high-fat diet for 7 weeks, OP mice showed apparent hepatic steatosis, with significantly higher body weight and lower hepatic thyroid hormone receptor b (TRb) expression and type 1 deiodinase (DIO1) activity than OR mice. Next-generation sequencing technology revealed that 13 miRs in liver were dysregulated between the two phenotypes, of which 8 miRs were predicted to target on Dio1 or TRb...
June 2, 2017: Journal of Endocrinology
https://www.readbyqxmd.com/read/28475135/modulation-of-ho-1-by-ferulic-acid-attenuates-adipocyte-differentiation-in-3t3-l1-cells
#4
Eun-Jeong Koh, Kui-Jin Kim, Young-Jin Seo, Jia Choi, Boo-Yong Lee
Ferulic acid (FA) is phenolic compound found in fruits. Many studies have reported that FA has diverse therapeutic effects against metabolic diseases. However, the mechanism by which FA modulates adipogenesis via the expression of heme oxygenase-1 (HO-1) implicated in suppression of adipocyte differentiation is not fully understood. We investigated whether HO-1 can be activated by FA and suppress adipogenic factors in 3T3-L1. Our results showed that FA suppresses triglyceride-synthesizing enzymes, fatty acid synthase (FASN) and acetyl-CoA carboxylase (ACC)...
May 5, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28449683/inhibition-of-nampt-aggravates-high-fat-diet-induced-hepatic-steatosis-in-mice-through-regulating-sirt1-ampk%C3%AE-srebp1-signaling-pathway
#5
Ling-Fang Wang, Xiao-Nv Wang, Cong-Cong Huang, Long Hu, Yun-Fei Xiao, Xiao-Hui Guan, Yi-Song Qian, Ke-Yu Deng, Hong-Bo Xin
BACKGROUND: Nonalcoholic fatty liver disease is one of the most common liver diseases in the world and is a typical hepatic manifestation of metabolic syndrome which is characterized with lipid accumulation in liver. Nicotinamide phosphoribosyltransferase (NAMPT) has been recently identified as an enzyme involved in nicotinamide adenine dinucleotide (NAD(+)) biosynthesis and plays an important role in cellular metabolism in variety of organs in mammals. The aim of this study was to investigate the effects of NAMPT on high fat diet-induced hepatic steatosis...
April 27, 2017: Lipids in Health and Disease
https://www.readbyqxmd.com/read/28387458/anti-tumorigenic-potential-of-a-novel-orlistat-aicar-combination-in-prostate-cancer-cells
#6
Clayton Wright, Anand Krishnan V Iyer, Vivek Kaushik, Neelam Azad
Prostate cancer (PCa) is one of the leading causes of cancer-related deaths in men worldwide. Fatty acid synthase (FASN) is reported to be overexpressed in several cancers including PCa, and this has led to clinical cancer treatments that utilize various FASN inhibitors such as the anti-obesity drug, Orlistat. However, pharmacological limitations have impeded the progress in cancer treatments expected thus far with FASN inhibition. In this study, we investigated a novel therapeutic combination to enhance the toxic potential of Orlistat in three different PCa cell-lines (DU145, PC3, and LNCaP)...
April 7, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28386750/fatty-acid-synthase-regulates-the-chemosensitivity-of-breast-cancer-cells-to-cisplatin-induced-apoptosis
#7
Shadia Al-Bahlani, Hanaa Al-Lawati, Moza Al-Adawi, Nadia Al-Abri, Buthaina Al-Dhahli, Kawther Al-Adawi
Fatty acid synthase (FASN) is a key enzyme in fat biosynthesis that is over-expressed in advanced breast cancer stages. Cisplatin (CDDP) is a platinum-based drug used in the treatment of certain types of this disease. Although it was shown that FASN inhibition induced apoptosis by enhancing the cytotoxicity of certain drugs in breast cancer, its role in regulating the chemosensitivity of different types of breast cancer cells to CDDP-induced apoptosis is not established yet. Therefore, two different breast cancer cell lines; triple negative breast cancer (TNBC; MDA-MB-231) and triple positive breast cancer (TPBC; BT-474) cells were used to examine such role...
June 2017: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/28339092/macc1-decreases-the-chemosensitivity-of-gastric-cancer-cells-to-oxaliplatin-by-regulating-fasn-expression
#8
Jiangman Duan, Lishan Chen, Minyu Zhou, Jingwen Zhang, Li Sun, Na Huang, Jianping Bin, Yulin Liao, Wangjun Liao
The effect of chemotherapeutic agents is limited as a result of drug resistance, which demands prompt solutions provided by clinical studies. To date, the underlying mechanisms of chemotherapy resistance are relatively unknown. Metastasis-associated in colon cancer 1 (MACC1) is an oncogene associated with the progression and prognosis of gastric cancer (GC). Bioinformatic analysis revealed that MACC1 is positively associated with fatty acid synthase (FASN), a major enzyme of lipogenesis, and drives chemoresistance to oxaliplatin in GC...
May 2017: Oncology Reports
https://www.readbyqxmd.com/read/28260110/inhibitory-effect-of-emodin-on-fatty-acid-synthase-colon-cancer-proliferation-and-apoptosis
#9
Kyung Ha Lee, Myung Sun Lee, Eun Young Cha, Ji Young Sul, Jin Sun Lee, Jin Su Kim, Jun Beom Park, Ji Yeon Kim
Fatty acid synthase (FASN) is a key anabolic enzyme for de novo fatty acid synthesis, which is important in the development of colon carcinoma. The high expression of FASN is considered a promising molecular target for colon cancer therapy. Emodin, a naturally occurring anthraquinone, exhibits an anticancer effect in various types of human cancer, including colon cancer; however, the molecular mechanisms remain to be fully elucidated. Cell viability was evaluated using a Cell Counting Kit‑8 assay. The apoptosis rate of cells was quantified via flow cytometry following Annexin V/propidium iodide staining...
April 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28240737/fatty-acid-synthase-regulates-estrogen-receptor-%C3%AE-signaling-in-breast-cancer-cells
#10
J A Menendez, R Lupu
Fatty acid synthase (FASN), the key enzyme for endogenous synthesis of fatty acids, is overexpressed and hyperactivated in a biologically aggressive subset of sex steroid-related tumors, including breast carcinomas. Using pharmacological and genetic approaches, we assessed the molecular relationship between FASN signaling and estrogen receptor alpha (ERα) signaling in breast cancer. The small compound C75, a synthetic slow-binding inhibitor of FASN activity, induced a dramatic augmentation of estradiol (E2)-stimulated, ERα-driven transcription...
February 27, 2017: Oncogenesis
https://www.readbyqxmd.com/read/28218386/glucose-adsorption-to-chitosan-membranes-increases-proliferation-of-human-chondrocyte-via-mammalian-target-of-rapamycin-complex-1-and-sterol-regulatory-element-binding-protein-1-signaling
#11
Shun-Fu Chang, Kuo-Chin Huang, Chin-Chang Cheng, Yu-Ping Su, Ko-Chao Lee, Cheng-Nan Chen, Hsin-I Chang
Osteoarthritis (OA) is currently still an irreversible degenerative disease of the articular cartilage. Recent, dextrose (d-glucose) intraarticular injection prolotherapy for OA patients has been reported to benefit the chondrogenic stimulation of damaged cartilage. However, the detailed mechanism of glucose's effect on cartilage repair remains unclear. Chitosan, a naturally derived polysaccharide, has recently been investigated as a surgical or dental dressing to control breeding. Therefore, in this study, glucose was adsorbed to chitosan membranes (CTS-Glc), and the study aimed to investigate whether CTS-Glc complex membranes could regulate the proliferation of human OA chondrocytes and to explore the underlying mechanism...
October 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28107461/inhibition-of-fatty-acid-synthase-reduces-blastocyst-hatching-through-regulation-of-the-akt-pathway-in-pigs
#12
Jing Guo, Nam-Hyung Kim, Xiang-Shun Cui
Fatty acid synthase (FASN) is an enzyme responsible for the de novo synthesis of long-chain fatty acids. During oncogenesis, FASN plays a role in growth and survival rather than acting within the energy storage pathways. Here, the function of FASN during early embryonic development was studied using its specific inhibitor, C75. We found that the presence of the inhibitor reduced blastocyst hatching. FASN inhibition decreased Cpt1 expression, leading to a reduction in mitochondria numbers and ATP content. This inhibition of FASN resulted in the down-regulation of the AKT pathway, thereby triggering apoptosis through the activation of the p53 pathway...
2017: PloS One
https://www.readbyqxmd.com/read/27918556/effects-of-fatty-acid-synthase-inhibitors-on-lymphatic-vessels-an-in-vitro-and-in-vivo-study-in-a-melanoma-model
#13
Débora C Bastos, Jenny Paupert, Catherine Maillard, Fabiana Seguin, Marco A Carvalho, Michelle Agostini, Ricardo D Coletta, Agnès Noël, Edgard Graner
Fatty acid synthase (FASN) is responsible for the endogenous production of fatty acids from acetyl-CoA and malonyl-CoA. Its overexpression is associated with poor prognosis in human cancers including melanomas. Our group has previously shown that the inhibition of FASN with orlistat reduces spontaneous lymphatic metastasis in experimental B16-F10 melanomas, which is a consequence, at least in part, of the reduction of proliferation and induction of apoptosis. Here, we sought to investigate the effects of pharmacological FASN inhibition on lymphatic vessels by using cell culture and mouse models...
February 2017: Laboratory Investigation; a Journal of Technical Methods and Pathology
https://www.readbyqxmd.com/read/27765901/a-fasn-tgf-%C3%AE-1-fasn-regulatory-loop-contributes-to-high-emt-metastatic-potential-of-cisplatin-resistant-non-small-cell-lung-cancer
#14
Li Yang, Fuquan Zhang, Xin Wang, Ying Tsai, Kuang-Hsiang Chuang, Peter C Keng, Soo Ok Lee, Yuhchyau Chen
Cisplatin-resistant A549CisR and H157CisR cell lines were developed by treating parental A549 (A549P) and H157 (H157P) cells. These cisplatin-resistant cells showed slight growth retardation, but exhibited higher epithelial-mesenchymal transition (EMT) and increased metastatic potential compared to parental cells. We observed a highly up-regulated fatty acid synthase (FASN) level in A549CisR and H157CisR cells compared to parental cells and the up-regulation of FASN was also detected in A549P and H157P cells after short time treatment with cisplatin, suggesting that the high level of FASN in cisplatin-resistant cells may be from the accumulated cellular responses during cisplatin-resistance developmental process...
August 23, 2016: Oncotarget
https://www.readbyqxmd.com/read/27760195/prolyl-oligopeptidase-inhibition-attenuates-steatosis-in-the-l02-human-liver-cell-line
#15
Da Zhou, Bing-Hang Li, Jing Wang, Yong-Nian Ding, Yan Dong, Yuan-Wen Chen, Jian-Gao Fan
BACKGROUND: Prolyl oligopeptidase (POP) is a serine endopeptidase that is widely distributed in vivo, particularly in the liver. Significant changes in functional mitochondrial proteins involved with mitochondrial oxidoreductases/transporters and nucleic acid binding proteins were observed after POP inhibition in the liver, which suggested a role of POP in regulating liver energy metabolism. Steatosis in nonalcoholic fatty liver disease (NAFLD) is associated with disturbances in lipid and energy metabolism in hepatocytes...
2016: PloS One
https://www.readbyqxmd.com/read/27758890/destabilization-of-fatty-acid-synthase-by-acetylation-inhibits-de-novo-lipogenesis-and-tumor-cell-growth
#16
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
Fatty acid synthase (FASN) is the terminal enzyme in de novo lipogenesis and plays a key role in cell proliferation. Pharmacologic inhibitors of FASN are being evaluated in clinical trials for treatment of cancer, obesity, and other diseases. Here, we report a previously unknown mechanism of FASN regulation involving its acetylation by KAT8 and its deacetylation by HDAC3. FASN acetylation promoted its degradation via the ubiquitin-proteasome pathway. FASN acetylation enhanced its association with the E3 ubiquitin ligase TRIM21...
December 1, 2016: Cancer Research
https://www.readbyqxmd.com/read/27714708/clinical-and-therapeutic-relevance-of-the-metabolic-oncogene-fatty-acid-synthase-in-her2-breast-cancer
#17
Bruna Corominas-Faja, Luciano Vellon, Elisabet Cuyàs, Maria Buxó, Begoña Martin-Castillo, Dolors Serra, Jordi García, Ruth Lupu, Javier A Menendez
Fatty acid synthase (FASN) is a key lipogenic enzyme for de novo fatty acid biosynthesis and a druggable metabolic oncoprotein that is activated in most human cancers. We evaluated whether the HER2-driven lipogenic phenotype might represent a biomarker for sensitivity to pharmacological FASN blockade. A majority of clinically HER2-positive tumors were scored as FASN overexpressors in a series of almost 200 patients with invasive breast carcinoma. Re-classification of HER2-positive breast tumors based on FASN gene expression predicted a significantly inferior relapse-free and distant metastasis-free survival in HER2+/FASN+ patients...
July 2017: Histology and Histopathology
https://www.readbyqxmd.com/read/27701891/recent-advances-in-targeting-the-fatty-acid-biosynthetic-pathway-using-fatty-acid-synthase-inhibitors
#18
REVIEW
Thelma S Angeles, Robert L Hudkins
Elevated lipogenesis has been associated with a variety of diseases including obesity, cancer and nonalcoholic fatty liver disease (NAFLD). Fatty acid synthase (FASN) plays a pivotal role in de novo lipogenesis, making this multi-catalytic protein an attractive target for therapeutic intervention. Recently, the first FASN inhibitor successfully advanced through the drug development process and entered clinical evaluation in oncology. Areas covered: This review discusses the biological roles of FASN in three prominent disease areas: cancer, obesity-related disorders and NAFLD...
December 2016: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/27670404/metabolic-programming-of-a-beige-adipocyte-phenotype-by-genistein
#19
Sadat A Aziz, Luisa A Wakeling, Satomi Miwa, Goiuri Alberdi, John E Hesketh, Dianne Ford
SCOPE: Promoting the development of brown or beige adipose tissue may protect against obesity and related metabolic features, and potentially underlies protective effects of genistein in mice. METHODS AND RESULTS: We observed that application of genistein to 3T3-L1 adipocytes changed the lipid distribution from large droplets to a multilocular distribution, reduced mRNAs indicative of white adipocytes (ACC, Fasn, Fabp4, HSL, chemerin, and resistin) and increased mRNAs that are a characteristic feature of brown/beige adipocytes (CD-137 and UCP1)...
February 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/27641336/the-microrna-182-pdk4-axis-regulates-lung-tumorigenesis-by-modulating-pyruvate-dehydrogenase-and-lipogenesis
#20
G Li, M Li, J Hu, R Lei, H Xiong, H Ji, H Yin, Q Wei, G Hu
Reprogrammed metabolism is one of the hallmarks of cancer. The dysregulation of glycolysis in cancer has been heavily studied. However, it remains largely unclear how other metabolic processes are regulated in cancer cells. Here we show that microRNA-182 (miR-182) suppresses pyruvate dehydrogenase (PDH) kinase 4 (PDK4) and promotes lung tumorigenesis. miR-182 is dysregulated and inversely correlated with PDK4 in human lung adenocarcinomas. The miR-182-PDK4 axis regulates lung cancer cell growth by modulating the activity of PDH, the gatekeeping enzyme of pyruvate flux into acetyl-CoA, and subsequently de novo lipogenesis of cancer cells...
September 19, 2016: Oncogene
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