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https://www.readbyqxmd.com/read/28922023/fatty-acid-synthase-fasn-as-a-therapeutic-target-in-breast-cancer
#1
Javier A Menendez, Ruth Lupu
Ten years ago, we put forward the metabolo-oncogenic nature of fatty acid synthase (FASN) in breast cancer. Since the conception of this hypothesis, which provided a model to explain how FASN is intertwined with various signaling networks to cell-autonomously regulate breast cancer initiation and progression, FASN has received considerable attention as a therapeutic target. However, despite the ever-growing evidence demonstrating the involvement of FASN as part of the cancer-associated metabolic reprogramming, translation of the basic science-discovery aspects of FASN blockade to the clinical arena remains a challenge...
September 18, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28871635/fatty-acid-synthase-as-a-potential-therapeutic-target-in-feline-oral-squamous-cell-carcinoma
#2
J Z Walz, J Saha, A Arora, A Khammanivong, M G O'Sullivan, E B Dickerson
Oral squamous cell carcinoma (OSCC) is an aggressive and treatment-resistant malignancy in both feline and human patients. Recent work has demonstrated aberrant expression of fatty acid synthase (FASN) and an increased capacity for lipogenesis in human OSCC and other cancers. In human OSCC, inhibition of FASN decreased cell viability and growth in vitro, and diminished tumour growth and metastasis in murine preclinical models. This study aimed to characterize FASN as a therapeutic target in feline OSCC. Immunohistochemistry revealed high FASN expression in primary feline OSCC tumours, and FASN expression was detected in OSCC cell lines (3 feline and 3 human) by immunoblotting and quantitative real-time-polymerase chain reaction (qRT-PCR)...
September 4, 2017: Veterinary and Comparative Oncology
https://www.readbyqxmd.com/read/28835435/mir-15b-negatively-correlates-with-lipid-metabolism-in-mammary-epithelial-cells
#3
Meiqiang Chu, Yong Zhao, Shuai Yu, Yanan Hao, Pengfei Zhang, Yanni Feng, Hongfu Zhang, Dongxue Ma, Jing Liu, Ming Cheng, Lan Li, Wei Shen, Hongfang Cao, Qiang Li, Lingjiang Min
Mammary epithelial cells are regulated by steroid hormones, growth factors, and even microRNAs. MiR-15b has been found to regulate lipid metabolism in adipocytes; however its effects on lipid metabolism in mammary epithelial cells, the cells of lipid synthesis and secretion, are as yet unknown. The main purpose of this investigation was to explore the effect of miR-15b on lipid metabolism in mammary epithelial cells, along with the underlying mechanisms. MiR-15b was overexpressed or inhibited by miRNA mimics or inhibitors; subsequently lipid formation in mammary epithelial cells, and proteins related to lipid metabolism, were investigated...
August 23, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/28833137/tert-ezh2-network-regulates-lipid-metabolism-and-dna-damage-responses-in-glioblastoma
#4
Fahim Ahmad, Shruti Patrick, Touseef Sheikh, Vikas Sharma, Pankaj Pathak, Prit Benny Malgulwar, Anupam Kumar, Shanker Datt Joshi, Chitra Sarkar, Ellora Sen
Elevated expression of enhancer of zeste homolog 2 (EZH2) - a histone H3K27 methyltransferase was observed in gliomas harboring telomerase reverse transcriptase (TERT) promoter mutations. Given the known involvement of TERT and EZH2 in glioma progression, the co-relation between the two and subsequently its involvement in metabolic programming was investigated. Inhibition of hTERT either pharmacologically or through genetic manipulation not only decreased EZH2 expression, but also (i) abrogated FASN levels, (ii) decreased de novo fatty acid accumulation, and (iii) increased Ataxia-telangiectasia mutated (ATM) phosphorylation levels...
August 21, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28811332/de-novo-lipid-synthesis-facilitates-gemcitabine-resistance-through-endoplasmic-reticulum-stress-in-pancreatic-cancer
#5
Saber Tadros, Surendra K Shukla, Ryan J King, Venugopal Gunda, Enza Vernucci, Jaime Abrego, Nina CHaika, Fang Yu, Audrey J Lazenby, Lyudmyla Berim, Jean L Grem, Aaron Sasson, Pankaj K Singh
Pancreatic adenocarcinoma is moderately responsive to gemcitabine-based chemotherapy, the most widely used single agent therapy for pancreatic cancer. While the prognosis in pancreatic cancer remains grim in part due to poor response to therapy, previous attempts at identifying and targeting the resistance mechanisms have not been very successful. By leveraging TCGA dataset, we identified lipid metabolism as the metabolic pathway that most significantly correlated with poor gemcitabine response in pancreatic cancer patients...
August 15, 2017: Cancer Research
https://www.readbyqxmd.com/read/28775317/interaction-between-von-hippel-lindau-protein-and-fatty-acid-synthase-modulates-hypoxia-target-gene-expression
#6
Wendi Sun, Hiroyuki Kato, Shojiro Kitajima, Kian Leong Lee, Katarina Gradin, Takashi Okamoto, Lorenz Poelllinger
Hypoxia-inducible factors (HIFs) play a central role in the transcriptional response to changes in oxygen availability. Stability of HIFs is regulated by multi-step reactions including recognition by the von Hippel-Lindau tumour suppressor protein (pVHL) in association with an E3 ligase complex. Here we show that pVHL physically interacts with fatty acid synthase (FASN), displacing the E3 ubiquitin ligase complex. This results in HIF-α protein stabilization and activation of HIF target genes even in normoxia such as during adipocyte differentiation...
August 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28729415/an-essential-role-for-the-tumor-suppressor-merlin-in-regulating-fatty-acid-synthesis
#7
Dina S Stepanova, Galina Semenova, Yin-Ming Kuo, Andrew J Andrews, Sylwia Ammoun, C Oliver Hanemann, Jonathan Chernoff
Neurofibromatosis type 2 (NF2) is an autosomal dominant disorder characterized by the development of multiple tumors in the central nervous system, most notably schwannomas, and meningiomas. Mutational inactivation of the NF2 gene encoding the protein Merlin is found in most sporadic and inherited schwannomas, but the molecular mechanisms underlying neoplastic changes in schwannoma cells remain unclear. We report here that Nf2-deficient cells display elevated expression levels of key enzymes involved in lipogenesis and that this upregulation is caused by increased activity of Torc1...
September 15, 2017: Cancer Research
https://www.readbyqxmd.com/read/28726934/clove-extract-functions-as-a-natural-fatty-acid-synthesis-inhibitor-and-prevents-obesity-in-a-mouse-model
#8
Yiran Ding, Zhennan Gu, Yihe Wang, Shunhe Wang, Haiqin Chen, Hao Zhang, Wei Chen, Yong Q Chen
Numerous medicinal plants have been reported to prevent various chronic diseases. In this study, we screened a new FASN inhibitor-alcohol extract of clove (AEC) using a fast microplate method developed in our laboratory. The major components of AEC were: eugenol (42.27%), acetyl eugenol (29.12%), caryophyllene (15.40%), and humulene (3.22%). Fatty acid synthase (FASN) is a key enzyme for de novo lipogenesis, and it has been suggested as a potential therapeutic target in cancer and obesity. We have tested the ability of AEC to inhibit FASN in mammalian cells and tissues...
August 1, 2017: Food & Function
https://www.readbyqxmd.com/read/28668964/glp-1-glp-1r-signaling-in-regulation-of-adipocyte-differentiation-and-lipogenesis
#9
Jicui Chen, Huichen Zhao, Xiaoli Ma, Yuchao Zhang, Sumei Lu, Yangang Wang, Chen Zong, Dandan Qin, Yuanmei Wang, Yingfeng Yingfeng Yang, Xiangdong Wang, Yuantao Liu
BACKGROUND/AIMS: The aim of this study was to determine the direct role of liraglutide (LG) in adipogenesis and lipid metabolism. METHODS: Lipid accumulation was evaluated by oil red O staining, quantitative real-time PCR (qPCR) was performed to determine glucagon-like peptide 1 receptor (GLP-1R), fatty acid synthase (FASN) and adipose triglyceride lipase (ATGL) expression in 3T3-L1 preadipocytes, differentiated adipocytes and in adipose tissues from mice. The effects of LG on 3T3-L1 adipogenesis and lipid metabolism were analyzed with qPCR, Western Blotting, oil red O staining, immunohistochemistry (IHC) and immunofluorescence (IF)...
June 30, 2017: Cellular Physiology and Biochemistry
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
#10
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...
September 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28588696/mapk-p53-mediated-fasn-expression-in-bone-tumors
#11
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
#12
Shu-Fang Xia, Xiao-Mei Duan, Xiang-Rong Cheng, Li-Mei Chen, Yan-Jun Kang, Peng Wang, Xue Tang, Yong-Hui Shi, Guo-Wei 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 HFD for 7 weeks, OP mice showed apparent hepatic steatosis, with significantly higher body weight and lower hepatic TH 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 When mice were fed for 17 weeks, OR mice had mild hepatic steatosis and increased Dio1 and TRb expression than OP mice, with downregulation of T3 target genes (including Srebp1c, Acc1, Scd1 and Fasn) and upregulation of Cpt1α, Atp5c1, Cox7c and Cyp7a1 A stem-loop qRT-PCR analysis confirmed that the levels of miR-383, miR-34a and miR-146b were inversely correlated with those of DIO1 or TRb...
August 2017: Journal of Endocrinology
https://www.readbyqxmd.com/read/28475135/modulation-of-ho-1-by-ferulic-acid-attenuates-adipocyte-differentiation-in-3t3-l1-cells
#13
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
#14
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
#15
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)...
November 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
#16
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
#17
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
#18
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
#19
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
#20
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
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