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Fasn inhibitors

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https://www.readbyqxmd.com/read/29789508/dual-effects-of-metformin-on-adipogenic-differentiation-of-3t3-l1-preadipocyte-in-ampk-dependent-and-independent-manners
#1
Dian Chen, Ying Wang, Kaikai Wu, Xingya Wang
Metformin has been reported to have body weight lowering effects while treating type 2 diabetes. However, limited studies examined the effects of metformin on adipogenesis in vitro, and available data are inconclusive and contradictory. In this study, we examined the effects of a variety of concentrations of metformin on adipocyte differentiation of 3T3-L1 preadipocytes and found metformin exhibits a dual effect on adipogenesis. Metformin at lower concentrations (1.25⁻2.5 mM) significantly induced adipogenesis while at higher concentrations (5⁻10 mM) metformin significantly inhibited adipogenesis in 3T3-L1 cells...
May 23, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29779975/design-and-synthesis-of-a-series-of-bioavailable-fatty-acid-synthase-fasn-kr-domain-inhibitors-for-cancer-therapy
#2
Tianbao Lu, Carsten Schubert, Maxwell D Cummings, Gilles Bignan, Peter J Connolly, Karine Smans, Donald Ludovici, Michael H Parker, Christophe Meyer, Christian Rocaboy, Richard Alexander, Bruce Grasberger, Sabine De Breucker, Norbert Esser, Erwin Fraiponts, Ron Gilissen, Boudewijn Janssens, Danielle Peeters, Luc Van Nuffel, Peter Vermeulen, James Bischoff, Lieven Meerpoel
We designed and synthesized a new series of fatty acid synthase (FASN) inhibitors with potential utility for the treatment of cancer. Extensive SAR studies led to highly active FASN inhibitors with good cellular activity and oral bioavailability, exemplified by compound 34. Compound 34 is a potent inhibitor of human FASN (IC50  = 28 nM) that effectively inhibits proliferation of A2780 ovarian cells (IC50  = 13 nM) in lipid-reduced serum (LRS). This cellular activity can be rescued by addition of palmitate, consistent with an on-target effect...
May 8, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29751678/-epigallocatechin-3-gallate-synthetic-analogues-inhibit-fatty-acid-synthase-and-show-anticancer-activity-in-triple-negative-breast-cancer
#3
Joan Crous-Masó, Sònia Palomeras, Joana Relat, Cristina Camó, Úrsula Martínez-Garza, Marta Planas, Lidia Feliu, Teresa Puig
(-)-Epigallocatechin 3-gallate (EGCG) is a natural polyphenol from green tea with reported anticancer activity and capacity to inhibit the lipogenic enzyme fatty acid synthase (FASN), which is overexpressed in several human carcinomas. To improve the pharmacological profile of EGCG, we previously developed a family of EGCG derivatives and the lead compounds G28, G37 and G56 were characterized in HER2-positive breast cancer cells overexpressing FASN. Here, diesters G28, G37 and G56 and two G28 derivatives, monoesters M1 and M2, were synthesized and assessed in vitro for their cytotoxic, FASN inhibition and apoptotic activities in MDA-MB-231 triple-negative breast cancer (TNBC) cells...
May 11, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29746884/inhibition-of-cellular-fatty-acid-synthase-impairs-replication-of-budded-virions-of-autographa-californica-multiple-nucleopolyhedrovirus-in-spodoptera-frugiperda-cells
#4
Jingfeng Li, Yu Sun, Yuying Li, Ximeng Liu, Qi Yue, Zhaofei Li
Fatty acid synthase (FASN) catalyzes the synthesis of palmitate, which is required for formation of complex fatty acids and phospholipids that are involved in energy production, membrane remodeling and modification of host and viral proteins. Presently, the roles of cellular fatty acid synthesis pathway in Autographa californica multiple nucleopolyhedrovirus (AcMNPV) infection is not clear. In this study, we found that the transcripts level of fasn was significantly up-regulated at the early stage of AcMNPV infection...
May 7, 2018: Virus Research
https://www.readbyqxmd.com/read/29723075/orlistat-as-a-fasn-inhibitor-and-multitargeted-agent-for-cancer-therapy
#5
Alejandro Schcolnik-Cabrera, Alma Chávez-Blanco, Guadalupe Domínguez-Gómez, Lucia Taja-Chayeb, Rocio Cardenas-Barcenas, Catalina Trejo-Becerril, Enrique Perez-Cardenas, Aurora Gonzalez-Fierro, Alfonso Dueñas-González
Cancer cells have increased glycolysis and glutaminolysis. Their third feature is increased de novo lipogenesis. As such, fatty acid (FA) synthesis enzymes are over-expressed in cancer and their depletion causes antitumor effects. As fatty acid synthase (FASN) plays a pivotal role in this process, it is an attractive target for cancer therapy. Areas covered: This is a review of the lipogenic phenotype of cancer and how this phenomenon can be exploited for cancer therapy using inhibitors of FASN, with particular emphasis on orlistat as a repurposing drug...
May 3, 2018: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/29466694/lipid-pathway-deregulation-in-advanced-prostate-cancer
#6
REVIEW
Laura Galbraith, Hing Y Leung, Imran Ahmad
The link between prostate cancer (PC) development and lipid metabolism is well established, with AR intimately involved in a number of lipogenic processes involving SREBP1, PPARG, FASN, ACC, ACLY and SCD1. Recently, there is growing evidence implicating the role of obesity and peri-prostatic adipose tissue (PPAT) in PC aggressiveness and related mortality, suggesting the importance of lipid pathways in both localised and disseminated disease. A number of promising agents are in development to target the lipogenic axis in PC, and the likelihood is that these agents will form part of combination drug strategies, with targeting of multiple metabolic pathways (e...
May 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29463677/an-unexpected-link-between-fatty-acid-synthase-and-cholesterol-synthesis-in-proinflammatory-macrophage-activation
#7
Richard G Carroll, Zbigniew Zasłona, Silvia Galván-Peña, Emma L Koppe, Daniel C Sévin, Stefano Angiari, Martha Triantafilou, Kathy Triantafilou, Louise K Modis, Luke A O'Neill
Different immune activation states require distinct metabolic features and activities in immune cells. For instance, inhibition of fatty acid synthase (FASN), which catalyzes the synthesis of long-chain fatty acids, prevents the proinflammatory response in macrophages; however, the precise role of this enzyme in this response remains poorly defined. Consistent with previous studies, we found here that FASN is essential for lipopolysaccharide-induced, Toll-like receptor (TLR)-mediated macrophage activation. Interestingly, only agents that block FASN upstream of acetoacetyl-CoA synthesis, including the well-characterized FASN inhibitor C75, inhibited TLR4 signaling, while those acting downstream had no effect...
April 13, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29462818/effects-of-microrna-206-on-osteosarcoma-cell-proliferation-apoptosis-migration-and-invasion-by-targeting-anxa2-through-the-akt-signaling-pathway
#8
Bao-Long Pan, Zong-Wu Tong, Ling Wu, Li Pan, Jun-E Li, You-Guang Huang, Shu-De Li, Shi-Xun Du, Xu-Dong Li
BACKGROUND/AIMS: This study aimed to investigate the mechanism by which microRNA-206 (miR-206) affects the proliferation, apoptosis, migration and invasion of osteosarcoma (OS) cells by targeting ANXA2 via the AKT signaling pathway. METHODS: A total of 132 OS tissues and 120 osteochondroma tissues were examined in this study. The targeting relationship between miR-206 and ANXA2 was verified with a dual-luciferase reporter assay. The miR-206 expression and ANXA2, AKT, PARP, FASN, Survivin, Bax, Mcl-1 and Bcl-1 mRNA and protein expression in the above two groups were examined by qRT-PCR and western blotting...
2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29449326/fatty-acid-synthase-mediates-egfr-palmitoylation-in-egfr-mutated-non-small-cell-lung-cancer
#9
Azhar Ali, Elena Levantini, Jun Ting Teo, Julian Goggi, John G Clohessy, Chan Shuo Wu, Leilei Chen, Henry Yang, Indira Krishnan, Olivier Kocher, Junyan Zhang, Ross A Soo, Kishore Bhakoo, Tan Min Chin, Daniel G Tenen
Metabolic reprogramming is widely known as a hallmark of cancer cells to allow adaptation of cells to sustain survival signals. In this report, we describe a novel oncogenic signaling pathway exclusively acting in mutated epidermal growth factor receptor (EGFR) non-small cell lung cancer (NSCLC) with acquired tyrosine kinase inhibitor (TKI) resistance. Mutated EGFR mediates TKI resistance through regulation of the fatty acid synthase (FASN), which produces 16-C saturated fatty acid palmitate. Our work shows that the persistent signaling by mutated EGFR in TKI-resistant tumor cells relies on EGFR palmitoylation and can be targeted by Orlistat, an FDA-approved anti-obesity drug...
February 15, 2018: EMBO Molecular Medicine
https://www.readbyqxmd.com/read/29407795/beyond-regulation-of-pol-iii-role-of-maf1-in-growth-metabolism-aging-and-cancer
#10
REVIEW
Shanshan Zhang, Xiaoxing Li, Hui-Yun Wang, X F Steven Zheng
MAF1 was discovered as a master repressor of Pol III-dependent transcription in response to diverse extracellular signals, including growth factor, nutrient and stress. It is regulated through posttranslational mechanisms such as phosphorylation. A prominent upstream regulator of MAF1 is the mechanistic target of rapamycin (mTOR) pathway. mTOR kinase directly phosphorylates MAF1, controlling its localization and transcriptional activity. In mammals, MAF1 has also been shown to regulate Pol I- and Pol II-dependent transcription...
April 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29344187/patuletin-induces-apoptosis-of-human-breast-cancer-sk-br-3-cell-line-via-inhibiting-fatty-acid-synthase-gene-expression-and-activity
#11
Wanwan Zhu, Chunmei Lv, Jiao Wang, Qiang Gao, Hui Zhu, Haixia Wen
Fatty acid synthase (FASN) is a key enzyme involved in fatty acid biosynthesis and serves an important role in breast cancer development. The aim of the present study was to investigate the effects of patuletin on the gene expression and activity of FASN in the human breast cancer SK-BR-3 cell line, and the apoptotic effects of patuletin to breast cancer cells. Quantitative reverse transcription polymerase chain reaction, western blotting and intracellular FASN activity assays were used to evaluate FASN gene expression, protein expression and activity in patuletin-treated SK-BR-3 cells...
December 2017: Oncology Letters
https://www.readbyqxmd.com/read/29306075/fasn-tgf-%C3%AE-1-pd-l1-axis-contributes-to-the-development-of-resistance-to-nk-cell-cytotoxicity-of-cisplatin-resistant-lung-cancer-cells
#12
Mingjing Shen, Ying Tsai, Rongying Zhu, Peter C Keng, Yongbing Chen, Yuhchyau Chen, Soo Ok Lee
Cisplatin remains the most effective therapy for non-small cell lung cancer (NSCLC). We previously have found cisplatin-resistant lung cancer cells (A549CisR and H157CisR) were more resistant to natural killer (NK) cell-mediated cytotoxicity than parental cells. We also discovered that fatty acid synthase (FASN) levels in cisplatin-resistant cells were significantly higher than in parental cells. To reveal whether a link exists between the up-regulated FASN levels and higher resistance to NK cell cytotoxicity, we performed inhibition studies using a FASN inhibitor and applied the FASN knockdown approach...
March 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29302209/histone-deacetylase-inhibition-attenuates-hepatic-steatosis-in-rats-with-experimental-cushing-s-syndrome
#13
Mina Kim, Hae-Ahm Lee, Hyun-Min Cho, Seol-Hee Kang, Eunjo Lee, In Kyeom Kim
Cushing's syndrome (CS) is a collection of symptoms caused by prolonged exposure to excess cortisol. Chronically elevated glucocorticoid (GC) levels contribute to hepatic steatosis. We hypothesized that histone deacetylase inhibitors (HDACi) could attenuate hepatic steatosis through glucocorticoid receptor (GR) acetylation in experimental CS. To induce CS, we administered adrenocorticotropic hormone (ACTH; 40 ng/kg/day) to Sprague-Dawley rats by subcutaneous infusion with osmotic mini-pumps. We administered the HDACi, sodium valproate (VPA; 0...
January 2018: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/29282029/docosahexaenoic-acid-reduces-sterol-regulatory-element-binding-protein-1-and-fatty-acid-synthase-expression-and-inhibits-cell-proliferation-by-inhibiting-pakt-signaling-in-a-human-breast-cancer-mcf-7-cell-line
#14
Li-Hsuan Huang, Hsin-Yun Chung, Hui-Min Su
BACKGROUND: Fatty acid synthase (FASN), the major enzyme in de novo fatty acid synthesis, is highly expressed in breast cancer and its expression is reduced by polyunsaturated fatty acids (PUFAs) in liver. We previously found a positive association between rat mammary tumor levels of the n-6 PUFA arachidonic acid (AA) and tumor weight. We examined the roles of the major n-3 PUFA, docosahexaenoic acid (DHA, 22:6n-3), and the major n-6 PUFA, AA, in FASN expression in, and proliferation of, human breast cancer MCF-7 cells...
December 28, 2017: BMC Cancer
https://www.readbyqxmd.com/read/29113229/fatty-acid-synthase-affects-expression-of-erbb-receptors-in-epithelial-to-mesenchymal-transition-of-breast-cancer-cells-and-invasive-ductal-carcinoma
#15
Tingting Chen, Lan Zhou, Hua Li, Yuan Tian, Junqin Li, Lihua Dong, Yuhua Zhao, Dapeng Wei
The aim of the present study was to investigate changes in the expression of ErbBs during epithelial-mesenchymal transition (EMT) of breast cancer cells and its association with the expression of fatty acid synthase (FASN). MCF-7-MEK5 cells were used as the experimental model, while MCF-7 cells were used as a control. Tumor cells were implanted into nude mice for in vivo analysis. Cerulenin was used as a FASN inhibitor. Reverse transcription-polymerase chain reaction and western blot analysis were used to detect expression levels of FASN and ErbB1-4...
November 2017: Oncology Letters
https://www.readbyqxmd.com/read/29112683/targeting-de-novo-lipogenesis-as-a-novel-approach-in-anti-cancer-therapy
#16
Katharina Stoiber, Olga Nagło, Carla Pernpeintner, Siwei Zhang, Andreas Koeberle, Melanie Ulrich, Oliver Werz, Rolf Müller, Stefan Zahler, Theobald Lohmüller, Jochen Feldmann, Simone Braig
BACKGROUND: Although altered membrane physiology has been discussed within the context of cancer, targeting membrane characteristics by drugs being an attractive therapeutic strategy has received little attention so far. METHODS: Various acetyl-CoA carboxylase 1 (ACC1), and fatty acid synthase (FASN) inhibitors (like Soraphen A and Cerulenin) as well as genetic knockdown approaches were employed to study the effects of disturbed phospholipid composition on membrane properties and its functional impact on cancer progression...
January 2018: British Journal of Cancer
https://www.readbyqxmd.com/read/29056532/lamp3-regulates-hepatic-lipid-metabolism-through-activating-pi3k-akt-pathway
#17
Xiaoyu Liao, Lingyu Song, Linlin Zhang, Hui Wang, Qiang Tong, Jing Xu, Gangyi Yang, Shiming Yang, Hongting Zheng
Lysosome associated membrane protein 3 (LAMP3), a highly glycosylated protein, is one member of the LAMPs family. LAMPs family plays a critical role in the autolysosome fusion process. Autophagy was recently confirmed to regulate hepatic lipolysis. However, the physiological function of LAMP3 in lipid metabolism is not clear. In the current study, we discovered that the LAMP3 expression level was higher in the liver tissues of non-alcoholic fatty liver disease (NAFLD) patients and high-fat diet and ob/ob mice than in the matched control groups...
October 19, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28984821/mir-425-5p-inhibits-differentiation-and-proliferation-in-porcine-intramuscular-preadipocytes
#18
Fen-Fen Chen, Yan Xiong, Ying Peng, Yun Gao, Jin Qin, Gui-Yan Chu, Wei-Jun Pang, Gong-She Yang
Intramuscular fat (IMF) content affects the tenderness, juiciness, and flavor of pork. An increasing number of studies are focusing on the functions of microRNAs (miRs) during porcine intramuscular preadipocyte development. Previous studies have proved that miR-425-5p was enriched in porcine skeletal muscles and played important roles in multiple physiological processes; however, its functions during intramuscular adipogenesis remain unclear. To explore the role of miR-425-5p in porcine intramuscular adipogenesis, miR-425-5p agomir and inhibitor were used to perform miR-425-5p overexpression and knockdown in intramuscular preadipocytes, respectively...
October 6, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28962653/cellular-fatty-acid-synthase-is-required-for-late-stages-of-hiv-1-replication
#19
Manjusha M Kulkarni, Annette N Ratcliff, Menakshi Bhat, Yazan Alwarawrah, Philip Hughes, Jesus Arcos, David Loiselle, Jordi B Torrelles, Nicholas T Funderburg, Timothy A Haystead, Jesse J Kwiek
BACKGROUND: Like all viruses, HIV-1 relies on host systems to replicate. The human purinome consists of approximately two thousand proteins that bind and use purines such as ATP, NADH, and NADPH. By virtue of their purine binding pockets, purinome proteins are highly druggable, and many existing drugs target purine-using enzymes. Leveraging a protein affinity media that uses the purine-binding pocket to capture the entire purinome, we sought to define purine-binding proteins regulated by HIV-1 infection...
September 29, 2017: Retrovirology
https://www.readbyqxmd.com/read/28922023/fatty-acid-synthase-fasn-as-a-therapeutic-target-in-breast-cancer
#20
REVIEW
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...
November 2017: Expert Opinion on Therapeutic Targets
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