194 results match your criteria fabp4 inhibitor

HDAC inhibitor Trichostatin A suppresses adipogenesis in 3T3-L1 preadipocytes.

Aging (Albany NY) 2021 07 7;13(13):17489-17498. Epub 2021 Jul 7.

Department of Pathology, The Seventh Affiliated Hospital of Sun Yat-Sen University, Shenzhen 518000, Guangdong, China.

Background And Purpose: Obesity is becoming a major global health issue and is mainly induced by the accumulation of adipose tissues mediated by adipogenesis, which is reported to be regulated by peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT enhancer-binding protein α (C/EBPα). Trichostatin A (TSA) is a novel histone deacetylase inhibitor (HDACI) that was recently reported to exert multiple pharmacological functions. The present study will investigate the inhibitory effect of TSA on adipogenesis, as well as the underlying mechanism. Read More

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Exogenous L-carnitine ameliorates burn-induced cellular and mitochondrial injury of hepatocytes by restoring CPT1 activity.

Nutr Metab (Lond) 2021 Jun 24;18(1):65. Epub 2021 Jun 24.

Department of Immunology, School of Basic Medical Sciences of Anhui Medical University, No. 81 Meishan Road, Hefei, 230032, Anhui, China.

Background: Impaired hepatic fatty acid metabolism and persistent mitochondrial dysfunction are phenomena commonly associated with liver failure. Decreased serum levels of L-carnitine, a amino acid derivative involved in fatty-acid and energy metabolism, have been reported in severe burn patients. The current study aimed to evaluate the effects of L-carnitine supplementation on mitochondrial damage and other hepatocyte injuries following severe burns and the related mechanisms. Read More

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Roflumilast Suppresses Adipogenic Differentiation  AMPK Mediated Pathway.

Front Endocrinol (Lausanne) 2021 7;12:662451. Epub 2021 Jun 7.

Department of Endocrine, Xiangyang Central Hospital, Affiliated Hospital of Hubei University of Arts and Science, Xiangyang City, China.

Obesity and related disorders have increasingly become global health problems over the years. In recent years, obesity has been recognized as the most important risk factor for a variety of diseases including cardiovascular diseases, type 2 diabetes, steatohepatitis, and cancer. The medical anti-obesity treatment is to intervene in the metabolic process of adipocytes by suppressing adipogenesis and promoting lipolysis. Read More

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Histone Deacetylase Inhibitor SAHA Induces Expression of Fatty Acid-Binding Protein 4 and Inhibits Replication of Human Cytomegalovirus.

Virol Sin 2021 Jun 22. Epub 2021 Jun 22.

CAS Key Laboratory of Molecular Virology and Immunology, Institute Pasteur of Shanghai, Chinese Academy of Sciences, University of the Chinese Academy of Sciences, Shanghai, 200031, China.

Suberoylanilide hydroxamic acid (SAHA) is a histone deacetylase inhibitor that shows marked efficacy against many types of cancers and is approved to treat severe metastatic cutaneous T-cell lymphomas. In addition to its anticancer activity, SAHA has significant effects on the growth of many viruses. The effect of SAHA on replication of human cytomegalovirus (HCMV) has not, however, been investigated. Read More

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Combined treatment with FABP4 inhibitor ameliorates rosiglitazone-induced liver steatosis in obese diabetic db/db mice.

Basic Clin Pharmacol Toxicol 2021 Sep 15;129(3):173-182. Epub 2021 Jun 15.

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.

Rosiglitazone has been reported to exert dual effects on liver steatosis, and it could exacerbate liver steatosis in obese animal models, which was suggested to be closely related to the elevated hepatic expression of FABP4. This study aimed to investigate whether combined treatment with FABP4 inhibitor I-9 could alleviate rosiglitazone-induced liver steatosis in obese diabetic db/db mice. Male C57BL/KsJ-db/db mice were orally treated with rosiglitazone, rosiglitazone combined with I-9 daily for 8 weeks. Read More

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September 2021

Pre-emptive pharmacological inhibition of fatty acid-binding protein 4 attenuates kidney fibrosis by reprogramming tubular lipid metabolism.

Cell Death Dis 2021 06 3;12(6):572. Epub 2021 Jun 3.

Department of Geriatrics, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.

Kidney fibrosis is a hallmark of chronic kidney disease (CKD) progression that is caused by tubular injury and dysregulated lipid metabolism. Genetic abolition fatty acid-binding protein 4 (FABP4), a key lipid transporter, has been reported to suppress kidney interstitial fibrosis. However, the role and underlying mechanism of chemical inhibition of FABP4 in fibrotic kidney have not been well-documented. Read More

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Tumor resistance to ferroptosis driven by Stearoyl-CoA Desaturase-1 (SCD1) in cancer cells and Fatty Acid Biding Protein-4 (FABP4) in tumor microenvironment promote tumor recurrence.

Redox Biol 2021 07 14;43:102006. Epub 2021 May 14.

Laboratory of Biology of Tumor and Developmental Biology, GIGA Cancer, Liège University, Liège, Belgium; Cancer Metabolism and Tumor Microenvironment Group, GIGA Cancer, Liège University, Liège, Belgium. Electronic address:

Problem: Tumor recurrence is a major clinical issue that represents the principal cause of cancer-related deaths, with few targetable common pathways. Mechanisms by which residual tumors persist and progress under a continuous shift between hypoxia-reoxygenation after neoadjuvent-therapy are unknown. In this study, we investigated the role of lipid metabolism and tumor redox balance in tumor recurrence. Read More

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FABP4 facilitates inflammasome activation to induce the Treg/Th17 imbalance in preeclampsia via forming a positive feedback with IL-17A.

Mol Ther Nucleic Acids 2021 Jun 2;24:743-754. Epub 2021 Apr 2.

Department of Critical Care Medicine, The First Affiliated Hospital of Harbin Medical University, Harbin 150001, Heilongjiang Province, P.R. China.

Preeclampsia (PE) is one of the leading causes of maternal death worldwide. Elevated fatty acid binding protein 4 (FABP4) levels have been observed in patients with PE, however, the mechanism by which FABP4 contributes to the pathogenesis of PE remains unclear. In this study, we compared the levels of FABP4 and cytokines between 20 PE patients and 10 healthy pregnant women by using ELISA, immunohistochemistry (IHC) analysis, and flow cytometry (fluorescence-activated cell sorting, FACS). Read More

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5-Bis-(2,6-difluoro-benzylidene) Cyclopentanone Acts as a Selective 11β-Hydroxysteroid Dehydrogenase one Inhibitor to Treat Diet-Induced Nonalcoholic Fatty Liver Disease in Mice.

Front Pharmacol 2021 12;12:594437. Epub 2021 Apr 12.

Department of Pharmacy, Zhejiang Hospital, Hangzhou, China.

11β-Hydroxysteroid dehydrogenase one is responsible for activating inert glucocorticoid cortisone into biologically active cortisol in humans and may be a novel target for the treatment of nonalcoholic fatty liver disease. A series of benzylidene cyclopentanone derivatives were synthesized, and the selective inhibitory effects on rat, mouse and human 11β-hydroxysteroid dehydrogenase one and two were screened. The most potent compound [5-bis-(2,6-difluoro-benzylidene)-cyclopentanone] (WZS08), was used to treat nonalcoholic fatty liver disease in mice fed a high-fat-diet for 100 days. Read More

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Molecular mechanisms of inhibitor bindings to A-FABP deciphered by using molecular dynamics simulations and calculations of MM-GBSA.

SAR QSAR Environ Res 2021 Apr 3;32(4):293-315. Epub 2021 Mar 3.

School of Science, Shandong Jiaotong University, Jinan, China.

Adipocyte fatty-acid binding protein (A-FABP) plays a central role in many aspects of metabolic diseases. It is an important target in drug design for treatment of FABP-related diseases. In this study, molecular dynamics (MD) simulations followed by calculations of molecular mechanics generalized Born surface area (MM-GBSA) and principal components analysis (PCA) were implemented to decipher molecular mechanism correlating with binding of inhibitors 57Q, 57P and L96 to A-FABP. Read More

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Akebia saponin D ameliorates metabolic syndrome (MetS) via remodeling gut microbiota and attenuating intestinal barrier injury.

Biomed Pharmacother 2021 Jun 27;138:111441. Epub 2021 Feb 27.

Beijing Chao-Yang Hospital, Capital Medical University, Beijing 100020, China. Electronic address:

Metabolic syndrome (MetS) is a complex, multifactorial disease which lead to an increased risk of cardiovascular disease, type 2 diabetes, and stroke. However, selective, and potent drugs for the treatment of MetS are still lacking. Previous studies have found that Akebia saponin D (ASD) has beneficial effects on metabolic diseases such as obesity, atherosclerosis, and non-alcoholic fatty liver disease (NAFLD). Read More

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Single-cell RNA sequencing of preadipocytes reveals the cell fate heterogeneity induced by melatonin.

J Pineal Res 2021 Apr 5;70(3):e12725. Epub 2021 Mar 5.

State Key Laboratory for Conservation and Utilization of Subtropical Agro-Bioresources, Lingnan Guangdong Laboratory of Agriculture, College of Animal Science, South China Agricultural University, Guangzhou, China.

Obesity is a global epidemic health disorder and associated with several diseases. Body weight-reducing effects of melatonin have been reported; however, no investigation toward examining whether the beneficial effects of melatonin are associated with preadipocyte heterogeneity has been reported. In this study, we profiled 25 071 transcriptomes of normal and melatonin-treated preadipocytes using scRNA-seq. Read More

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FABP4 alleviates endoplasmic reticulum stress-mediated ischemia-reperfusion injury in PC12 cells via regulation of PPARγ.

Exp Ther Med 2021 Mar 5;21(3):181. Epub 2021 Jan 5.

Department of Neurology, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 201100, P.R. China.

Ischemic stroke is a life-threatening complication with a high rate of morbidity. Circulating fatty acid binding protein 4 (FABP4) has been reported to be associated with the outcome of acute ischemic stroke. The present study aimed to illustrate the function of FABP4 in ischemic stroke. Read More

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Galectin-1 accelerates high-fat diet-induced obesity by activation of peroxisome proliferator-activated receptor gamma (PPARγ) in mice.

Cell Death Dis 2021 01 11;12(1):66. Epub 2021 Jan 11.

Department of Biochemistry and Molecular Biology, Yonsei University College of Medicine, Seoul, South Korea.

Galectin-1 contains a carbohydrate-recognition domain (CRD) as a member of the lectin family. Here, we investigated whether galectin-1 regulates adipogenesis and lipid accumulation. Galectin-1 mRNA is highly expressed in metabolic tissues such as the muscle and adipose tissues. Read More

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January 2021

Functional inhibition of fatty acid binding protein 4 ameliorates impaired ciliogenesis in GCs.

Biochem Biophys Res Commun 2021 02 5;539:28-33. Epub 2021 Jan 5.

Chemical Genomics Global Research Laboratory, Department of Biotechnology, College of Life Science & Biotechnology, Yonsei University, Seoul, 03722, South Korea. Electronic address:

Ciliogenesis is often impaired in some cancer cells, leading to acceleration of cancer phenotypes such as cell migration and proliferation. From the investigation of primary cilia of 16 gastric cancer cells (GCs), we found that GCs could be grouped into four primary cilia (PC)-positive GCs and 12 PC-negative GCs. The proliferation of the PC-positive GCs was lower than that of PC-negative GCs. Read More

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February 2021

FABP4 inhibitor attenuates inflammation and endoplasmic reticulum stress of islet in leptin receptor knockout rats.

Eur Rev Med Pharmacol Sci 2020 12;24(24):12808-12820

Department of Pathology, Hebei Medical University, Shijiazhuang, Hebei, China.

Objective: Metabolic syndrome is characterized by abdominal obesity, hypertriglyceridemia and hyperglycemia. Fatty acid binding protein 4 (FABP4), as a member of intracellular lipid chaperones, is not only engaged in lipid transport but involved in inflammation and insulin resistance. The present study was to investigate the effects of BMS309403, a specific FABP4 inhibitor, on metabolic syndrome and its possible molecular mechanisms in islets. Read More

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December 2020

D-Mannose Inhibits Adipogenic Differentiation of Adipose Tissue-Derived Stem Cells the miR669b/MAPK Pathway.

Stem Cells Int 2020 10;2020:8866048. Epub 2020 Dec 10.

Laboratory of Tissue Regeneration and Immunology and Department of Periodontics, Beijing Key Laboratory of Tooth Regeneration and Function Reconstruction, School of Stomatology, Capital Medical University, China.

The adipogenic differentiation of adipose tissue-derived stem cells (ADSCs) plays an important role in the process of obesity and host metabolism. D-Mannose shows a potential regulating function for fat tissue expansion and glucose metabolism. To explore the mechanisms through which D-mannose affects the adipogenic differentiation of adipose-derived stem cells , we cultured the ADSCs with adipogenic medium inducement containing D-mannose or glucose as the control. Read More

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December 2020

miR-340-5p inhibits sheep adipocyte differentiation by targeting ATF7.

Anim Sci J 2020 Jan;91(1):e13462

College of Animal Science and Veterinary Medicine, Shanxi Agricultural University, Taigu, China.

Several microRNAs (miRNAs) have been identified to play roles in adipocyte differentiation. However, little is known about their involvement in the differentiation of ovine intramuscular adipocytes. Here, the role of one such miRNA, miR-340-5p, in ovine adipocyte differentiation was investigated. Read More

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January 2020

Autophagy receptor OPTN (optineurin) regulates mesenchymal stem cell fate and bone-fat balance during aging by clearing FABP3.

Autophagy 2020 Nov 4:1-17. Epub 2020 Nov 4.

Department of Orthopedics, Xiangya Hospital, Central South University, Changsha, Hunan, China.

Senile osteoporosis (OP) is often concomitant with decreased autophagic activity. OPTN (optineurin), a macroautophagy/autophagy (hereinafter referred to as autophagy) receptor, is found to play a pivotal role in selective autophagy, coupling autophagy with bone metabolism. However, its role in osteogenesis is still mysterious. Read More

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November 2020

Inhibition of Fatty Acid-Binding Protein 4 Attenuated Kidney Fibrosis by Mediating Macrophage-to-Myofibroblast Transition.

Front Immunol 2020 30;11:566535. Epub 2020 Sep 30.

Division of Nephrology and National Clinical Research Center for Geriatrics, Kidney Research Institute, West China Hospital of Sichuan University, Chengdu, China.

The macrophage-to-myofibroblast transition (MMT) process is an important pathway that contributing to renal interstitial fibrosis (RIF). Fatty acid-binding protein 4 (FABP4) deteriorated RIF via promoting inflammation in obstructive nephropathy. However, the clinical significance of FABP4 in fibrotic kidney disease remains to be determined and little is known of the FABP4 signaling in MMT. Read More

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FABP4 promotes invasion and metastasis of colon cancer by regulating fatty acid transport.

Cancer Cell Int 2020 19;20:512. Epub 2020 Oct 19.

Department of Gastroenterology, Wuxi People's Hospital Affiliated to Nanjing Medical University, 299 Qing Yang Road, Wuxi, 214023 Jiangsu People's Republic of China.

Background: The prognosis of colon cancer is poor for metastasis, while the mechanism, especially adipocytes related, is not yet clear. The purpose of this study is to determine the effects of fatty acid binding protein 4 (FABP4), a transporter for lipids, on colon cancer progression.

Methods: The distribution of lipids and FABP4 was tested in the colon cancer tissues and adjacent normal tissues, and their relationship was also verified in vitro. Read More

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October 2020

Human adipocyte differentiation and composition of disease-relevant lipids are regulated by miR-221-3p.

Biochim Biophys Acta Mol Cell Biol Lipids 2021 01 16;1866(1):158841. Epub 2020 Oct 16.

Minerva Foundation Institute for Medical Research, Biomedicum 2U, Helsinki, Finland; Department of Anatomy, Faculty of Medicine, University of Helsinki, Finland. Electronic address:

MicroRNA-221-3p (miR-221-3p) is associated with both metabolic diseases and cancers. However, its role in terminal adipocyte differentiation and lipid metabolism are uncharacterized. miR-221-3p or its inhibitor was transfected into differentiating or mature human adipocytes. Read More

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January 2021

Independent and Distinct Associations of FABP4 and FABP5 With Metabolic Parameters in Type 2 Diabetes Mellitus.

Front Endocrinol (Lausanne) 2020 23;11:575557. Epub 2020 Sep 23.

Department of Pharmacology and Therapeutics, University of the Ryukyus, Okinawa, Japan.

Among fatty acid-binding proteins (FABPs), secreted forms of FABP4 and FABP5, which are expressed in adipocytes and macrophages, act as bioactive molecules. We investigated concentrations of FABP4 and FABP5 in patients with type 2 diabetes mellitus. As a sub-analysis study of the Randomized Evaluation of Anagliptin vs. Read More

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Proteomic exploration of common pathophysiological pathways in diabetes and cardiovascular disease.

ESC Heart Fail 2020 Oct 13. Epub 2020 Oct 13.

Department of Clinical Sciences, Lund University, Clinical Research Center, Inga Marie Nilssons gata 47, Malmö, 20502, Sweden.

Aims: The epidemiological association between diabetes and cardiovascular disease is well established, but the pathophysiological link is complex and multifactorial. We investigated seven proteins, previously linked to incident diabetes mellitus, and their association with cardiovascular disease and mortality.

Methods And Results: Plasma samples from 1713 individuals from the Swedish population-based Malmö Preventive Project (mean age 67. Read More

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October 2020

Laquinimod Prevents Adipogenesis and Obesity by Down-Regulating PPAR-γ and C/EBPα through Activating AMPK.

ACS Omega 2020 Sep 1;5(36):22958-22965. Epub 2020 Sep 1.

Department of Endocrinology and Metabolism, The First Hospital of Jilin University, Changchun, Jilin 130021, China.

Background And Purpose: obesity is defined as excessive accumulation of adipose tissues and is becoming one of the main global severe public health issues. The present study aims to investigate the anti-adipogenesis of laquinimod and the underlying mechanism.

Methods: a differentiation cocktail was used to differentiate 3T3-L1 cells, and mice were fed with high fat food to establish the obesity animal model. Read More

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September 2020

Pharmacological inhibition of fatty acid-binding protein 4 alleviated kidney inflammation and fibrosis in hyperuricemic nephropathy.

Eur J Pharmacol 2020 Nov 17;887:173570. Epub 2020 Sep 17.

Division of Nephrology and National Clinical Research Center for Geriatrics, Kidney Research Institute, West China Hospital of Sichuan University, Chengdu, 610041, China.

Hyperuricemia is an independent risk factor for chronic kidney disease (CKD). Excessive uric acid (UA) level in the blood leads to hyperuricemic nephropathy (HN), which is characterized by glomerular hypertension, arteriolosclerosis and tubulointerstitial fibrosis. Fatty acid binding protein 4 (FABP4) is a potential mediator of inflammatory responses which contributes to renal interstitial fibrosis. Read More

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November 2020

FABP4 inhibitor BMS309403 protects against hypoxia-induced H9c2 cardiomyocyte apoptosis through attenuating endoplasmic reticulum stress.

J Cell Mol Med 2020 10 7;24(19):11188-11197. Epub 2020 Sep 7.

Department of Cardiovascular Surgery, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, China.

Acute myocardial infarction is characterized by ischaemia-induced cardiomyocyte apoptosis, in which the endoplasmic reticulum (ER) stress plays an important role. The fatty acid-binding protein-4 (FABP4) has been implicated in regulating ER stress and apoptosis. Yet, whether FABP4 is involved in modulating cardiomyocyte apoptosis remains unclarified. Read More

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October 2020

The diabetes medication canagliflozin promotes mitochondrial remodelling of adipocyte via the AMPK-Sirt1-Pgc-1α signalling pathway.

Adipocyte 2020 12;9(1):484-494

Department of Pharmacy, State Key Laboratory of Biotherapy, West China Hospital, Sichuan University . Chengdu China.

The diabetes medication canagliflozin (Cana) is a sodium glucose cotransporter 2 (SGLT2) inhibitor acting by increasing urinary glucose excretion and thus reducing hyperglycaemia. Cana treatment also reduces body weight. However, it remains unclear whether Cana could directly work on adipose tissue. Read More

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December 2020

The role of BAMBI in regulating adipogenesis and myogenesis and the association between its polymorphisms and growth traits in cattle.

Mol Biol Rep 2020 Aug 1;47(8):5963-5974. Epub 2020 Aug 1.

College of Animal Science and Technology, Northwest A & F University, Yangling, 712100, Shaanxi, China.

Bone morphogenic protein and activin membrane-bound inhibitor (BAMBI) is a transmembrane protein that affects the growth, development and muscle regeneration of the body by regulating the TGF-β, BMP and Wnt signaling pathways. Studies have found that BAMBI has important regulatory functions in skeletal muscle and preadipocytes in vivo and in vitro. However, research on this protein in cattle is lacking. Read More

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Bromodomain-containing protein 4 regulates a cascade of lipid-accumulation-related genes at the transcriptional level in the 3T3-L1 white adipocyte-like cell line.

Eur J Pharmacol 2020 Sep 8;883:173351. Epub 2020 Jul 8.

Laboratory of Nutritional Physiology, University of Shizuoka, Graduate School of Nutritional and Environmental Sciences, Shizuoka, Japan.

Our previous study demonstrated that the transfection of a short hairpin (sh)RNA targeting bromodomain-containing protein 4 (BRD4), a member of the bromodomain and extra-terminal (BET) family of proteins, into 3T3-L1 cells, a white adipocyte-like cell line, reduced the expression of insulin sensitivity genes, such as Adipoq, Fabp4, Lpl, Slc2a4 and Dgat1, and that BRD4 directly bound to the Adipoq, Slc2a4 and Lpl genes. In the present study, we aimed to identify other target genes of BRD4 by microarray analysis of Brd4 shRNA- and control shRNA-transfected cells. We found that the expression of many genes related to fat metabolism, and particularly those involved in fat accumulation in the glycolytic pathway, tricarboxylic acid cycle, and triacylglycerol synthesis, such as Dgat2, Gpd1, Acsl1, Pnpla2, Pgkfb3, Pcx, Fasn, Acacb and Cidec, was reduced by Brd4 shRNA transfection 2 and 8 days after the end of adipocyte differentiation. Read More

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September 2020