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Total 179 results found since Jan 2013.

Atorvastatin Induces FXR and CYP7A1 Activation as a Result of the Sequential Action of PPAR γ/PGC-1α/HNF-4α in Hep3B Cells
CONCLUSIONS: Atorvastatin induces FXR and CYP7A1 activation as a result of sequential action of PPARγ-PGC-1α-HNF-4α in human hepatocytes. We propose that atorvastatin enhances solubility of cholesterol in bile by simultaneously activating of FXR and CYP7A1.PMID:33686046 | DOI:10.4166/kjg.2020.156
Source: Korean J Gastroenter... - March 9, 2021 Category: Gastroenterology Authors: Jin Lee Eun Mi Hong Jang Han Jung Se Woo Park Sang Pyo Lee Dong Hee Koh Hyun Joo Jang Sea Hyub Kae Source Type: research

Inclisiran: First Approval
This article summarizes the milestones in the development of inclisiran leading to this first approval for primary hypercholesterolaemia or mixed dyslipidaemia.
Source: Drugs - February 23, 2021 Category: Drugs & Pharmacology Source Type: research

The growth of siRNA-based therapeutics: updated clinical studies.
Abstract More than two decades after the natural gene-silencing mechanism of RNA interference was elucidated, small interfering RNA (siRNA)-based therapeutics have finally broken into the pharmaceutical market. With three agents already approved and many others in advanced stages of the drug development pipeline, siRNA drugs are on their way to becoming a standard modality of pharmacotherapy. The majority of late-stage candidates are indicated for rare or orphan diseases, whose patients have an urgent need for novel and effective therapies. Additionally, there are agents that have the potential to meet the need of...
Source: Biochemical Pharmacology - January 26, 2021 Category: Drugs & Pharmacology Authors: Zhang MM, Bahal R, Rasmussen TP, Manautou JE, Zhong XB Tags: Biochem Pharmacol Source Type: research

Endothelial Klf2-Foxp1-TGF β signal mediates the inhibitory effects of simvastatin on maladaptive cardiac remodeling
Conclusions: We conclude that cardiac microvasculature ECs are important in the modulation of pressure overload induced maladaptive cardiac remodeling and dysfunction, and the endothelial Klf2-TGFβ1 or Klf2-Foxp1-TGFβ1 pathway mediates the preventive effects of simvastatin. This study demonstrates a novel mechanism of the non-cholesterol lowering effects of simvastatin for HF prevention.
Source: Theranostics - January 15, 2021 Category: Molecular Biology Authors: Hongda Li, Yanfang Wang, Jiwen Liu, Xiaoli Chen, Yunhao Duan, Xiaoyu Wang, Yajing Shen, Yashu Kuang, Tao Zhuang, Brain Tomlinson, Paul Chan, Zuoren Yu, Yu Cheng, Lin Zhang, Zhongmin Liu, Yuzhen Zhang, Zhenlin Zhao, Qi Zhang, Jie Liu Tags: Research Paper Source Type: research

Cholesterol synthesis inhibition promotes axonal regeneration in the injured central nervous system.
Abstract Neuronal regeneration in the injured central nervous system is hampered by multiple extracellular proteins. These proteins exert their inhibitory action through interactions with receptors that are located in cholesterol rich compartments of the membrane termed lipid rafts. Here we show that cholesterol-synthesis inhibition prevents the association of the Neogenin receptor with lipid rafts. Furthermore, we show that cholesterol-synthesis inhibition enhances axonal growth both on inhibitory -myelin and -RGMa substrates. Following optic nerve injury, lowering cholesterol synthesis with both drugs and siRNA-...
Source: Neurobiology of Disease - January 9, 2021 Category: Neurology Authors: Shabanzadeh AP, Charish J, Tassew NG, Farhani N, Feng J, Qin X, Sugita S, Mothe AJ, Wälchli T, Koeberle PD, Monnier PP Tags: Neurobiol Dis Source Type: research

New Trends in Dyslipidemia Treatment.
Abstract Dyslipidemia is one of the most important risk factors for cardiovascular (CV) disease. Statin therapy has dramatically improved CV outcomes and is the backbone of current lipid-lowering therapy, but despite well-controlled low-density lipoprotein cholesterol (LDL-C) levels through statin administration, up to 40% patients still experience CV disease. New therapeutic agents to tackle such residual cholesterol risk by lowering not only LDL-C but triglycerides (TG), TG-rich lipoproteins (TRL), or lipoprotein(a) (Lp(a)) are being introduced. Ezetimibe, proprotein convertase subtilisin/kexin type 9 (PCSK9) mo...
Source: Circulation Journal - November 12, 2020 Category: Cardiology Authors: Jang AY, Lim S, Jo SH, Han SH, Koh KK Tags: Circ J Source Type: research

Simvastatin Suppresses Human Breast Cancer Cell Invasion by Decreasing the Expression of Pituitary Tumor-Transforming Gene 1
Statins, or 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors, have been widely used to lower cholesterol and prevent cardiovascular diseases. Recent preclinical and clinical studies have shown that statins exert beneficial effects in the management of breast cancer, while the underlying mechanisms remain to be elucidated. Herein, we sought to investigate the effect of statins on the expression of pituitary tumor-transforming gene 1 (PTTG1), a critical gene involved in human breast cancer invasion and metastasis. Our results showed that PTTG1 is highly expressed in malignant Hs578T and MDA-MB-231 breast cancer cel...
Source: Frontiers in Pharmacology - November 4, 2020 Category: Drugs & Pharmacology Source Type: research

PCSK9 Inhibition and Atherosclerosis: Current Therapeutic Option and Prospection.
Abstract Low-density lipoprotein cholesterol (LDL-C) is a pivotal factor in atherosclerotic cardiovascular disease (ASCVD), the leading cause of worldwide mortality. The limitations of statin therapy require alternative treatment strategies to achieve target LDL-C level. Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays an important role in LDLR recycling, consequently regulating plasma cholesterol levels. Monoclonal antibodies targeting PCSK9 increased expression of LDLRs at the cell surface and therefore decreased circulating LDL-C. PCSK9 inhibitors have shown great efficacy in reducing plasma LDL-C le...
Source: Mol Biol Cell - July 28, 2020 Category: Molecular Biology Authors: Pandey P, Zhao C, Liu B Tags: Methods Mol Biol Source Type: research

Berberine Promotes OATP1B1 Expression and Rosuvastatin Uptake by Inducing Nuclear Translocation of FXR and LXR α
In conclusion, berberine-induced nuclear translocation of FXR and LXRα could activate OATP1B1 promoter, resulting in enhanced expression of OATP1B1 and increased uptake of rosuvastatin.
Source: Frontiers in Pharmacology - March 26, 2020 Category: Drugs & Pharmacology Source Type: research