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Condition: Cholesterol

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Total 21 results found since Jan 2013.

PCSK9 as a new player in cancer: New opportunity or red herring?
Curr Med Chem. 2021 Nov 15. doi: 10.2174/0929867328666211115122324. Online ahead of print.ABSTRACTInitially described as a factor involved in liver regeneration and neuronal differentiation, proprotein convertase subtilisin/kexin type 9 (PCSK9) has become one of the key regulators of low-density lipoprotein cholesterol. Besides that, a number of studies have suggested PCSK9 may play a role in cancer biology. This is particularly true for gastroenteric (gastric and liver cancers) and lung cancers, where higher PCSK9 levels were associated with the increased ability of the tumor to develop and give metastasis as well as with...
Source: Current Medicinal Chemistry - November 16, 2021 Category: Chemistry Authors: Aldo Bonaventura Alessandra Vecchi é Massimiliano Ruscica Francesco Grossi Francesco Dentali Source Type: research

Molecules, Vol. 26, Pages 4626: Cholesterol Sequestration from Caveolae/Lipid Rafts Enhances Cationic Liposome-Mediated Nucleic Acid Delivery into Endothelial Cells
In this study, we demonstrated that the transient modulation of caveolae/lipid rafts mediated endocytosis with the cholesterol-sequestrating agents, nystatin, filipin III, and siRNA against Cav-1, which significantly increased the transfection properties of cationic lipid-(2-hydroxy-N-methyl-N,N-bis(2-tetradecanamidoethyl)ethanaminium chloride), namely, amide liposomes in combination with 1,2-Dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) (AD Liposomes) in liver sinusoidal endothelial cells (SK-Hep1). In particular, nystatin was found to be highly effective with 2–3-fold enhanced transfection efficacy when compared wit...
Source: Molecules - July 30, 2021 Category: Chemistry Authors: Santhosh Chandar Maddila Chandrashekhar Voshavar Porkizhi Arjunan Rashmi Prakash Chowath Hari Krishna Reddy Rachamalla Balaji Balakrishnan Poonkuzhali Balasubramanian Rajkumar Banerjee Srujan Marepally Tags: Article Source Type: research

Molecules, Vol. 26, Pages 2119: A Versatile Solid-Phase Approach to the Synthesis of Oligonucleotide Conjugates with Biodegradable Hydrazone Linker
aminova One of the ways to efficiently deliver various drugs, including therapeutic nucleic acids, into the cells is conjugating them with different transport ligands via labile or stable bonds. A convenient solid-phase approach for the synthesis of 5′-conjugates of oligonucleotides with biodegradable pH-sensitive hydrazone covalent bonds is proposed in this article. The approach relies on introducing a hydrazide of the ligand under aqueous/organic media to a fully protected support-bound oligonucleotide containing aldehyde function at the 5′-end. We demonstrated the proof-of-principle of this approach by synthesiz...
Source: Molecules - April 7, 2021 Category: Chemistry Authors: Mariya I. Meschaninova Nina S. Entelis Elena L. Chernolovskaya Alya G. Venyaminova Tags: Article Source Type: research

Molecules, Vol. 25, Pages 1877: Trimeric Small Interfering RNAs and Their Cholesterol-Containing Conjugates Exhibit Improved Accumulation in Tumors, but Dramatically Reduced Silencing Activity
ernolovskaya Cholesterol derivatives of nuclease-resistant, anti-MDR1 small-interfering RNAs were designed to contain a 2’-OMe-modified 21-bp siRNA and a 63-bp TsiRNA in order to investigate their accumulation and silencing activity in vitro and in vivo. The results showed that increasing the length of the RNA duplex in such a conjugate increases its biological activity when delivered using a transfection agent. However, the efficiency of accumulation in human drug-resistant KB-8-5 cells during delivery in vitro in a carrier-free mode was reduced as well as efficiency of target gene silencing. TsiRNAs dem...
Source: Molecules - April 17, 2020 Category: Chemistry Authors: Ivan V. Chernikov Daniil V. Gladkikh Ulyana A. Karelina Mariya I. Meschaninova Alya G. Ven ’yaminova Valentin V. Vlassov Elena L. Chernolovskaya Tags: Article Source Type: research

Molecules, Vol. 24, Pages 3413: Design of Peptidomimetic Functionalized Cholesterol Based Lipid Nanoparticles for Efficient Delivery of Therapeutic Nucleic Acids
a Baigude Lipid nanoparticles (LNP) are the most potent carriers for the delivery of nucleic acid-based therapeutics. The first FDA approved a short interfering RNA (siRNA) drug that uses a cationic LNP system for the delivery of siRNA against human transthyretin (hTTR). However, preparation of such LNP involves tedious multi-step synthesis with relatively low yields. In the present study, we synthesized cationic peptidomimetic functionalized cholesterol (denote Chorn) in straightforward chemical approaches with high yield. When formulated with helper lipids, Chorn LNPs complexed with siRNA to form nanoparticles with a...
Source: Molecules - September 18, 2019 Category: Chemistry Authors: Ehexige Ehexige Tsogzolmaa Ganbold Xiang Yu Shuqin Han Huricha Baigude Tags: Article Source Type: research

Sterol carrier protein-2 deficiency attenuates diet-induced dyslipidemia and atherosclerosis in mice Metabolism
Intracellular cholesterol transport proteins move cholesterol to different subcellular compartments and thereby regulate its final metabolic fate. In hepatocytes, for example, delivery of high-density lipoprotein (HDL)–associated cholesterol for bile acid synthesis or secretion into bile facilitates cholesterol elimination from the body (anti-atherogenic effect), whereas delivery for esterification and subsequent incorporation into apolipoprotein B–containing atherogenic lipoproteins (e.g. very-low-density lipoprotein (VLDL)) enhances cholesterol secretion into the systemic circulation (pro-atherogenic effect). Intrace...
Source: Journal of Biological Chemistry - June 15, 2018 Category: Chemistry Authors: Hongliang He, Jing Wang, Paul J. Yannie, Genta Kakiyama, William J. Korzun, Shobha Ghosh Tags: Lipids Source Type: research

PCSK9 Inhibitors: Novel Therapeutic Strategies for Lowering LDL-Cholesterol.
Abstract Statins are currently the major therapeutic strategies to lower low-density lipoprotein cholesterol (LDL-C) levels. However, a number of hypercholesterolemia patients still have a residual cardiovascular disease (CVD) risk despite taking the maximum-tolerated dose of statins. Proprotein convertase subtilisin/kexin type 9 (PCSK9) binds to low-density lipoprotein receptor (LDLR), inducing its degradation in the lysosome and inhibiting LDLR recirculating to the cell membranes. The gain-of-function mutations in PCSK9 elevate the LDL-C levels in plasma. Therefore, PCSK9 inhibitors become novel therapeutic appr...
Source: Mini Reviews in Medicinal Chemistry - April 22, 2018 Category: Chemistry Authors: Liu ZP, Wang Y Tags: Mini Rev Med Chem Source Type: research

Rac1 GTPase regulates 11{beta} hydroxysteroid dehydrogenase type 2 and fibrotic remodeling Molecular Bases of Disease
In conclusion, Rac1 GTPase regulates 11β-HSD2 expression, MR activation, and MR-mediated pro-fibrotic signaling.
Source: Journal of Biological Chemistry - May 5, 2017 Category: Chemistry Authors: Daniel Lavall, Pia Schuster, Nadine Jacobs, Andrey Kazakov, Michael Bohm, Ulrich Laufs Tags: Signal Transduction Source Type: research

CCL2 Inhibits HDL Internalization and Cholesterol Efflux Metabolism
In this study, we aim to characterize HDL internalization and cholesterol efflux in ECs and regulatory mechanisms. We found mature HDL particles were reduced in patients with coronary artery disease (CAD), which was associated with an increase in CC-chemokine ligand 2 (CCL2). In cultured primary human coronary artery endothelial cells and human umbilical vein endothelial cells, we determined that CCL2 suppressed the binding (4 °C) and association (37 °C) of HDL to/with ECs and HDL cellular internalization. Furthermore, CCL2 inhibited [3H]cholesterol efflux to HDL/apoA1 in ECs. We further found that CCL2 induced CC-chemok...
Source: Journal of Biological Chemistry - September 8, 2016 Category: Chemistry Authors: Sun, R.-L., Huang, C.-X., Bao, J.-L., Jiang, J.-Y., Zhang, B., Zhou, S.-X., Cai, W.-B., Wang, H., Wang, J.-F., Zhang, Y.-L. Tags: Lipids Source Type: research

CC-Chemokine Ligand 2 (CCL2) Suppresses High Density Lipoprotein (HDL) Internalization and Cholesterol Efflux via CC-Chemokine Receptor 2 (CCR2) Induction and p42/44 Mitogen-activated Protein Kinase (MAPK) Activation in Human Endothelial Cells Metabolism
In this study, we aim to characterize HDL internalization and cholesterol efflux in ECs and regulatory mechanisms. We found mature HDL particles were reduced in patients with coronary artery disease (CAD), which was associated with an increase in CC-chemokine ligand 2 (CCL2). In cultured primary human coronary artery endothelial cells and human umbilical vein endothelial cells, we determined that CCL2 suppressed the binding (4 °C) and association (37 °C) of HDL to/with ECs and HDL cellular internalization. Furthermore, CCL2 inhibited [3H]cholesterol efflux to HDL/apoA1 in ECs. We further found that CCL2 induced CC-chemok...
Source: Journal of Biological Chemistry - September 8, 2016 Category: Chemistry Authors: Run-Lu Sun, Can-Xia Huang, Jin-Lan Bao, Jie-Yu Jiang, Bo Zhang, Shu-Xian Zhou, Wei-Bin Cai, Hong Wang, Jing-Feng Wang, Yu-Ling Zhang Tags: Lipids Source Type: research

HCV-activated NLRP3 Inflammasome Regulates Lipid Metabolism Molecular Bases of Disease
In this study, we elucidate the potential link between chronic hepatitis C-associated inflammation and alteration of lipid homeostasis in infected cells. Our results reveal that the HCV-activated NLRP3 inflammasome is required for the up-regulation of lipogenic genes such as 3-hydroxy-3-methylglutaryl-coenzyme A synthase, fatty acid synthase, and stearoyl-CoA desaturase. Using pharmacological inhibitors and siRNA against the inflammasome components (NLRP3, apoptosis-associated speck-like protein containing a CARD, and caspase-1), we further show that the activation of the NLRP3 inflammasome plays a critical role in lipid d...
Source: Journal of Biological Chemistry - February 12, 2016 Category: Chemistry Authors: McRae, S., Iqbal, J., Sarkar-Dutta, M., Lane, S., Nagaraj, A., Ali, N., Waris, G. Tags: Microbiology Source Type: research

Annexin A6 Modulates Cell Migration Molecular Bases of Disease
Annexins are a family of proteins that bind to phospholipids in a calcium-dependent manner. Earlier studies implicated annexin A6 (AnxA6) to inhibit secretion and participate in the organization of the extracellular matrix. We recently showed that elevated AnxA6 levels significantly reduced secretion of the extracellular matrix protein fibronectin (FN). Because FN is directly linked to the ability of cells to migrate, this prompted us to investigate the role of AnxA6 in cell migration. Up-regulation of AnxA6 in several cell models was associated with reduced cell migration in wound healing, individual cell tracking and thr...
Source: Journal of Biological Chemistry - January 15, 2016 Category: Chemistry Authors: Garcia–Melero, A., Reverter, M., Hoque, M., Meneses–Salas, E., Koese, M., Conway, J. R. W., Johnsen, C. H., Alvarez–Guaita, A., Morales–Paytuvi, F., Elmaghrabi, Y. A., Pol, A., Tebar, F., Murray, R. Z., Timpson, P., Enrich, C., Gre Tags: Cell Biology Source Type: research

Topo II Inhibitors Induce CETP Expression and RCT Gene Regulation
In this study we determined if Topo II activity can influence cholesterol metabolism by regulating hepatic CETP expression. Inhibition of Topo II by etoposide, teniposide, or Topo II siRNA increased CETP expression in human hepatic cell line, HepG2 cells, which was associated with increased CETP secretion and mRNA expression. Meanwhile, inhibition of LXR expression by LXR siRNA attenuated induction of CETP expression by etoposide and teniposide. Etoposide and teniposide induced LXRα expression and LXRα/β nuclear translocation while inhibiting expression of receptor interacting protein 140 (RIP140), an LXR co-repressor. ...
Source: Journal of Biological Chemistry - June 4, 2015 Category: Chemistry Authors: Liu, M., Chen, Y., Zhang, L., Wang, Q., Ma, X., Li, X., Xiang, R., Zhu, Y., Qin, S., Yu, Y., Jiang, X.-c., Duan, Y., Han, J. Tags: Lipids Source Type: research

VDAC2 Regulates Steroidogenesis Membrane Biology
Steroid hormones are essential for carbohydrate metabolism, stress management, and reproduction and are synthesized from cholesterol in mitochondria of adrenal glands and gonads/ovaries. In acute stress or hormonal stimulation, steroidogenic acute regulatory protein (StAR) transports substrate cholesterol into the mitochondria for steroidogenesis by an unknown mechanism. Here, we report for the first time that StAR interacts with voltage-dependent anion channel 2 (VDAC2) at the mitochondria-associated endoplasmic reticulum membrane (MAM) prior to its translocation to the mitochondrial matrix. In the MAM, StAR interacts wit...
Source: Journal of Biological Chemistry - January 28, 2015 Category: Chemistry Authors: Prasad, M., Kaur, J., Pawlak, K. J., Bose, M., Whittal, R. M., Bose, H. S. Tags: Molecular Bases of Disease Source Type: research