Browse Items · NEOMED Bibliography Database

Transcriptional regulation of the human cholesterol 7 alpha-hydroxylase gene (CYP7A) in HepG2 cells.

A stable HepG2 cell line harboring a human cholesterol 7 alpha-hydroxylase (CYP7A) minigene/luciferase reporter gene construct was selected for studying transcriptional regulation of CYP7A gene promoter. Insulin and phorbol

Peroxisome proliferator-activated receptor alpha (PPARalpha) and agonist inhibit cholesterol 7alpha-hydroxylase gene (CYP7A1) transcription.

Fibrates are widely used hypolipidemic drugs that regulate the expression of many genes involved in lipid metabolism by activating the peroxisome proliferator-activated receptor alpha (PPARalpha). The objective of this study was to investigate the…

Tags: *DNA-Binding Proteins, *Regulatory Sequences, 2000, Animals, Anticholesteremic Agents/pharmacology, Basic Helix-Loop-Helix Leucine Zipper Transcription Factors, Binding Sites, Chiang J Y, Cholesterol 7-alpha-Hydroxylase/biosynthesis/*genetics, Clofibric Acid/pharmacology, Cytoplasmic and Nuclear/*agonists, Department of Integrative Medical Sciences, Enzymologic, Gene Expression Regulation, Genes, Genetic, Hepatocyte Nuclear Factor 4, Humans, Journal of lipid research, Liver/metabolism, Marrapodi M, Models, NEOMED College of Medicine, Nucleic Acid, Peroxisome Proliferators/pharmacology, Phosphoproteins/metabolism, Promoter Regions, Protein Binding, Pyrimidines/pharmacology, Rats, Receptors, Reporter, Response Elements, Retinoic Acid/metabolism, Retinoid X Receptors, Species Specificity, Transcription, Transcription Factors/*agonists/metabolism, Transcriptional Activation

Regulation of cholesterol 7alpha-hydroxylase gene (CYP7A1) transcription by the liver orphan receptor (LXRalpha).

The cholesterol 7alpha-hydroxylase gene (CYP7A1) plays an important role in regulation of bile acid biosynthesis and cholesterol homeostasis. Oxysterol receptor, LXR, stimulates, whereas the bile acid receptor, FXR, inhibits CYP7A1 transcription. The…

Analysis of the thymidine kinase of a herpes simplex virus type 1 isolate that exhibits resistance to (E)-5-(2-bromovinyl)-2'-deoxyuridine.

The mechanism responsible for the decreased sensitivity of a clinical herpes simplex virus type 1 (HSV-1) isolate, HSV-145, to (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) was examined. Measurements of 50% inhibitory doses of several drugs…

Transcriptional regulation of the human sterol 12alpha-hydroxylase gene (CYP8B1): roles of heaptocyte nuclear factor 4alpha in mediating bile acid repression.

Sterol 12alpha-hydroxylase catalyzes the synthesis of cholic acid and controls the ratio of cholic acid over chenodeoxycholic acid in the bile. Transcription of CYP8B1 is inhibited by bile acids, cholesterol, and insulin. To study the mechanism of…

Protein thiyl radical mediates S-glutathionylation of complex I.

Complex I is a critical site of O(2)(*-) production and the major host of reactive protein thiols in mitochondria. In response to oxidative stress, complex I protein thiols at the 51- and 75-kDa subunits are reversibly

Tags: *Oxidative Stress, 2012, Amino Acid Motifs, Amino Acid Sequence, Animals, Binding Sites, Cattle, Cell Line, Chen Chwen-Lih, Chen Jingfeng, Chen Yeong-Renn, Cyclic N-Oxides/chemistry/pharmacology, Cysteine/chemistry/*metabolism, Department of Integrative Medical Sciences, Electron Transport Complex I/chemistry/*metabolism, Free radical biology & medicine, Free Radical Scavengers/chemistry/pharmacology, Free Radicals/chemistry/*metabolism, Glutathione/chemistry/*metabolism, Green Kari B, Heart/enzymology/metabolism, Kang Patrick T, Mice, Mitochondria, Models, Molecular, Molecular Sequence Data, Muscle Cells/drug effects/metabolism, NEOMED College of Medicine, Onium Compounds/pharmacology, Peptide Fragments/chemistry, Peptide Mapping, Protein, Rats, Rotenone/pharmacology, Structural Homology, Superoxides/metabolism, Zhang Liwen

Wogonin, a natural flavonoid, intercalates with genomic DNA and exhibits protective effects in IL-1beta stimulated osteoarthritis chondrocytes.

Wogonin has recently been shown to possess anti-inflammatory and chondroprotective properties and is of considerable interest due to its broad pharmacological activities. The present study highlights that Wogonin binds DNA and exerts…

Novel compounds that target lipoprotein lipase and mediate growth arrest in acute lymphoblastic leukemia.

Over the past decade, the therapeutic strategies employed to treat B-precursor acute lymphoblastic leukemia (ALL) have been progressively successful in treating the disease. Unfortunately, the treatment associated dyslipidemia, either acute or…

Tags: *Acute lymphoblastic leukemia, *Cancer, *Co-culture model, *Lipids, *Lipoprotein lipase, *Metabolism, 2018, Amides/chemistry/metabolism/pharmacology, Antineoplastic Agents/*chemistry/metabolism/pharmacology, Binding Sites, Bioorganic & medicinal chemistry letters, Cell Line, Cell Proliferation/drug effects, Coculture Techniques, Department of Pharmaceutical Sciences, Department of Pharmacy Practice, Dyslipidemias/complications/metabolism/pathology, Geldenhuys Werner J, Gibson Laura F, Humans, Lipoprotein Lipase/antagonists & inhibitors/*metabolism, Mesenchymal Stem Cells/cytology/metabolism, Molecular Docking Simulation, Nair Rajesh R, NEOMED College of Graduate Studies, NEOMED College of Pharmacy, Piktel Debbie, Precursor Cell Lymphoblastic Leukemia-Lymphoma/complications/metabolism/pathology, Protein Binding, Protein Structure, Sadana Prabodh, Serum Albumin/chemistry/metabolism, Tertiary, Tumor

3D-QSAR and docking studies of pentacycloundecylamines at the sigma-1 (sigma1) receptor.

Pentacycloundecylamine (PCU) derived compounds have been shown to be promising lead structures for the development of novel drug candidates aimed at a variety of neurodegenerative and psychiatric diseases. Here we show for the first time a 3D…

Tags: *Quantitative Structure-Activity Relationship, 2013, Amines/*chemistry/metabolism, Aza Compounds/chemistry, Binding Sites, Bioorganic & medicinal chemistry letters, Geldenhuys Werner J, Kinetics, Malan Sarel F, Molecular Docking Simulation, Novotny Nicholas, Protein Binding, Protein Structure, Receptors, sigma/*chemistry/metabolism, Tertiary, Van der Schyf Cornelis J

Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson's disease.

A series of compounds related to piperine and antiepilepsirine was screened in a monoamine oxidase A and B assay. Piperine is an alkaloid from the source plant of both black and white pepper grains, Piper nigrum. Piperine has been shown to have a…

Identification of a novel serum and glucocorticoid regulated kinase-1 (SGK1) ligand from virtual screening.

The serum and glucocorticoid regulated kinase-1 (SGK1) is part of the serine/threonine kinase family and has therapeutic potential in several neurodegenerative diseases such as ischemic stroke and Parkinson's disease. Here we use structure-based…

Tags: 2012, Binding Sites, Bioorganic & medicinal chemistry letters, Department of Pharmaceutical Sciences, Department of Pharmacy Practice, Drug Discovery, Geldenhuys Werner J, Humans, Immediate-Early Proteins/*antagonists & inhibitors/chemistry/metabolism, Ligands, Molecular Docking Simulation, NEOMED College of Graduate Studies, NEOMED College of Pharmacy, Protein Kinase Inhibitors/*chemistry/*pharmacology, Protein-Serine-Threonine Kinases/*antagonists & inhibitors/chemistry/metabolism, Sadana Prabodh, Talasila Phani K

3D-Quantitative structure-activity relationship and docking studies of the tachykinin NK3 receptor.

The tachykinin NK(3) receptor (NK(3)R) is a novel drug target for schizophrenia and drug abuse. Since few non-peptide antagonists of this G protein-coupled receptor are available, we have initiated this study to gain a better understanding of the…

Tags: *Quantitative Structure-Activity Relationship, 2011, Binding Sites, Bioorganic & medicinal chemistry letters, Computer Simulation, Drug Design, Geldenhuys Werner J, Humans, Ligands, Models, Molecular, Neurokinin-3/*chemistry/metabolism, Protein Structure, Quinolines/chemistry, Receptors, Simmons Mark A, Tertiary

3-D-QSAR and docking studies on the neuronal choline transporter.

The high affinity neuronal choline transporter (CHT1) is responsible for the uptake of choline into the pre-synaptic terminal of cholinergic neurons. Considering our past experience with modeling the blood-brain barrier choline transporter (BBBCHT)…

Tags: 2010, Allen David D, Binding Sites, Bioorganic & medicinal chemistry letters, Blood-Brain Barrier/metabolism, Computer Simulation, Geldenhuys Werner J, Lockman Paul R, Membrane Transport Proteins/*chemistry/metabolism, Models, Molecular, Neurons/*metabolism, Quantitative Structure-Activity Relationship, Quaternary Ammonium Compounds/chemistry

Multiple binding sites for [125I]RTI-121 and other cocaine analogs in rat frontal cerebral cortex.

In an effort to identify novel binding sites for cocaine and its analogs, we carried out binding studies with the high-affinity and selective ligand [125I]RTI-121 in rat frontal cortical tissue. Very low densities of binding sites were found.…

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