Browse Items · NEOMED Bibliography Database

Identification of novel pathways that control farnesoid X receptor-mediated hypocholesterolemia.

Farnesoid X receptor (FXR) plays important regulatory roles in bile acid, lipoprotein, and glucose homeostasis. Here, we have utilized Fxr(-/-) mice and mice deficient in scavenger receptor class B type I (SR-BI), together with an

Glucose and insulin induction of bile acid synthesis: mechanisms and implication in diabetes and obesity.

Bile acids facilitate postprandial absorption of nutrients. Bile acids also activate the farnesoid X receptor (FXR) and the G protein-coupled receptor TGR5 and play a major role in regulating lipid, glucose, and energy metabolism. Transgenic…

Farnesoid X receptor induces Takeda G-protein receptor 5 cross-talk to regulate bile acid synthesis and hepatic metabolism.

The bile acid-activated receptors, nuclear farnesoid X receptor (FXR) and the membrane Takeda G-protein receptor 5 (TGR5), are known to improve glucose and insulin sensitivity in obese and diabetic mice. However, the metabolic roles of these two…

Effect of aging on the substance P receptor, NK-1, in the spinal cord of rats with peripheral nerve injury.

Substance P (SP) levels in the spinal cords of very old rats are less than the levels in younger rats (Bergman et al., 1996). After injury to a peripheral nerve in young rats, immunoreactivity (ir) to the SP receptor, NK-1 (neurokinin-1), increases…

Bile acids as metabolic regulators.

PURPOSE OF REVIEW: This review focuses on the latest understanding of the molecular mechanisms underlying the complex interactions between intestine and liver bile acid signaling, gut microbiota, and their impact on whole-body lipid, glucose and…

Two GABAA responses with distinct kinetics in a sound localization circuit.

The temporal characteristics and functional diversity of GABAergic inhibition are determined by the spatiotemporal neurotransmitter profile, intrinsic properties of GABAA receptors, and other factors. Here, we report two distinct GABAA responses and…

Tags: *Sound, 2012, Animals, Chick Embryo, Chickens, Department of Anatomy & Neurobiology, Female, GABA-A/*physiology, gamma-Aminobutyric Acid/metabolism, Lu Yong, Male, NEOMED College of Medicine, Neurons/*metabolism, Pitch Discrimination, Receptors, Sound Localization/*physiology, Synapses/physiology, Tang Zheng-Quan, The Journal of physiology

Rifampicin induction of CYP3A4 requires pregnane X receptor cross talk with hepatocyte nuclear factor 4alpha and coactivators, and suppression of small heterodimer partner gene expression.

Bile acids and drugs activate pregnane X receptor (PXR) to induce CYP3A4, which is the predominant cytochrome P450 enzyme expressed in the liver and intestine and plays a critical role in detoxifying bile acids and drugs, and protecting against…

Tags: 2006, Antibiotics, Antitubercular/*pharmacology, Blotting, Cell Line, Chiang John Y L, Chromatin/metabolism, Cytochrome P-450 CYP3A, Cytochrome P-450 Enzyme System/*biosynthesis, Cytoplasmic and Nuclear/*biosynthesis/*drug effects/genetics, Department of Integrative Medical Sciences, Drug metabolism and disposition: the biological fate of chemicals, Electrophoretic Mobility Shift Assay, Enzyme Induction/drug effects, Glutathione Transferase/metabolism, Hepatocyte Nuclear Factor 4/genetics/*metabolism, Hepatocytes/drug effects/metabolism, Humans, Immunoprecipitation, Li Tiangang, Messenger/biosynthesis, NEOMED College of Medicine, Plasmids/genetics, Pregnane X Receptor, Receptor Cross-Talk/drug effects, Receptors, Reverse Transcriptase Polymerase Chain Reaction, Rifampin/*pharmacology, RNA, Steroid/*drug effects/genetics, Transfection, Tumor, Western

Mechanism of vitamin D receptor inhibition of cholesterol 7alpha-hydroxylase gene transcription in human hepatocytes.

Lithocholic acid (LCA) is a potent endogenous vitamin D receptor (VDR) ligand. In cholestasis, LCA levels increase in the liver and intestine. The objective of this study is to test the hypothesis that VDR plays a role in inhibiting cholesterol…

Farnesoid X Receptor Agonist Represses Cytochrome P450 2D6 Expression by Upregulating Small Heterodimer Partner.

Cytochrome P450 2D6 (CYP2D6) is a major drug-metabolizing enzyme responsible for eliminating approximately 20% of marketed drugs. Studies have shown that differential transcriptional regulation of CYP2D6 may contribute to large interindividual…

A novel mechanism of neurokinin-1 receptor resensitization.

Prolonged or repeated activation of many G protein-coupled receptors induces rapid desensitization followed by a period during which receptors are resensitized. In this study, concanavalin A (Con A) and monensin were used to investigate the…

Tags: 2002, Animals, Bennett V J, Cell Membrane/drug effects/metabolism, CHO Cells, Concanavalin A/pharmacology, Cricetinae, Monensin/pharmacology, Neurokinin-1/*agonists/*metabolism, Perrine S A, Phosphorylation/drug effects, Rats, Receptors, Simmons M A, The Journal of pharmacology and experimental therapeutics

Activation of metabotropic glutamate receptor 1 dimers requires glutamate binding in both subunits.

Group I metabotropic glutamate receptors (mGluRs) form stable, disulfide-linked homodimers. Lack of a verifiably monomeric mGluR1 mutant has led to difficulty in assessing the role of dimerization in the molecular mechanism of mGluR1 activation. The…

Neurokinin-1 receptor resensitization precedes receptor recycling.

Following agonist binding, neurokinin-1 receptors undergo rapid desensitization followed by internalization and recycling. Desensitization requires receptor phosphorylation but does not require internalization, whereas resensitization is thought to…

Tags: 2005, Adenosine Triphosphate/pharmacology, Animals, Bennett V J, Binding, Calcium/metabolism, CHO Cells, Competitive, Cricetinae, Guanylyl Imidodiphosphate/pharmacology, Neurokinin-1/*metabolism, Perrine S A, Phosphorylation, Rats, Receptors, Simmons M A, Substance P/metabolism, The Journal of pharmacology and experimental therapeutics

Functional selectivity of NK1 receptor signaling: peptide agonists can preferentially produce receptor activation or desensitization.

A cascade of events follows binding of an agonist ligand to the tachykinin NK(1) receptor. These events include activation of multiple signal transduction pathways as well as cellular modulation of receptor function by the process of desensitization.…

Tags: 2006, Animals, CHO Cells, Cricetinae, Dose-Response Relationship, Drug, Humans, Neurokinin-1/agonists/drug effects/*physiology, Rana catesbeiana, Rats, Receptors, Signal Transduction/*physiology, Simmons Mark A, Substance P/metabolism/pharmacology, Tachykinins/metabolism/pharmacology, The Journal of pharmacology and experimental therapeutics

A noninflammatory interleukin-1beta fragment stimulates fetal lung fluid absorption in guinea pigs.

We have previously demonstrated that full-length interleukin (IL)-1beta can induce and stimulate lung fluid absorption in near-term guinea pig fetuses via stimulation of fetal cortisol synthesis and release. To develop a potentially clinically useful…

Functional selectivity, ligand-directed trafficking, conformation-specific agonism: what's in a name?

Research on the design of compounds to selectively affect specific subsets of signals downstream of receptors has burgeoned lately, and several reports discussed at Experimental Biology 2005 indicate progress is being made in the understanding of…

Tags: 2005, G-Protein-Coupled/*agonists/*chemistry, Humans, Ligands, Molecular Conformation, Molecular interventions, Protein Transport, Receptors, Signal Transduction, Simmons Mark A

Let's go rafting: ligand functional selectivity may depend on membrane structure.

Tags: 2008, Animals, Humans, Ligands, Membrane Microdomains/*chemistry/*metabolism, Molecular interventions, mu/metabolism, Opioid, Receptors, Signal Transduction, Simmons Mark A

Specificity of metabotropic glutamate receptor 2 coupling to G proteins.

Metabotropic glutamate receptor 2 (mGluR2) is a class 3 G protein-coupled receptor and an important mediator of synaptic activity in the central nervous system. Previous work demonstrated that mGluR2 couples to pertussis toxin (PTX)-sensitive G…

Bile acid signaling in metabolic disease and drug therapy.

Bile acids are the end products of cholesterol catabolism. Hepatic bile acid synthesis accounts for a major fraction of daily cholesterol turnover in humans. Biliary secretion of bile acids generates bile flow and facilitates hepatobiliary secretion…

Estrogen-related receptor gamma controls hepatic CB1 receptor-mediated CYP2E1 expression and oxidative liver injury by alcohol.

BACKGROUND: The hepatic endocannabinoid system and cytochrome P450 2E1 (CYP2E1), a key enzyme causing alcohol-induced reactive oxygen species (ROS) generation, are major contributors to the pathogenesis of alcoholic liver disease. The nuclear hormone…

Tags: 2013, Alcohol-Induced Injury, Alcoholic Liver Disease, Alcoholic/genetics/*metabolism/prevention & control, Animals, Cannabinoid, CB1/*physiology, Chiang John Y L, Choi Hueng-Sik, Cytochrome P-450 CYP2E1 Inhibitors, Cytochrome P-450 CYP2E1/genetics/*metabolism, Department of Integrative Medical Sciences, Enzyme Inhibitors/pharmacology/therapeutic use, Enzymologic/drug effects/physiology, Estrogen/deficiency/genetics/*physiology, Ethanol/pharmacology, Gene Expression Profiling/methods, Gene Expression Regulation, Gene Regulation, Genetic/physiology, Gut, Inbred C57BL, Jang Hyun-Hee, Jeong Won-Il, Kim Don-Kyu, Kim Jung Ran, Kim Yong-Hoon, Knockout, Koh Minseob, Koo Seung-Hoi, Lee Chul-Ho, Liver, Liver Diseases, Liver Metabolism, Liver/metabolism, Male, Mice, NEOMED College of Medicine, Oxidation-Reduction, Oxidative Stress/physiology, Park Jinyoung, Park Seung Bum, Park Tae-Sik, Receptor, Receptors, Signal Transduction/drug effects/physiology, Tamoxifen/analogs & derivatives/pharmacology/therapeutic use, Transcription, Yun Chul-Ho

Mechanism of rifampicin and pregnane X receptor inhibition of human cholesterol 7 alpha-hydroxylase gene transcription.

Bile acids, steroids, and drugs activate steroid and xenobiotic receptor pregnane X receptor (PXR; NR1I2), which induces human cytochrome P4503A4 (CYP3A4) in drug metabolism and cholesterol 7 alpha-hydroxylase (CYP7A1) in bile acid synthesis in the…

Enhanced ethanol catabolism in orphan nuclear receptor SHP-null mice.

Deficiency of the orphan nuclear hormone receptor small heterodimer partner (SHP, NR0B2) protects mice from diet-induced hepatic steatosis, in part, via repression of peroxisome proliferator-activated receptor (PPAR)-gamma2 (Pparg2) gene expression.…

Bile acid regulation of hepatic physiology: III. Bile acids and nuclear receptors.

Bile acids are physiological detergents that facilitate excretion, absorption, and transport of fats and sterols in the intestine and liver. Recent studies reveal that bile acids also are signaling molecules that activate several nuclear receptors…

Tags: 2003, American journal of physiology. Gastrointestinal and liver physiology, Animals, Bile Acids and Salts/biosynthesis/genetics/*physiology, Bile/*physiology, Cardiovascular Diseases/genetics/physiopathology, Chiang John Y L, Cholesterol/physiology, Cytoplasmic and Nuclear/*physiology, Department of Integrative Medical Sciences, Feedback/physiology, Gene Expression Regulation/physiology, Humans, Liver Diseases/genetics/physiopathology, Liver/*physiology, NEOMED College of Medicine, Receptors

Early upregulation of myocardial CXCR4 expression is critical for dimethyloxalylglycine-induced cardiac improvement in acute myocardial infarction.

The stromal cell-derived factor-1 (SDF-1):CXCR4 is important in myocardial repair. In this study we tested the hypothesis that early upregulation of cardiomyocyte CXCR4 (CM-CXCR4) at a time of high myocardial SDF-1 expression could be a strategy to…

Tags: 2016, alpha Subunit/metabolism, American journal of physiology. Heart and circulatory physiology, Amino Acids, Animal, Animals, Apoptosis/drug effects, Cardiotonic Agents/*pharmacology, Cell Hypoxia, Cell Line, Chilian William M, CXCR4/deficiency/genetics/*metabolism, Department of Integrative Medical Sciences, Dicarboxylic/*pharmacology, Disease Models, Dong Feng, Enzyme Inhibitors/pharmacology, Forudi Farhad, hypoxia, Hypoxia-Inducible Factor 1, Hypoxia-Inducible Factor-Proline Dioxygenases/antagonists & inhibitors/metabolism, Inbred C57BL, Kiedrowski Matthew, Knockout, Left/*drug effects, Mayorga Mari, Mice, myocardial infarction, Myocardial Infarction/*drug therapy/genetics/metabolism/pathology/physiopathology, Myocardium/*metabolism/pathology, NEOMED College of Medicine, Penn Marc S, Rats, Receptors, Recovery of Function, Shamhart Patricia, Signal Transduction/drug effects, stem cells, Stem Cells/drug effects/metabolism, Stroke Volume/drug effects, Time Factors, Up-Regulation, Ventricular Function, Weber Kristal

Impaired alveolar liquid clearance after 48-h isoproterenol infusion spontaneously recovers by 96 h of continuous infusion.

We previously demonstrated that 48-h isoproterenol (Iso) infusion in rats impaired the ability of beta-adrenoceptor (beta-AR) agonists to increase alveolar liquid clearance (ALC). In this study, we determined whether this impairment persisted over…

Postreceptor defects in alveolar epithelial beta-adrenergic signaling after prolonged isoproterenol infusion.

We previously found that prolonged isoproterenol (Iso) infusion in rats impaired the ability of beta-adrenoceptor (beta-AR) agonists to increase alveolar liquid clearance (ALC). Here, we determined if postreceptor defects in beta-AR signaling…

Prolonged isoproterenol infusion impairs the ability of beta(2)-agonists to increase alveolar liquid clearance.

We determined if prolonged isoproterenol (Iso) infusion in rats impaired the ability of the beta(2)-adrenergic agonist terbutaline to increase alveolar liquid clearance (ALC). We infused rats with Iso (at rates of 4, 40, or 400 microg.kg(-1).h(-1))…

Beta-adrenoceptor stimulation of alveolar fluid clearance is increased in rats with heart failure.

The alveolar epithelium plays a critical role in resolving pulmonary edema. We thus hypothesized that its function might be upregulated in rats with heart failure, a condition that severely challenges the lung's ability to maintain fluid balance.…

Reduced vascular responsiveness after a single bout of dynamic exercise in the conscious rabbit.

We measured agonist-induced changes in the iliac artery blood flow velocity (IFV) independent of baroreflex-mediated compensatory mechanisms in chronically instrumented New Zealand White rabbits (n = 8). Animals were instrumented with a Doppler flow…

Effect of epinephrine on alveolar liquid clearance in the rat.

Endogenous epinephrine has been found to increase alveolar liquid clearance (ALC) in several pulmonary edema models. In this study, we infused epinephrine intravenously for 1 h in anesthetized rats to produce plasma epinephrine concentrations…

Glycinergic inhibition creates a form of auditory spectral integration in nuclei of the lateral lemniscus.

For analyses of complex sounds, many neurons integrate information across different spectral elements via suppressive effects that are distant from the neurons' excitatory tuning. In the mustached bat, suppression evoked by sounds within the first…

Endogenous mGluR activity suppresses GABAergic transmission in avian cochlear nucleus magnocellularis neurons.

GABAergic transmission in the avian cochlear nucleus magnocellularis (NM) of the chick is subject to modulation by gamma-aminobutyric acid type B (GABA(B)) autoreceptors. Here, I investigated modulation of GABAergic transmission in NM by metabotropic…

Tags: 2-Amino-5-phosphonovalerate/pharmacology, 2007, Amino Acids/pharmacology, Animals, Chickens/*physiology, Cochlear Nucleus/*cytology/*physiology, Department of Anatomy & Neurobiology, Electric Stimulation, Excitatory Amino Acid Antagonists/pharmacology, Excitatory Postsynaptic Potentials/physiology, GABA-B Receptor Agonists, GABA-B Receptor Antagonists, GABA-B/physiology, gamma-Aminobutyric Acid/*physiology, Glycine/analogs & derivatives/pharmacology, In Vitro Techniques, Journal of neurophysiology, Kinetics, Lu Yong, Membrane Potentials/drug effects, Metabotropic Glutamate/agonists/antagonists & inhibitors/*metabolism/physiology, Models, NEOMED College of Medicine, Neurological, Neurons/*physiology, Patch-Clamp Techniques, Receptors, Resorcinols/pharmacology, Synapses/physiology, Synaptic Transmission/*physiology, Xanthenes/pharmacology

Roles of inhibition in complex auditory responses in the inferior colliculus: inhibited combination-sensitive neurons.

We studied the functional properties and underlying neural mechanisms associated with inhibitory combination-sensitive neurons in the mustached bat's inferior colliculus (IC). In these neurons, the excitatory response to best frequency tones was…

Hyperpolarizing and depolarizing GABAA receptor-mediated dendritic inhibition in area CA1 of the rat hippocampus.

1. gamma-Aminobutyric acidA (GABAA) receptor-mediated inhibition of pyramidal neuron dendrites was studied in area CA1 of the rat hippocampal slice preparation with the use of intracellular and extracellular recording and one-dimensional current…

Role of HCO3- ions in depolarizing GABAA receptor-mediated responses in pyramidal cells of rat hippocampus.

1. Activation of GABAA receptors can produce both hyperpolarizing and depolarizing responses in CA1 pyramidal cells. The hyperpolarizing response is mediated by a Cl- conductance, but the ionic basis of the depolarizing response is not clear. We…

VDCCs and NMDARs underlie two forms of LTP in CA1 hippocampus in vivo.

N-methyl-D-aspartate receptor/channel (NMDAR) and voltage-dependent calcium channel (VDCC) antagonists applied independently reduce the magnitude of long-term potentiation (LTP) in area CA1 of the hippocampal slice preparation. When used in…

Tags: 1999, Animals, Calcium Channel Blockers/*pharmacology, Dizocilpine Maleate/pharmacology, Excitatory Amino Acid Antagonists/*pharmacology, Excitatory Postsynaptic Potentials/drug effects, Hippocampus/*drug effects, Journal of neurophysiology, Long-Evans, Long-Term Potentiation/*drug effects, Male, Membrane Potentials/physiology, Morgan S L, N-Methyl-D-Aspartate/*antagonists & inhibitors, Rats, Receptors, Teyler T J, Verapamil/pharmacology

Electrical stimuli patterned after the theta-rhythm induce multiple forms of LTP.

The induction of long-term potentiation (LTP) by high-frequency stimulation is considered an acceptable model for the study of learning and memory. In area CA1 calcium influx through N-methyl-D-aspartate receptors (NMDARs; nmdaLTP) and/or

Role of the adjacent stroma cells in prostate cancer development and progression: synergy between TGF-beta and IGF signaling.

This review postulates the role of transforming growth factor-beta (TGF-beta) and insulin-like growth factor (IGF-I/IGF-II) signaling in stromal cells during prostate carcinogenesis and progression. It is known that stromal cells have a reciprocal…

Intestinal Farnesoid X Receptor and Takeda G Protein Couple Receptor 5 Signaling in Metabolic Regulation.

Bile acids play a critical role in the regulation of glucose, lipid and energy metabolisms by activating the nuclear bile acid receptor farnesoid X receptor (FXR) and membrane G protein-coupled bile acid receptor-1 (aka takeda G protein couple…

Tags: *Signal Transduction, 2017, Animals, Bile Acids and Salts/biosynthesis/metabolism, Boehme Shannon, Chiang John Y L, Cytoplasmic and Nuclear/*metabolism, Department of Integrative Medical Sciences, Digestive diseases (Basel, Switzerland), Donepudi Ajay, Ferrell Jessica, G-Protein-Coupled/*metabolism, Humans, Intestinal Mucosa/*metabolism, Liu Hailiang, Liver/metabolism, NEOMED College of Medicine, Pathak Preeti, Receptors

Farnesoid X Receptor Activation by Obeticholic Acid Elevates Liver Low-Density Lipoprotein Receptor Expression by mRNA Stabilization and Reduces Plasma Low-Density Lipoprotein Cholesterol in Mice.

Objective- The objective of this study was to determine whether and how activation of farnesoid X receptor (FXR) by obeticholic acid (OCA), a clinical FXR agonist, modulates liver low-density lipoprotein receptor (LDLR) expression under…

Tags: 2018, Arteriosclerosis, thrombosis, and vascular biology, Dong Bin, Human, Kraemer Fredric B, LDL, LDLR protein, Liu Jingwen, Obeticholic acid, Receptors, RNA Stability, Singh Amar Bahadur, untranslated regions, Xu Yanyong, Zhang Yanqiao

Myocardial CXCR4 expression is required for mesenchymal stem cell mediated repair following acute myocardial infarction.

BACKGROUND: Overexpression of stromal cell-derived factor-1 in injured tissue leads to improved end-organ function. In this study, we quantify the local trophic effects of mesenchymal stem cell (MSC) stromal cell-derived factor-1 release on the…

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