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  • Antagonists
  • The ORL-1 Receptor System: Are There Opportunities for Antagonists in Pain Therapy? (ebscohost.com)
  • Side effects are similar to other angiotensin II receptor antagonists and include tachycardia and bradycardia (fast or slow heartbeat), hypotension (low blood pressure), edema (swelling of arms, legs, lips, tongue, or throat, the latter leading to breathing problems), and allergic reactions. (wikipedia.org)
  • peroxisome
  • To address this possibility a reporter gene assay was developed, allowing the high-throughput screening of pollutants for their interactions with piscine NHRs with critical roles in energy homeostasis, stress reponse and immune functions, namely the peroxisome proliferator-activated receptors (PPARs) and corticosteroid receptors (CRs) from European plaice (Pleuronectes platessa) and European flounder (Platichthys flesus), respectively. (bl.uk)
  • The objective of the present study was to investigate the influence of the Pro12Ala polymorphism of the peroxisome proliferator-activated receptor-gamma2 (PPAR-gamma2) gene on serum lipid and lipoprotein responses to n-3 fatty acid supplementation. (biomedsearch.com)
  • Telmisartan's activity at the peroxisome proliferator-activated receptor delta (PPAR-δ) receptor has prompted speculation around its potential as a sport doping agent as an alternative to GW 501516. (wikipedia.org)
  • aldosterone
  • Dystrophy of rat kidney caused by denervation did not affect the binding of 3H-aldosterone with specific receptors of cytoplasm and nuclei in the small tubular cells. (msk.ru)
  • Azhipa Ya.I., Akimov I.A., Rodionov A.A., Neurogenic dystrophy of the rat kidney and interaction of aldosterone with cytoplasmic and nuclear receptors of kidney tubules, Voprosy meditsinskoi khimii, 1985, vol: 31(5), 71-75. (msk.ru)
  • The cell membrane aldosterone receptor has shown to increase the activity of the basolateral Na/K ATPase, ENaC sodium channels and ROMK potassium channels of the principal cell in the distal tubule and cortical collecting duct of nephrons (as well as in the large bowel and possibly in sweat glands). (wikipedia.org)
  • Humans
  • Several fibrates, a group of pharmaceutical compounds used to treat dyslipidemia in humans by targeting the PPARs, were able to activate plaice Gal4-PPARα and Gal4-PPARβ in the reporter gene assay, indicative of an interaction with PPAR receptors in non-target species. (bl.uk)
  • Mice
  • We report on the antiatherogenic properties of the steroidal liver X receptor agonist N,N-dimethyl-3beta-hydroxy-cholenamide (DMHCA) in apolipoprotein E (apoE)-deficient mice. (nih.gov)
  • PPAR
  • Several aquatic pollutants including pharmaceuticals, industrial by-products and biocides were tested for their potential to disrupt PPAR and CR functions by interacting with these receptors in an agonistic or antagonistic manner. (bl.uk)
  • The mechanisms of telmisartan's anti-cancer activity have been found to include up-regulation of proliferator-activated-receptor (PPAR) pathway, Bcl-2, and caspase activation. (wikipedia.org)
  • Some of these receptors such as FXR, LXR, and PPAR bind a number of metabolic intermediates such as fatty acids, bile acids and/or sterols with relatively low affinity. (wikipedia.org)
  • bind
  • Components of the extracellular matrix such as fibronectin and hyaluronan can also bind to such receptors (integrins and CD44, respectively). (wikipedia.org)
  • When such chemical signals bind to a receptor, they cause some form of cellular/tissue response, e.g. a change in the electrical activity of a cell. (wikipedia.org)
  • biological
  • They regulate biological events in mammals by acting on nuclear receptors and membrane-bound receptors. (tdl.org)
  • Unique among biological processes, SP release (and expression of its NK1 Receptor (through autocrine, paracrine, and endocrine-like processes)) may not naturally subside in diseases marked by chronic inflammation (including cancer). (wikipedia.org)
  • membranes
  • Membrane receptors may be isolated from cell membranes by complex extraction procedures using solvents, detergents, and/or affinity purification. (wikipedia.org)
  • Its receptor - the neurokinin type 1 - is distributed over cytoplasmic and nuclear membranes of many cell types (neurons, glia, endothelia of capillaries and lymphatics, fibroblasts, stem cells, white blood cells) in many tissues and organs. (wikipedia.org)
  • Substance
  • Substance P and the NK1 receptor are widely distributed in the brain and are found in brain regions that are specific to regulating emotion (hypothalamus, amygdala, and the periaqueductal gray). (wikipedia.org)
  • It has been shown that vasodilatation to substance P is dependent on the NK1 receptor located on the endothelium. (wikipedia.org)
  • assays
  • TRalpha export is not sensitive to treatment with the CRM1-specific inhibitor leptomycin B (LMB) in heterokaryon assays, suggesting a role for an export receptor other than CRM1. (nih.gov)
  • Here, we have used a combined approach of in vivo fluorescence recovery after photobleaching experiments, in vitro permeabilized cell nuclear export assays, and glutathione S-transferase pull-down assays to investigate the export pathway used by TRalpha. (nih.gov)
  • We have used a combination of in vivo FRAP experiments, in vitro digitonin-permeabilized cell nuclear export assays of transiently transfected cells, and GST pull-down assays to investigate aspects of TRα subcellular trafficking. (nih.gov)
  • affinity
  • Telmisartan is an angiotensin II receptor blocker that shows high affinity for the angiotensin II receptor type 1 (AT1), with a binding affinity 3000 times greater for AT1 than AT2. (wikipedia.org)
  • pathway
  • A, nuclear export complex in cells expressing CRT (HeLa, crt+/+) in which CRT binding promotes a cooperative export pathway involving CRM1. (nih.gov)
  • D, crt-/- cells do not support nuclear export of TRα because CRT is not present to facilitate the CRM1-dependent component of the export pathway. (nih.gov)
  • Thus, CRT may be the most important component of the TRα nuclear export pathway. (nih.gov)
  • The changes elicited by ligand binding (or signal sensing) in a receptor give rise to a signaling cascade, which is a chain of biochemical events along a signaling pathway. (wikipedia.org)
  • citation needed] Each receptor is linked to a specific cellular biochemical pathway. (wikipedia.org)
  • interactions
  • Complementary DNA (cDNA) sequences encoding the ligand-binding domains of PPARs and CRs, critical for receptor-ligand interactions and receptor activation, were ligated to the DNA-binding domain (DBD) of the yeast Gal4 transcription activator protein to create experimental expression plasmid constructs. (bl.uk)
  • and, depending on these interactions, it can modify the binding/activity of the receptor. (wikipedia.org)
  • genes
  • Many of these regulated genes are associated with various diseases, which explains why the molecular targets of approximately 13% of U.S. Food and Drug Administration (FDA) approved drugs target nuclear receptors. (wikipedia.org)
  • pore
  • An important aspect of the shuttling activity of TRalpha is its ability to exit the nucleus through the nuclear pore complex. (nih.gov)
  • The virus exits the host cell by nuclear pore export, and tubule-guided viral movement. (wikipedia.org)
  • Expression
  • A-C, Confocal fluorescence microscopy of AR-V4 and AR-V6 subcellular localization when expressed alone ( A ) or when coexpressed with AR-V7 in PC-3 cells ( B and C ). Right ( B and C ), quantitation of the percentage of nuclear AR-V4 or -V6 expression. (aacrjournals.org)
  • Bottom, quantitation of the percentage of nuclear AR-FL, AR-V4, or AR-V6 expression. (aacrjournals.org)
  • 520:163-175 Psyrri A, Yu Z, Weinberger PM: Quantitative Determination of nuclear and cytoplasmic epidermal growth factor receptor expression in oropharyngeal squamous cell cancer by using automated quantitative analysis. (wikipedia.org)
  • Other nuclear receptors, such as CAR and PXR appear to function as xenobiotic sensors up-regulating the expression of cytochrome P450 enzymes that metabolize these xenobiotics. (wikipedia.org)
  • activation
  • We review factors known to control these processes with an emphasis on nuclear receptor activation as one signaling control that may be abnormal and contribute to increased brain volume in autistic disorders. (nih.gov)
  • and, activation of these receptors results in changes in ion movement across a membrane. (wikipedia.org)
  • Nuclear receptors are modular in structure and contain the following domains: (A-B) N-terminal regulatory domain: Contains the activation function 1 (AF-1) whose action is independent of the presence of ligand. (wikipedia.org)