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  • blood
  • MetS is a highly prevalent condition currently considered to be a constellation of metabolic abnormalities, including blood pressure elevation, abdominal obesity, impaired glucose metabolism and hyperglycemia associated with insulin resistance (IR) [ 1 - 3 ]. (mdpi.com)
  • Conscious 2K1C rats with blood pressure of 150 mm Hg or higher were classified according to their sensitivity to the blood pressure-lowering effect of the angiotensin II antagonist saralasin. (ahajournals.org)
  • losartan
  • Addition of either ramipril or losartan significantly decreased plasma PAI-1 antigen ( P =0.046). (ahajournals.org)
  • However, the effect of losartan on PAI-1 antigen was not sustained throughout the 6-week treatment period, such that there was a significant drug×time interaction ( P =0.043). (ahajournals.org)
  • Irbesartan and losartan have trial data showing benefit in hypertensive patients with type II diabetes,[citation needed] and may delay the progression of diabetic nephropathy. (wikipedia.org)
  • The specific AT1 affinity relates to how specifically attracted the medicine is for the correct receptor, the US FDA PI rates for AT1 affinity are as follows: Losartan 1000-fold Telmisartan 3000-fold Irbesartan 8500-fold Candesartan greater than 10000-fold Olmesartan 12500-fold Valsartan 30000-fold Saprisartan The third area needed to complete the overall efficacy picture of an ARB is its biological half-life. (wikipedia.org)
  • All of the physiological effects of angiotensin II, including release of aldosterone, are antagonized in the presence of losartan. (wikipedia.org)
  • As a result of losartan dosing, plasma renin activity increases due to removal of the angiotensin II feedback. (wikipedia.org)
  • As a specific inhibitor of the urate transporter 1 (SLC22A12, URAT1), losartan blocks the uptake of uric acid into cells, thus leaving more available in the bloodstream to be filtered and excreted by the kidneys. (wikipedia.org)
  • EXP3174 is 10-40 times more potent in blocking AT1 receptors than losartan. (wikipedia.org)
  • tyrosine kinases
  • The activated receptor in turn couples to Gq/11 and thus activates phospholipase C and increases the cytosolic Ca2+ concentrations, which in turn triggers cellular responses such as stimulation of protein kinase C. Activated receptor also inhibits adenylate cyclase and activates various tyrosine kinases. (wikipedia.org)
  • 7 The multiple actions of Ang II, mediated through the AT 1 R, are a result of complex intracellular signaling pathways including stimulation of the phospholipase C/inositol 1,4,5-trisphosphate/diacylglycerol cascade, mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinases, tyrosine kinases, and RhoA/Rho kinase. (ahajournals.org)
  • novel
  • Therefore, the characteristics of AT1R inhibitors could make it a potential novel therapeutics for prevention and treatment of type 2 diabetes. (hindawi.com)
  • mRNA
  • The protein's mRNA has been reported to interact with Mir-132 microRNA as part of an RNA silencing mechanism that reduces receptor expression. (wikipedia.org)
  • A schematic representation of the rat and human AT 1 R genes and their potential to generate AT 1 R mRNA splice variants. (ahajournals.org)
  • 0.05) decrease of AT 1 R mRNA in HUVECs exposed to SS during 3 (6±2% of static control), 6 (4±1%), 12 (4±1%), and 24 hours (15±4%), suggesting a transcriptional downregulation of AT 1 R at length. (ahajournals.org)
  • Exons 1 and 2 encode for 5' untranslated mRNA sequence and exon 3 harbors the entire uninterrupted open reading frame. (wikipedia.org)
  • ARBs
  • To identify new antidiabetic mechanisms of ARBs, we studied the regulation of adiponectin by angiotensin II (Ang II) and different ARBs in murine 3T3-L1 adipocytes and obese Zucker rats. (ahajournals.org)
  • Recently, certain ARBs (irbesartan, telmisartan) were identified as ligands of the peroxisome proliferator-activated receptor (PPAR)γ. (ahajournals.org)
  • Angiotensin II, through AT1 receptor stimulation, is a major stress hormone and, because (ARBs) block these receptors, in addition to their eliciting anti-hypertensive effects, may be considered for the treatment of stress-related disorders. (wikipedia.org)
  • binds
  • The apelin receptor (also known as the APJ receptor) is a G protein-coupled receptor which binds apelin and Apela/ELABELA/Toddler. (wikipedia.org)
  • While it binds to the same receptors as opioid analgesics, TRV734 has very weak β-arrestin recruitment, unlike other available opioids, and produced fewer off-target effects. (wikipedia.org)
  • inhibitor
  • The Survival and Ventricular Enlargement trial revealed that administration of angiotensin-converting enzyme (ACE) inhibitor after myocardial infarction reduced the incidence of recurrence of myocardial infarction. (ahajournals.org)
  • Objective: To evaluate the current use of angiotensin-converting enzyme inhibitor (ACEI) therapy for the treatment of chronic heart failure in elderly nursing home patients. (ebscohost.com)
  • Systolic blood pressure, as well as plasma cholesterol, dimer D, plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) were measured. (ahajournals.org)
  • The combination is sometimes described as an "angiotensin receptor-neprilysin inhibitor" (ARNi). (wikipedia.org)
  • Telmisartan
  • In addition to blocking the RAS, telmisartan acts as a selective modulator of peroxisome proliferator-activated receptor gamma (PPAR-γ), a central regulator of insulin and glucose metabolism. (wikipedia.org)
  • Telmisartan activates PPAR-δ receptors in several tissues. (wikipedia.org)
  • Gene
  • however, it is now believed that there is only one type 1 receptor gene in humans. (wikipedia.org)
  • This review will summarize the transcriptional and posttranscriptional mechanisms by which AT 1 R gene expression is regulated and discuss the pathological relevance of these mechanisms in mediating cardiovascular disease. (ahajournals.org)
  • To initiate the investigations into the mechanisms by which AT 1 R expression is regulated, the AT 1 R gene has been cloned from a variety of species. (ahajournals.org)
  • Uniquely, the rodent genome harbors 2 distinct AT 1 R genes: AT 1A R and AT 1B R. 9-15 The AT 1A R gene has been localized to chromosomes 17 and 13 of the rat and mouse, respectively, whereas the AT 1B R gene has been localized to chromosomes 2 and 3 of the rat and mouse, respectively. (ahajournals.org)
  • 29 The rAT 1B R gene is also composed of 3 exons, with exons 1 and 2 encoding the 5′-UTR and the third exon harboring the ORF. (ahajournals.org)
  • Angiotensin II receptor type 2, also known as the AT2 receptor is a protein that in humans is encoded by the AGTR2 gene. (wikipedia.org)
  • Type-1 angiotensin II receptor-associated protein is a protein that in humans is encoded by the AGTRAP gene. (wikipedia.org)
  • Staphylococcal nuclease domain-containing protein 1 also known as 100 kDa coactivator or Tudor domain-containing protein 11 (TDRD11) is a protein that in humans is encoded by the SND1 gene. (wikipedia.org)
  • protein
  • Angiotensin II receptor type 1 has been shown to interact with Zinc finger and BTB domain-containing protein 16. (wikipedia.org)
  • Belongs to the G-protein coupled receptor 1 family. (abcam.com)
  • The biological responses of Ang II are mediated by its interaction with 2 distinct high-affinity G protein-coupled receptors now designated Ang II type 1 receptor (AT 1 R) and Ang II type 2 receptor. (ahajournals.org)
  • To understand the molecular regulation of the AT 1 R in normal physiology and pathophysiology, methods for sensitive and specific detection of AT 1 R protein are required. (ahajournals.org)
  • For the 3 antibodies tested, Western blots of protein homogenates from wild-type kidneys yielded distinct bands with the expected size range for AT 1 R. In addition, these bands appeared identical in samples from mice lacking 1 or both murine AT 1 R isoforms. (ahajournals.org)
  • The regulation and importance of monocyte chemoattractant protein-1. (semanticscholar.org)
  • Shear-induced downregulation of AT 1 R was abolished by treatment with protein kinase A and G inhibitors or N G -nitro- l -arginine methyl ester (L-NAME). (ahajournals.org)
  • Fittingly, stimulating static HUVECs with an NO donor decreased AT 1 R protein levels. (ahajournals.org)
  • 4-6 In contrast, oscillatory blood flow or low SS induces the expression of adhesion molecules (intracellular adhesion molecule-1, vascular cell adhesion molecule-1), chemokines (monocyte chemoattractant protein-1, interleukins), and growth factors that contribute to leukocyte recruitment and infiltration, 7,8 which constitute the early steps of plaque formation. (ahajournals.org)
  • Simultaneously, significant increased protein levels of IRS-1 (by 85%), IRS-2 (by 95%), PI3K(85) (by 112.5%), and p-Akt2 (by 164%) were found by western blot. (hindawi.com)
  • AGTR2 belongs to a family 1 of G protein-coupled receptors. (wikipedia.org)
  • Once miR-155 pri-miRNA is transcribed, this transcript is cleaved by the nuclear microprocessor complex, of which the core components are the RNase III type endonuclease Drosha and the DiGeorge critical region 8 (DGCR8) protein, to produce a 65 nucleotide stem-loop precursor miRNA (pre-mir-155) (see Figure 2). (wikipedia.org)
  • SND1 also interacts with G3BP (stress granule protein) and AEG-1. (wikipedia.org)
  • miR-802 expression in the kidney is stimulated by a high potassium intake, along with caveolin-1 expression, one of the many miR-802 protein targets. (wikipedia.org)
  • Plasma protein binding is over 99.5%, mainly to albumin and alpha-1-acid glycoprotein. (wikipedia.org)
  • Trevena Inc is a clinical stage biopharmaceutical company, headquartered in Chesterbrook, Pennsylvania, USA, and is involved in the discovery and development of G-protein coupled receptors (GPCR) biased ligands. (wikipedia.org)
  • Trevena's leading drug candidate is Oliceridine (TRV130), a G protein-biased ligand binding to the mu opioid receptor for the intravenous treatment of acute moderate-to-severe post-operative pain. (wikipedia.org)
  • pressor
  • 21 These conclusions were based on the observation that AT 1A R knockout (AT 1 R −/− ) mice were found to exhibit low blood pressure and attenuated Ang II pressor response. (ahajournals.org)
  • vascular smooth
  • 7 Most of the known physiological and pathophysiological effects of Ang II are mediated via the AT 1 R. 1-7 This receptor subtype is expressed in cardiovascular-relevant cell types including vascular smooth muscle cells (VSMCs), endothelial cells, cardiac myocytes, cardiac fibroblasts, and renal mesangial cells. (ahajournals.org)
  • Although preincubation of vascular smooth muscle cells with T0901317 for 30 minutes had no effect on angiotensin II-induced extracellular signal-regulated kinase phosphorylation, phosphorylation of extracellular signal-regulated kinase by angiotensin II was markedly suppressed after 6 hours of preincubation. (ahajournals.org)
  • 1-3 The protective effect of SS is largely attributable to the local release of nitric oxide (NO), an important vasoprotective agent, known to reduce endothelial permeability, leukocyte adhesion, vascular smooth muscle cell proliferation, and thrombosis, while favoring endothelial survival. (ahajournals.org)
  • 16,17 Moreover, the expression of AT 1 R is reduced in vascular smooth muscle cells exposed to an NO donor, 18,19 suggesting that SS may not only modulate the vascular response to Ang II through the opposing effects of NO but may also directly influence AT 1 R expression in vascular cells. (ahajournals.org)
  • Forasartan is a competitive and reversible ARB that competes with the angiotensin II binding site on AT1 and relaxes vascular smooth muscle, resulting in decreased blood pressure. (wikipedia.org)
  • murine
  • For these studies, we carried out Western blotting and immunohistochemistry with kidney tissue from wild-type mice and genetically modified mice lacking the major murine AT 1 R isoform, AT 1A (AT 1A KO), or with combined deficiency of both the AT 1A and AT 1B isoforms (AT 1AB KO). (ahajournals.org)
  • apelin receptor
  • In the present study, we sought to test the hypothesis that the apelin receptor is a dominant negative regulator of AT1. (ahajournals.org)
  • Using co-immunoprecipitation and bioluminescence resonance energy transfer (BRET) techniques, we confirm that the apelin receptor (APJ) and AT1 physically interact to form a heterodimeric complex. (ahajournals.org)
  • ELABELA: a hormone essential for heart development signals via the apelin receptor. (wikipedia.org)
  • hypertrophy
  • Fimasartan has been shown to reduce cardiac hypertrophy, fibrosis, remodelling, and unnecessary cell proliferation via blockage of AT1 activation conceivably through decreased Endothelin 1 production, a result of AT1 activation. (wikipedia.org)
  • regulation
  • 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)
  • ligand
  • In 2011, Treveva received another NIH grant as part of the NIH Blueprint Neurotherapeutics Network, potentially worth up to $10M USD, to support preclinical development of a delta opioid receptor biased ligand for major depressive disorder. (wikipedia.org)
  • Specificity
  • Here, we examined the specificity of a panel of putative AT 1 R antibodies that are commonly used by investigators in the field. (ahajournals.org)
  • Effects
  • 1,2,4,6,7 In addition, AT 1 Rs mediate many of their pathophysiological effects by stimulating reactive oxygen species generation via an reduced nicotinamide-adenine dinucleotide/reduced nicotinamide-adenine dinucleotide phosphate oxidase-dependent mechanism. (ahajournals.org)
  • 1 Ang II exerts its effects through 2 different receptors: angiotensin type-1 (AT1R) and type-2 (AT2R) receptor. (ahajournals.org)
  • The effects of angiotensin II (Ang II) are mediated by Ang II receptors, and so far 2 isoforms, type 1 receptor (AT1R) and type 2 receptor, have been identified. (ahajournals.org)
  • Our results demonstrate that SS may convey some of its atheroprotective effects through downregulation of AT 1 R in endothelial cells. (ahajournals.org)
  • In the present study, we hypothesized that SS may regulate the expression of AT 1 R in endothelial cells (ECs), which could account at least in part for the protective, antiatherogenic effects of SS. (ahajournals.org)
  • Co-expression of miR-802 with caveolin-1 blocks miR-802's upregulatory effects on ROMK channels. (wikipedia.org)
  • 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)
  • cardiac
  • It contributes to the cardiac transient outward potassium current (Ito1), the main contributing current to the repolarizing phase 1 of the cardiac action potential. (wikipedia.org)
  • Binding to beta-1 receptors in the myocardium increases the heart rate and makes contractions more forceful in an attempt to increase cardiac output. (wikipedia.org)
  • serum
  • Components and strategies Cell lifestyle MCF-7 cells had been grown up in DMEM moderate filled with 10% fetal leg serum and 1% penicillin/streptomycin serum as defined (9). (cancercurehere.com)
  • Mutations in this receptor cause familial glucocorticoid deficiency (FGD) type 1, in which patients have high levels of serum ACTH and low levels of cortisol. (wikipedia.org)
  • cytokine
  • Via genomic and faster non-genomic pathways, this causes, among other immune responses, a reduction in leukocyte and neutrophil infiltration, cytokine production, especially of cytokine CXCL-1, and increased phagocytosis of apoptotic neutrophils. (wikipedia.org)
  • adrenal
  • ACTH receptor is primarily found in the zona fasciculata of the human adrenal cortex. (wikipedia.org)
  • By the 1890s, the profound effect of adrenal extracts on many different tissue types had been discovered, setting off a search both for the mechanism of chemical signalling and efforts to exploit these observations for the development of new drugs. (wikipedia.org)
  • tissues
  • Viral tropism for the decidua and placenta is then dependent on viral entry receptor expression in these tissues as well as on the maternal immune response to the virus. (jci.org)
  • miRNA research revealed different sets of miRNAs expressed in different cell types and tissues and multiple roles for miRNAs in plant and animal development and in many other biological processes. (wikipedia.org)
  • genes
  • However, with exposure to constant light, the rhythmic expression of the ACTH receptor and MRAP genes reversed, suggesting ACTH-independent signalling pathways for MRAP and ACTH receptor transcription and expression. (wikipedia.org)
  • The human genome may encode over 1000 miRNAs, which are abundant in many mammalian cell types and appear to target about 60% of the genes of humans and other mammals. (wikipedia.org)
  • commonly
  • Fyn is located downstream of several cell surface receptors, commonly associated with neuronal development and T-cell signaling. (wikipedia.org)
  • deficiency
  • The corticosterone methyl oxidase deficiencies both share this effect however type I causes an overall deficiency of 18-hydroxycorticosterone while type II overproduces it. (wikipedia.org)
  • decrease
  • Fenoldopam causes arterial/arteriolar vasodilation leading to a decrease in blood pressure by activating peripheral D1 receptors. (wikipedia.org)
  • primarily
  • Lipolytic activity due to melanocortin receptors has been demonstrated in several types of test animals: rats and hamsters primarily respond to ACTH, rabbits respond to alpha and beta MSH's (therefore not using the ACTH receptor), and guinea pigs responding to both ACTH and other MSH's. (wikipedia.org)
  • lysosomal
  • In rat hepatic cells, LIMP-2 exhibited a half-life for internalization and lysosomal transport of 32 min and 2.0 h, respectively, which resembled that of well-known lysosomal proteins, lamp-1 and lamp-2, albeit different amino acid sequences in their cytoplasmic tails. (wikipedia.org)
  • calcium
  • Fluorescent strength of calcium mineral green-1 Rabbit polyclonal to PLS3 was assessed with an individual wavelength excitation at 488 nm and emission at 528 nm. (cancercurehere.com)
  • transcription
  • AP-1 was first discovered as a TPA-activated transcription factor that bound to a cis-regulatory element of the human metallothionein IIa (hMTIIa) promoter and SV40. (wikipedia.org)
  • AP-1 transcription factor is assembled through the dimerization of a characteristic bZIP domain (basic region leucine zipper) in the Fos and Jun subunits. (wikipedia.org)
  • AP-1 transcription factor has been shown to have a hand in a wide range of cellular processes, including cell growth, differentiation, and apoptosis. (wikipedia.org)
  • Below are some of the other important functions and biological roles AP-1 transcription factors have been shown to be involved in. (wikipedia.org)
  • The AP-1 transcription factor has been shown to play numerous roles in cell growth and proliferation. (wikipedia.org)
  • AP-1 transcription factor is associated with a broad range of apoptosis related interactions. (wikipedia.org)
  • cellular
  • AP-1 controls a number of cellular processes including differentiation, proliferation, and apoptosis. (wikipedia.org)
  • The growth factors TGF alpha, TGF beta, and IL2 have all been shown to stimulate c-Fos, and thereby stimulate cellular proliferation via AP-1 activation. (wikipedia.org)
  • viruses
  • This virus is part of the Alphacoronavirus 1 species of the Alphacoronavirus genus belonging to the Coronaviridae family of viruses. (wikipedia.org)
  • SCARB2 is a receptor for two viruses that cause hand, foot, and mouth disease in children, Enterovirus 71 and Coxsackievirus A16. (wikipedia.org)
  • concentrations
  • ACTH receptors are also expressed in the skin, and in both white and brown adipoctyes, and is expressed in greater concentrations when adipose cells differentiate. (wikipedia.org)
  • treatment
  • Further analysis employing a LIMP-2 knockout mouse demonstrated that animals lacking LIMP-2 failed to flight a normal hypertrophic response following Angiotensin II treatment, however they developed interstitial fibrosis and dilated cardiomyopathy coordinate with disrupted intercalated disc structure. (wikipedia.org)
  • Mice
  • These mice synthesize a misfolded type of mutant PrP within their brains that presents a high propensity to aggregate but provides considerably much less protease level of resistance than typical PrPSc, and is not infectious C. (stopvivisection.info)
  • cell
  • These factors vary by cell type and gestational age and can be affected by changes to the in utero environment and maternal immunity. (jci.org)
  • C-jun has been shown to be essential for fibroblast proliferation, and levels of both AP-1 subunits have been shown to be expressed above basal levels during cell division. (wikipedia.org)
  • AP-1 has been shown to be involved in cell differentiation in several systems. (wikipedia.org)
  • activity
  • AP-1 activity is often regulated via post-translational modifications, DNA binding dimer composition, and interaction with various binding partners. (wikipedia.org)
  • cause
  • Fenoldopam mesylate contains sodium metabisulfite, a sulfite that may rarely cause allergic-type reactions including anaphylactic symptoms and asthma in susceptible people. (wikipedia.org)
  • common
  • The type II cultures are generally easier to perform, which has resulted in an imbalance of experiments performed with many studies about type II (even though it is a far less common form). (wikipedia.org)
  • presence
  • Several hereditary prion diseases, actually, develop in Crenolanib the lack of protease-resistant PrP or in the current presence of other abnormal types of the proteins, and are not really transmissible to lab pets C. (stopvivisection.info)
  • cancer
  • in other types, most notably lung cancers, neprilysin is downregulated, and thus unable to modulate the pro-growth autocrine signaling of cancer cells via secreted peptides such as mammalian homologs related to bombesin. (wikipedia.org)