EnzymeInhibitorsAntagonistsARBsBlockersCardiovascularMediatesInhibitBlockadePeptideAT1RAbstractAntibodiesSecretionAntagonistVasoconstrictionGenePhysiologicalACE2AldosteroneVitamin D ReceptInhibitsHypertensionReninGenesNonpeptideBlockerInternalizationHomeostasisMechanismCell proliferationPolymorphismsProteinPeptidesSynthesisAffinitiesModulatesVascularSelectivelyCellsResponsesBindingActivationEffectsBind
Enzyme9
- By constant-pH Monte Carlo simulations and the PROCEEDpKa method, we have mapped the electrostatic epitopes for four monoclonal antibodies and the angiotensin-converting enzyme 2 (ACE2) on both SARS-CoV-1 and the new SARS-CoV-2 S receptor binding domain (RBD) proteins. (nih.gov)
- Angiotensin-converting enzyme-related carboxypeptidase (ACE2) is a recently identified zinc metalloprotease with carboxypeptidase activity that was identified using our genomics platform. (acs.org)
- Structure-Guided Chemical Optimization of Bicyclic Peptide (Bicycle) Inhibitors of Angiotensin-Converting Enzyme 2. (acs.org)
- Angiotensin-Converting Enzyme 2 Ectodomain Shedding Cleavage-Site Identification: Determinants and Constraints. (acs.org)
- Development of Potent and Selective Phosphinic Peptide Inhibitors of Angiotensin-Converting Enzyme 2. (acs.org)
- Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). (nih.gov)
- All components of the RAS (angiotensinogen, angiotensin converting enzyme, angiotensin receptors) are expressed in many types of tumours, including endometrial cancer ( 2 , 4 ). (spandidos-publications.com)
- Both heart cells and lung cells are covered with surface proteins known as angiotensin-converting enzyme 2 (ACE2) - these molecules serve as "doorways" for the virus to enter cells. (sott.net)
- These agents are competitive inhibitors of angiotensin-converting enzyme (ACE). (medscape.com)
Inhibitors4
- Chae YK, Brown EN, Lei X, Melhem-Bertrandt A, Giordano SH, Litton JK, Hortobagyi GN, Gonzalez-Angulo AM, Chavez-MacGregor M. Use of ACE Inhibitors and Angiotensin Receptor Blockers and Primary Breast Cancer Outcomes. (jcancer.org)
- ACE inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) may have anti-tumor properties. (jcancer.org)
- ACE inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) are the two widely used RAS antagonists. (jcancer.org)
- Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin II from angiotensin I, is widely used in the treatment of hypertension. (nih.gov)
Antagonists3
- Due to the hemodynamic pressure and volume effects mediated by AT1 receptors, AT1 receptor antagonists are widely prescribed drugs in the management of hypertension and stable heart failure. (wikipedia.org)
- These results indicate that up-regulation of AT 1A , PDGF-Rβ, and ECM-related genes in the balloon-injured carotid artery is in part an AT 1 -mediated phenomenon and that prevention of receptor up-regulation may contribute to the attenuating effects of AT 1 antagonists on neointimal formation after injury. (aspetjournals.org)
- Functional analysis using the cell-based assay receptor selection and amplification technology (R-SAT) revealed that three variants (AT 1 -G45R, AT 1 -F204S, and AT 1 -C289W) displayed altered responses to Ang II and other AT 1 receptor agonists and antagonists. (aspetjournals.org)
ARBs2
- Two SNP mutated structures of AT1R i.e. rs780860717 (G288T), rs868647200 (A182C) shows considerably less binding affinities in case of all angiotensin receptor blockers (ARBs). (wikipedia.org)
- ARBs inhibit angiotensin II binding to type 1 angiotensin II receptors. (medscape.com)
Blockers4
- Angiotensin II receptor blockers are drugs indicated for hypertension, diabetic nephropathy and congestive heart failure. (wikipedia.org)
- AT1 receptor blockers have been shown to reduce fear memory recall in mice, but the reliability and relevance of this finding are to be determined. (wikipedia.org)
- Beta-blockers bind to beta-adrenoceptors, which inhibit normal sympathetic effects that act through the receptors norepinephrine and epinephrine. (uspharmacist.com)
- Nonselective beta-blockers block both beta receptors, whereas cardioselective beta-blockers bind to the beta-adrenoceptor and partially activate the receptor while preventing other receptor agonists from binding. (uspharmacist.com)
Cardiovascular9
- The AT1 receptor mediates the major cardiovascular effects of angiotensin II. (wikipedia.org)
- AT 1 receptors are involved in the pathogenesis of several cardiovascular diseases, including hypertension, cardiac hypertrophy, and congestive heart failure, which are characterized by significant interindividual variation in disease risk, progression, and response to pharmacotherapy. (aspetjournals.org)
- Intro Angiotensin II is definitely a pivotal physiological regulator of blood pressure salt and fluid homeostasis and cardiovascular structure (1). (opioid-receptors.com)
- Moreover numerous clinical tests have shown the beneficial effects of pharmacologic therapy that reduces BMS 433796 AT1R activity in a wide variety of cardiovascular disorders (1). (opioid-receptors.com)
- There is also an AT 2 receptor found in many tissues, but AT 2 is not known to be associated with cardiovascular homeostasis. (nih.gov)
- Candesartan does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation. (nih.gov)
- The A 1166 C polymorphism of the AT 1 receptor gene may be associated with cardiovascular phenotypes, such as high arterial blood pressure, aortic stiffness, and increased cardiovascular risk. (techscience.com)
- Subtipo de receptor de angiotensina que se expresa, en grandes cantidades, en diversos tejidos adultos, tales como el SISTEMA CARDIOVASCULAR, el RIÑÓN, el SISTEMA ENDOCRINO y el SISTEMA NERVIOSO. (bvsalud.org)
- An angiotensin receptor subtype that is expressed at high levels in a variety of adult tissues including the CARDIOVASCULAR SYSTEM, the KIDNEY, the ENDOCRINE SYSTEM and the NERVOUS SYSTEM. (bvsalud.org)
Mediates1
- The angiotensin II type 1 receptor mediates the vasoconstrictor and growthpromoting effects of Ang II. (techscience.com)
Inhibit2
- They inhibit the effect of angiotensin II, and they are used in the treatment of hypertension, congestive heart failure, and diabetic nephropathy. (jcancer.org)
- These results point out hCG and Ang-(1 - 7) as effective compounds to inhibit cell proliferation, since they decrease cell viability and increase apoptosis in both normal and in tumoral breast cells, being the effect more pronounced in the tumoral cell line. (scirp.org)
Blockade1
- Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and angiotensin II circulating levels do not overcome the effect of candesartan on blood pressure. (nih.gov)
Peptide3
- The angiotensin receptor is activated by the vasoconstricting peptide angiotensin II. (wikipedia.org)
- The angiotensin II type 1 (AT 1 ) receptor is the primary effector for angiotensin II (Ang II), a key peptide regulator of blood pressure and fluid homeostasis. (aspetjournals.org)
- The renin angiotensin system (RAS) is a peptide based homeostatic gatekeeper system known to play a role in blood pressure control and electrolyte balance[ 1 , 2 ]. (jcancer.org)
AT1R8
- The angiotensin II type 1 receptor (AT1R) is definitely a G-protein-coupled receptor that confers most of the deleterious effects of angiotensin II while the type 2 receptor confers its protecting effects (2 3 Angiotensin-II-mediated triggering of AT1R has an important part in the pathogenesis of chronic renal failure heart failure hypertension and atherosclerosis. (opioid-receptors.com)
- Rules of AT1R manifestation is a critical mechanism that modulates the activity of renin-angiotensin system. (opioid-receptors.com)
- Cell surface manifestation of AT1R is definitely regulated by receptor internalization and this is definitely modulated by multiple proteins including BMS 433796 arrestins and ATRAP (4). (opioid-receptors.com)
- Transcriptional regulators of AT1R gene include glucocorticoids and interleukin 1β (5). (opioid-receptors.com)
- Type I angiotensin II receptors (AT1R) are somewhat unique in that they are expressed at apical (AP) and basolateral (BL) membranes in proximal tubule cells and both receptor sites undergo endocytosis. (duke.edu)
- We analyzed AT1R cytoplasmic (-COOH) tail deletion mutants to determine whether classic AT1R endocytosis motifs functioned similarly in polarized cells and simultaneously altered receptor properties. (duke.edu)
- Serially truncating the AT1R tail had little effect on AP/BL AT1R distribution as determined by 125I-angiotensin II binding in LLCPK(Cl4) cells transfected with an AT1R transcript. (duke.edu)
- AT(1)R in polarized cells contain dominant endocytosis signals but these motifs do not correlate with AP or BL AT1R expression. (duke.edu)
Abstract1
- Abstract Caveolin-1, the first member of caveolin family reported, is recognized as the structural component of caveola, a plasma membrane invagination or vesicles that are a subcompartment distinct from clathrin-coated pits. (techscience.com)
Antibodies4
- People develop type 1 diabetes when their bodies make antibodies that destroy the body's own insulin-making beta cells. (diabetes.org)
- Autoantibodies (AAB) against nuclear and membrane structures as well as neurotransmitter receptors including muscarinic cholinergic receptor M3/M4-antibodies (M3-mAChR/M4-mAChR) and beta-1 and -2-adrenergic receptor (beta1-AR/beta2-AR) have been described in patients with ME/CFS ( 3 , 6 - 8 ). (frontiersin.org)
- These antibodies belong to a network of natural antibodies against adrenergic, cholinergic and other G-protein coupled receptors (GPCR) which were shown to be dysregulated and dysfunctional in various autoimmune diseases ( 9 ). (frontiersin.org)
- The condyles were analyzed histologically, histomorphometrically, and immunohistochemically using the antibodies for bone sialoprotein (BSP), osteocalcin (OCC) and receptor activator of nuclear factor kappa-B ligand (RANKL). (bvsalud.org)
Secretion5
- The principal regulators of aldosterone synthesis and secretion are the renin-angiotensin system and the potassium ion concentration. (medscape.com)
- They reduce angiotensin II levels, decreasing aldosterone secretion. (medscape.com)
- Captopril prevents the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, resulting in lower aldosterone secretion. (medscape.com)
- Enalapril prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, resulting in increased levels of plasma renin and a reduction in aldosterone secretion. (medscape.com)
- It reduces angiotensin II levels, decreasing aldosterone secretion. (medscape.com)
Antagonist2
- We investigated the effects of the angiotensin II (Ang II) type 1 receptor (AT 1 ) antagonist KRH-594 on levels of the mRNAs for AT 1A , AT 1B , platelet-derived growth factor-receptor β (PDGF-Rβ), and extracellular matrix (ECM)-related genes using the competitive reverse transcription-polymerase chain reaction (RT-PCR) method and on neointimal formation in the balloon-injured rat carotid artery. (aspetjournals.org)
- Candesartan Cilexetil and Hydrochlorothiazide Tablets USP combine an angiotensin II receptor (type AT 1 ) antagonist and a diuretic, hydrochlorothiazide. (nih.gov)
Vasoconstriction2
- Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. (nih.gov)
- Activation of the type 1 angiotensin receptor causes VASOCONSTRICTION and sodium retention. (bvsalud.org)
Gene7
- however, it is now believed that there is only one type 1 receptor gene in humans. (wikipedia.org)
- KRH-594 (10 mg/kg/day) also suppressed the injury-induced gene expressions for transforming growth factor-β 1 and fibronectin and reduced collagen α1(I) and α1(III) mRNA levels for the first 7 days after injury. (aspetjournals.org)
- The AGTR1 gene provides instructions for making a protein called the angiotensin II receptor type 1 (AT1 receptor). (medlineplus.gov)
- The AGTR1 gene mutations that cause this disorder likely change or block the AT1 receptor's ability to stimulate signaling, which results in a nonfunctional renin-angiotensin system. (medlineplus.gov)
- Angiotensin II type 1 receptor gene polymorphisms in humans: physiology and pathophysiology of the genotypes. (medlineplus.gov)
- AGTR1, a gene encoding angiotensin receptor type 1, was found to be markedly expressed in 10-20% of human breast cancer tissues, mutually exclusive with ERBB2 overexpression. (jcancer.org)
- P. M. Frossard, M. J. Malloy, G. G. Lestringant and J. P. Kane, "Haplotypes of the Human Renin Gene Associated with Essential Hypertension and Stroke," Journal of Human Hypertension, Vol. 15, No. 1, 2001, pp. 49-55. (scirp.org)
Physiological1
- These data demonstrate that polymorphic variation in the human AT 1 receptor induces loss of functional phenotypes, which may constitute the molecular basis of variability of AT 1 receptor-mediated physiological responses. (aspetjournals.org)
ACE23
- However, the affinity between the S RBD protein from the new SARS-CoV-2 and ACE2 is higher than for any studied antibody previously found complexed with SARS-CoV-1. (nih.gov)
- Effect of an Inhibitor on the ACE2-Receptor-Binding Domain of SARS-CoV-2. (acs.org)
- Mechanism of Ligand Recognition by Human ACE2 Receptor. (acs.org)
Aldosterone5
- Binding of angiotensin II to the AT1 receptor also stimulates production of the hormone aldosterone, which triggers the absorption of water and salt by the kidneys. (medlineplus.gov)
- Ding W, Wang F, Fang Q, Zhang M, Chen J, Gu Y. Association between two genetic polymorphisms of the renin-angiotensin-aldosterone system and diabetic nephropathy: a meta-analysis. (medlineplus.gov)
- [ 1 , 2 ] Hyperaldosteronism represents part of a larger entity of hypermineralocorticoidism that may be caused by aldosterone, its mineralocorticoid precursors, or defects that modulate aldosterone effects on its target tissues. (medscape.com)
- Candesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT 1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. (nih.gov)
- Losartan inhibits the vasoconstrictor and aldosterone-secreting effects of angiotensin II by blocking the binding of angiotensin II to receptors. (medscape.com)
Vitamin D Recept1
- Structure-activity relationships of FXR-active compounds revealed by this screening were then compared against the androgen receptor, estrogen receptor α, peroxisome proliferator-activated receptors δ and γ and the vitamin D receptor. (nature.com)
Inhibits3
- 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 in hepatocytes and activates various tyrosine kinases. (wikipedia.org)
- Ramipril partially inhibits both tissue and circulating ACE activity, thereby reducing the formation of angiotensin II in the tissue and plasma. (medscape.com)
- Estrogen is a steroid hormone that is important for the growth and maintenance of the female skeleton and inhibits bone resorption 1 . (bvsalud.org)
Hypertension4
- Legislation of angiotensin II type 1 receptor (In1R) includes a pathophysiological function in hypertension atherosclerosis and center failing. (opioid-receptors.com)
- 1 It is estimated that the number of persons aged 65 years and older will increase to 72 million by the year 2030, which will in turn result in an increased rate of hypertension among the elderly. (uspharmacist.com)
- According to the Seventh Report of the Joint National Committee on the Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC 7), the SBP should be the primary target for diagnosis and treatment of hypertension in the elderly ( TABLE 1 ). (uspharmacist.com)
- I. F. Benter, D. I. Diz and C. M. Ferrari, "Pressor and Reflex Sensitivity Is Altered in Spontaneously Hypertensive Rats Treated with Angiotensin-(1 -7)," Hypertension, Vol. 26, No. 6, 1995, pp. 1138-1144. (scirp.org)
Renin8
- Elements of the renin-angiotensin system have been widely studied in a large variety of vertebrate animals including amphibians, reptiles, birds, and mammals. (wikipedia.org)
- This protein is part of the renin-angiotensin system, which regulates blood pressure and the balance of fluids and salts in the body. (medlineplus.gov)
- Through a series of steps, the renin-angiotensin system produces a molecule called angiotensin II, which attaches (binds) to the AT1 receptor, stimulating chemical signaling. (medlineplus.gov)
- Renal tubular dysgenesis can be caused by mutations in both copies of any of the genes involved in the renin-angiotensin system. (medlineplus.gov)
- Mutations in genes in the renin-angiotensin system are associated with autosomal recessive renal tubular dysgenesis. (medlineplus.gov)
- Angiotensin-(1 - 7) [Ang-(1 - 7)] is an endogenous heptapeptide hormone of the renin-angiotensin system that has anti proliferative properties. (scirp.org)
- Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. (nih.gov)
- Angiotensin II (Ang II) is the major octapeptide of the renin-angiotensin system (RAS). (spandidos-publications.com)
Genes1
- A subtype of angiotensin receptor found primarily in rodent species that have two type 1 angiotensin receptor genes. (bvsalud.org)
Nonpeptide1
- Candesartan cilexetil, a nonpeptide, is chemically described as (±)-1-Hydroxyethyl 2-ethoxy-1-[ p -( o -1 H -tetrazol-5-ylphenyl)benzyl]-7-benzimidazolecarboxylate, cyclohexyl carbonate (ester). (nih.gov)
Blocker2
- Angiotensin II receptor blocker", Wikipedia, 2022-07-26, retrieved 2022-08-10 Wilson JX (1984). (wikipedia.org)
- ARB stands for angiotensin (an-gee-oh-TEN-sin) receptor blocker. (diabetes.org)
Internalization1
- Scholars@Duke publication: The type 1 angiotensin II receptor tail affects receptor targeting, internalization, and membrane fusion properties. (duke.edu)
Homeostasis1
- The farnesoid X receptor (FXR) regulates the homeostasis of bile acids, lipids and glucose. (nature.com)
Mechanism1
- 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)
Cell proliferation1
- Therefore, various biologically active peptides such as angiotensin, affecting cell proliferation, have become a new area of study in endometrial cancer research. (spandidos-publications.com)
Polymorphisms1
- Such variation could arise from genomic polymorphisms in the AT 1 receptor. (aspetjournals.org)
Protein2
- Angiotensin II receptor type 1 has been shown to interact with Zinc finger and BTB domain-containing protein 16. (wikipedia.org)
- Angiotensin II Activates Extracellular Signal Regulated Kinases via Protein Kinase C and Epidermal Growth Factor Receptor in Breast Cancer Cells," Journal of Cellular Physiology, Vol. 196, No. 2, 2003, pp. 370-377. (scirp.org)
Peptides2
- Both cell lines received an hCG and angiotensin peptides 24-hour treatment, in combina tion or alone followed by cell viability, apoptosis and cell cycle assays performed by flow cytometer (GUAVA). (scirp.org)
- In summary, cell viability was decreased and apoptosis (initial, mid and late) was in creased after hCG and/or Ang-(1 - 7) peptides treatments. (scirp.org)
Synthesis1
- Its action is, therefore, independent of the pathways for angiotensin II synthesis. (nih.gov)
Affinities1
- AT 1 -C289W and AT 1 -F204S displayed reduced binding affinities of 3- and 5-fold and reduced cell surface expression of 43 and 60% of that observed for the WT receptor, respectively. (aspetjournals.org)
Modulates1
- Endocytosis modulates cell responses by removing and recycling receptors from the cell surface. (duke.edu)
Vascular1
- In patients with infection-triggered onset, the associations of low sCD26 with elevated autoantibodies (AAB) against alpha1 adrenergic (AR) and M3 muscarinic acetylcholine receptors (mAChR) point to a pathomechanism of infection-triggered autoimmune-mediated vascular and immunological dysregulation. (frontiersin.org)
Selectively1
- INT-747, so called obeticholic acid (OCA) or 6-alpha-ethyl chenodeoxycholic acid (6-ECDCA), is a 6-alpha-alkyl-substituted analog of CDCA selectively inducing FXR transactivation at 1 μM 15 . (nature.com)
Cells6
- Angiotensin II acts as a growth factor both in normal and cancer breast epithelial cells and promotes adhesion and invasion[ 15 , 16 ]. (jcancer.org)
- These cells had an increase in late apoptosis and necrosis after AngII Toac, hCG + Ang-(1 - 7) and hCG + Ang-(1 - 7)-Fmoc treatments. (scirp.org)
- sCD26 concentrations in infection-triggered ME/CFS were found to be associated with activated T cells, liver enzymes, creatin kinase (CK) and lactate dehydrogenase (LDH) and inversely with Interleukin-1 beta (IL-1b). (frontiersin.org)
- The aim of the present study was to evaluate the influence of angiotensin II (Ang II) on human EC cells. (spandidos-publications.com)
- The aim of this study was to determine the expression of caveolin-1 in adult rat Leydig cells. (techscience.com)
- Testis sections incubated with an antibody to caveolin-1 showed, by immunohistochemistry, a moderate number of Leydig cells with different degrees of immunoreaction and a strong reaction in endothelial cells and in the lamina propia of seminiferous tubules. (techscience.com)
Responses1
- Agonist responses to Ang II were absent for AT 1 -G45R and significantly reduced in potency for AT 1 -C289W (11-fold) and AT 1 -F204S (57-fold) compared with the wild-type (WT) receptor. (aspetjournals.org)
Binding2
- Radioligand binding studies revealed that AT 1 -G45R failed to bind Ang II, whereas cell surface staining clearly showed that it trafficked to the cell surface. (aspetjournals.org)
- GAPDH-binding site was mapped to 1-100 of 3′-UTR. (opioid-receptors.com)
Activation1
- Angiotensin II is now regarded as a tumor growth promoter via angiogenesis from activation of the VEGF pathway[ 4 - 6 ]. (jcancer.org)
Effects2
- 1 and 3 mg/kg/day p.o.), had similar effects on the morphological change and AT 1A mRNA level, whereas a smooth muscle relaxant, hydralazine (10 mg/kg/day p.o.), did not. (aspetjournals.org)
- Angiotensin II offers two receptors that mediate its effects. (opioid-receptors.com)
Bind1
- Because endogenous chemicals bind and activate FXR, it is important to examine which xenobiotic compounds would disrupt normal receptor function. (nature.com)