Search results for "Endothelin receptor"

showing 10 items of 43 documents

Large Between-Patient Variability in eGFR Decline before Clinical Trial Enrollment and Impact on Atrasentan’s Efficacy:

2021

n/a.

Oncologymedicine.medical_specialtyMEDLINEeGFR declineType 2 diabetesEgfr declineendothelin receptor antagonistlaw.inventionRandomized controlled triallawInternal medicinePost-hoc analysismedicinebusiness.industryEndothelin receptor antagonistAtrasentan22/2 OA procedureGeneral Medicinemedicine.diseaseClinical trialNephrologyrandomized controlled trialtype 2 diabetesbusinesschronic kidney diseasemedicine.drugJournal of the American Society of Nephrology
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Isolation of endothelin A receptor from bovine lungs.

1995

We isolated endothelin receptor A (ET A ) from bovine lungs in a single-step purification procedure using antibodies raised against synthetic peptides that correspond to extra- and intracellular domains of the rat bradykinin receptor. Two receptor species of 55 and 35 kDa were isolated and subjected to N-terminal microsequencing. The difference between the observed and expected molecular weight species suggests that bovine ET A receptor is glycosylated.

PharmacologyGlycosylationReceptors EndothelinBiologyIn vitroRatsMolecular Weightchemistry.chemical_compoundBiochemistryAffinity chromatographychemistrybiology.proteinAnimalsCattleRabbitsAntibodyBradykinin receptorCardiology and Cardiovascular MedicineEndothelin receptorReceptorLungIntracellularJournal of cardiovascular pharmacology
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Cigarette smoke exposure up-regulates endothelin receptor B in human pulmonary artery endothelial cells: molecular and functional consequences

2010

BACKGROUND AND PURPOSE Pulmonary arteries from smokers and chronic obstructive pulmonary disease patients show abnormal endothelium-dependent vascular reactivity. We studied the effect of cigarette smoke extract (CSE) on endothelin receptor B (ETB) expression in human pulmonary artery endothelial cells (HPAECs) and its role in endothelial dysfunction. EXPERIMENTAL APPROACH ETB receptor expression was measured by real time RT-PCR, Western blot and immunofluorescence. Cell contraction, intracellular Ca2+, F/G-actin, RhoA activity, myosin light chain phosphorylation, ET, NO, thromboxane (Tx)A2 and reactive oxygen species (ROS) were measured by traction microscopy, fluorescence microscopy, phal…

Pharmacologymedicine.medical_specialtyMyosin light-chain kinaseRHOAEndotheliumbiologyChemistryPharmacologyEndothelin 1Bosentanmedicine.anatomical_structureEndocrinologyInternal medicinemedicinebiology.proteinReceptorEndothelin receptorRho-associated protein kinasemedicine.drugBritish Journal of Pharmacology
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Endothelin receptor expression in idiopathic pulmonary arterial hypertension: effect of bosentan and epoprostenol treatment.

2011

Endothelin receptor antagonists are used to treat idiopathic pulmonary arterial hypertension (IPAH), but human pulmonary arterial endothelin receptor expression is not well defined. We hypothesised that disease and treatment would modify normal receptor distribution in pulmonary resistance arteries of children. Using immunohistochemistry and semiquantitative analysis, we investigated endothelin receptor subtypes A and B (ET(A) and ET(B), respectively), and endothelial nitric oxide synthase (eNOS) expression in peripheral pulmonary arteries of tissue from untreated children with IPAH (n=7), following extended combined bosentan and epoprostenol therapy (n=5) and from normal subjects (n=5). Cl…

Pulmonary and Respiratory MedicineMalePathologymedicine.medical_specialtyEndotheliumAdolescentNifedipineNitric Oxide Synthase Type IIIEndothelin A Receptor AntagonistsEndothelin B Receptor AntagonistsHypertension PulmonaryVasodilator AgentsPulmonary ArteryMuscle Smooth VascularPiperazinesSildenafil CitrateNitric oxidechemistry.chemical_compoundEnosInternal medicinemedicineHumansFamilial Primary Pulmonary HypertensionSulfonesReceptorChildAntihypertensive AgentsSulfonamidesbiologybusiness.industryBosentanbiology.organism_classificationReceptor Endothelin AEpoprostenolReceptor Endothelin BEndothelin A Receptor AntagonistsBosentanEndothelin B Receptor Antagonistsmedicine.anatomical_structureEndocrinologychemistryPurinesChild PreschoolDrug Therapy CombinationFemaleEndothelium VascularEndothelin receptorbusinessmedicine.drugThe European respiratory journal
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Chronic Therapy with Isosorbide-5-Mononitrate Causes Endothelial Dysfunction and Oxidative Stress – Improvement by Endothelin-Receptor Blocker (Bosen…

2012

business.industryPharmacologymedicine.diseasemedicine.disease_causeBiochemistryBosentanPhysiology (medical)Isosorbide-5-mononitratemedicineEndothelial dysfunctionEndothelin receptorbusinessOxidative stressmedicine.drugFree Radical Biology and Medicine
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Anti-endothelin drugs in solid tumors

2010

Importance of the field: The endothelin (ET) axis, which includes the biological functions of ETs and their receptors, has played a physiological role in normal tissue, acting as a modulator of vasomotor tone, tissue differentiation and development, cell proliferation and hormone production. Interestingly, it also functions in the growth and progression of various tumors. Several researchers have identified the blockade of the ET-1 receptor as a promising therapeutic approach. Areas covered in this review: The clinical investigation of an orally bioavailable ET antagonist, atrasentan, in prostate cancer, is encouraging. In this neoplasia, it has shown antitumor activity, bone metastasis con…

medicine.hormoneEndothelin Receptor AntagonistsMalemedicine.medical_specialtyPyrrolidinesSettore MED/06 - Oncologia Medicaatrasentan endothelins prostate cancer zibotentanModels BiologicalEndothelinsProstate cancerchemistry.chemical_compoundDrug Delivery SystemsInternal medicineNeoplasmsAntineoplastic Combined Chemotherapy ProtocolsmedicineHumansPharmacology (medical)ReceptorPharmacologyZibotentanbusiness.industryReceptors EndothelinEndothelinsAtrasentanBone metastasisProstatic NeoplasmsDrugs Investigationalmedicine.diseaseBlockadeEndocrinologychemistryAtrasentanCancer researchEndothelin receptorbusinessmedicine.drugSignal Transduction
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EndothelinA receptor antagonist BSF-208075 causes immune modulation and neuroprotection after stroke in gerbils.

2005

Leukocytes contribute to the ischemia-reperfusion injury. Recent studies suggested endothelins could be important mediators for leukocyte activation in stroke. We tested if the endothelinA receptor antagonist BSF-208075 (ambrisentan) could reduce an ischemic lesion by modulation of leukocyte-endothelium interactions. Twenty-four gerbils underwent either a sham operation (n=6) or 15 min of bilateral carotid artery occlusion resulting in global cerebral ischemia. Ischemic animals received normal saline (n=6), 5 mg/kg BSF-208075 (n=6) or 30 mg/kg (n=6) administered intravenously at 10 min of reperfusion. Leukocytes rolling or adhering to endothelium were counted by intravital microscopy in par…

medicine.hormoneMaleAmbrisentanmedicine.drug_classEndothelin A Receptor AntagonistsIschemiaPharmacologyBrain IschemiaEndothelinsLeukocytesMedicineAnimalsImmunologic FactorsMolecular BiologyStrokeDose-Response Relationship DrugPhenylpropionatesbusiness.industryGeneral NeuroscienceEndothelinsAntagonistBrainmedicine.diseaseReceptor antagonistReceptor Endothelin APyridazinesStrokeChemotaxis LeukocyteNeuroprotective AgentsTreatment OutcomeAnesthesiaCerebrovascular CirculationReperfusion InjuryNerve DegenerationEncephalitisNeurology (clinical)businessEndothelin receptorGerbillinaeIntravital microscopyDevelopmental Biologymedicine.drugBrain research
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COX-2, Another Important Player in the Nitric Oxide–Endothelin Cross-Talk

2006

See related article, pages 1439–1445 Traditionally, the role of the endothelium was thought to be primarily that of a selective barrier to the diffusion of macromolecules from the vessel lumen to the interstitial space. During the past 20 years, numerous additional roles for the endothelium have been defined such as regulation of vascular tone, modulation of inflammation, promotion as well as inhibition of vascular growth, and modulation of platelet aggregation and coagulation. Endothelial dysfunction is a characteristic feature of patients with cardiovascular risk factors such as hypercholesterolemia, hypertension, diabetes mellitus, and chronic smoking. More recent studies indicate that i…

medicine.hormonemedicine.medical_specialtyEndotheliumPhysiologyChemistryProstacyclinInflammationmedicine.diseaseEndothelin 1EndothelinsEndocrinologymedicine.anatomical_structureInternal medicinecardiovascular systemmedicineEndothelial dysfunctionmedicine.symptomCardiology and Cardiovascular MedicineReceptorEndothelin receptormedicine.drugCirculation Research
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Relationship between endothelin and insulin-like growth factor-1 in essential hypertension.

1999

medicine.hormonemedicine.medical_specialtybusiness.industrymedicine.medical_treatmentEssential hypertensionmedicine.diseaseEndothelinsInsulin-like growth factorEndocrinologyInternal medicinePathophysiology of hypertensionInternal MedicinemedicineEndothelin receptorbusinessAmerican Journal of Hypertension
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Sinusoidal endothelial liver cells in vitro release endothelin — Augmentation by transforming growth factorβ and Kupffer cell-conditioned media

1991

Endothelin is the most potent vasoconstrictor peptide known today. Using a radioimmunoassay for endothelin, we measured immunoreactive endothelin in culture media of guinea pig sinusoidal endothelial liver cells and human umbilical vein endothelial cells. A time-dependent release of immunoreactive endothelin by confluent sinusoidal endothelial liver cells in culture was found. Sinusoidal endothelial liver cells produced similar amounts of immunoreactive endothelin as umbilical vein endothelial cells, about 900 pg/microgram DNA per 24 h. In the presence of transforming growth factor beta a dose-dependent increase of immunoreactive endothelin release was measured. The maximal increase of 50% …

medicine.medical_specialtyKupffer CellsGuinea PigsRadioimmunoassayUmbilical veinTransforming Growth Factor betaInternal medicineDrug DiscoverymedicineAnimalsCells CulturedGenetics (clinical)Dose-Response Relationship DrugbiologyChemistryEndothelinsKupffer cellRadioimmunoassayGeneral MedicineTransforming growth factor betaEndothelin 1In vitroEndocrinologymedicine.anatomical_structureLivercardiovascular systembiology.proteinMolecular MedicineFemaleEndothelium VascularEndothelin receptorTransforming growth factorKlinische Wochenschrift
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