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Endothelin inhibitor

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https://www.readbyqxmd.com/read/28425346/ambrisentan-a-review-of-its-use-in-pulmonary-arterial-hypertension
#1
Belinda N Rivera-Lebron, Michael G Risbano
Pulmonary arterial hypertension (PAH) is a progressive disease defined by an elevation in pulmonary arterial pressure that can lead to right heart failure and death. Ambrisentan is a selective endothelin receptor antagonist approved for the treatment of idiopathic, heritable PAH and connective tissue disease-associated PAH. Ambrisentan has been shown to improve exercise capacity and hemodynamics with an acceptable side-effect profile. It has also proven to be safely used in combination with other PAH-specific medications, especially with phosphodiesterase-5 inhibitors...
April 1, 2017: Therapeutic Advances in Respiratory Disease
https://www.readbyqxmd.com/read/28420826/efficacy-and-safety-of-an-orally-administered-selective-prostacyclin-receptor-agonist-selexipag-in-japanese-patients-with-pulmonary-arterial-hypertension
#2
Nobuhiro Tanabe, Satoshi Ikeda, Nobuhiro Tahara, Keiichi Fukuda, Masaru Hatano, Hiroshi Ito, Tomotaka Nakayama, Toshihisa Anzai, Akiyoshi Hashimoto, Teruo Inoue, Kouji Kajinami, Yasuki Kihara, Hideyuki Kinoshita, Koichiro Kuwahara, Toyoaki Murohara, Osamu Okazaki, Satoshi Sakai, Toru Satoh, Yutaka Takeda, Yasuchika Takeishi, Mitsugu Taniguchi, Hiroshi Watanabe, Takeshi Yamamoto, Keiko Yamauchi-Takihara, Koichiro Yoshioka, Shigetake Sasayama
BACKGROUND: Selexipag is an orally available prostacyclin receptor (IP receptor) agonist with a non-prostanoid structure. In this open-label Phase II trial, the efficacy and safety of selexipag in Japanese patients with pulmonary arterial hypertension (PAH) is examined.Methods and Results:Selexipag was administered at 200 μg twice daily and titrated up to 1,600 μg by increments of 200 μg in 37 subjects to reach the individual maximum tolerated dose. At 16 weeks, in 33 patients comprising the per-protocol set, the pulmonary vascular resistance (PVR; primary endpoint) decreased from 683...
April 18, 2017: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/28416805/a-new-inhibitor-of-the-%C3%AE-arrestin-ap2-endocytic-complex-reveals-interplay-between-gpcr-internalization-and-signalling
#3
Alexandre Beautrait, Justine S Paradis, Brandon Zimmerman, Jenna Giubilaro, Ljiljana Nikolajev, Sylvain Armando, Hiroyuki Kobayashi, Lama Yamani, Yoon Namkung, Franziska M Heydenreich, Etienne Khoury, Martin Audet, Philippe P Roux, Dmitry B Veprintsev, Stéphane A Laporte, Michel Bouvier
In addition to G protein-coupled receptor (GPCR) desensitization and endocytosis, β-arrestin recruitment to ligand-stimulated GPCRs promotes non-canonical signalling cascades. Distinguishing the respective contributions of β-arrestin recruitment to the receptor and β-arrestin-promoted endocytosis in propagating receptor signalling has been limited by the lack of selective analytical tools. Here, using a combination of virtual screening and cell-based assays, we have identified a small molecule that selectively inhibits the interaction between β-arrestin and the β2-adaptin subunit of the clathrin adaptor protein AP2 without interfering with the formation of receptor/β-arrestin complexes...
April 18, 2017: Nature Communications
https://www.readbyqxmd.com/read/28412414/endothelin-1-promotes-hypertrophic-remodelling-of-cardiac-myocytes-by-activating-sustained-signalling-and-transcription-downstream-of-endothelin-type-a-receptors
#4
Caroline R Archer, Emma L Robinson, Faye M Drawnel, H Llewelyn Roderick
G-protein coupled receptor (GPCR) mediated activation of the MAPK signalling cascade is a key pathway in the induction of hypertrophic remodelling of the heart - a response to pathological cues including hypertension and myocardial infarction. While levels of pro-hypertrophic hormone agonists of GPCRs increase during periods of greater workload to enhance cardiac output, hypertrophy does not necessarily result. Here we investigated the relationship between the duration of exposure to the pro-hypertrophic GPCR agonist endothelin-1 (ET-1) and the induction of hypertrophic remodelling in neonatal rat ventricular myocytes (NRVM) and in the adult rat heart in vivo...
April 13, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28398455/systematic-evaluation-of-endothelin-1-measurement-relative-to-traditional-and-modern-biomarkers-for-clinical-assessment-and-prognosis-in-patients-with-chronic-systolic-heart-failure-serial-measurement-and-multimarker-testing
#5
Hanna K Gaggin, Quynh A Truong, Parul U Gandhi, Shweta R Motiwala, Arianna M Belcher, Rory B Weiner, Aaron L Baggish, James L Januzzi
Objectives: To define the role of single or serial measurement of endothelin 1 (ET-1) for prognostication beyond traditional and modern markers of risk in heart failure (HF). Methods: In total, 115 patients with chronic systolic HF were followed for 10 months. Clinical assessment and ET-1, N-terminal pro-B-type natriuretic peptide (NT-proBNP), highly sensitive troponin I (hsTnI), soluble ST2 (sST2), and galectin 3 were measured at each visit. Results: Elevated ET-1 was associated with worse HF, lower right ventricular function, higher pulmonary pressure, and higher left atrial volume index despite similar left ventricular function...
April 7, 2017: American Journal of Clinical Pathology
https://www.readbyqxmd.com/read/28393188/a-heptameric-peptide-purified-from-spirulina%C3%A2-sp-gastrointestinal-hydrolysate-inhibits-angiotensin-i-converting-enzyme-and-angiotensin%C3%A2-ii-induced-vascular-dysfunction-in-human-endothelial-cells
#6
Seong-Yeong Heo, Seok-Chun Ko, Chang Su Kim, Gun-Woo Oh, Bomi Ryu, Zhong-Ji Qian, Geunhyung Kim, Won Sun Park, Il-Whan Choi, Thi Tuong Vy Phan, Soo-Jin Heo, Do-Hyung Kang, Myunggi Yi, Won-Kyo Jung
In this study, a marine microalga Spirulina sp.-derived protein was hydrolyzed using gastrointestinal enzymes to produce an angiotensin I (Ang I)-converting enzyme (ACE) inhibitory peptide. Following consecutive purification, the potent ACE inhibitory peptide was composed of 7 amino acids, Thr-Met‑Glu‑Pro‑Gly‑Lys-Pro (molecular weight, 759 Da). Analysis using the Lineweaver-Burk plot and molecular modeling suggested that the purified peptide acted as a mixed non-competitive inhibitor of ACE...
April 4, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28388547/involvement-of-heparanase-in-the-pathogenesis-of-acute-kidney-injury-nephroprotective-effect-of-pg545
#7
Zaid Abassi, Shadi Hamoud, Ahmad Hassan, Iyad Khamaysi, Omri Nativ, Samuel N Heyman, Rabia Shekh Muhammad, Neta Ilan, Preeti Singh, Edward Hammond, Gianluigi Zaza, Antonio Lupo, Maurizio Onisto, Gloria Bellin, Valentina Masola, Israel Vlodavsky, Giovani Gambaro
Despite the high prevalence of acute kidney injury (AKI) and its association with increased morbidity and mortality, therapeutic approaches for AKI are disappointing. This is largely attributed to poor understanding of the pathogenesis of AKI. Heparanase, an endoglycosidase that cleaves heparan sulfate, is involved in extracellular matrix turnover, inflammation, kidney dysfunction, diabetes, fibrosis, angiogenesis and cancer progression. The current study examined the involvement of heparanase in the pathogenesis of ischemic reperfusion (I/R) AKI in a mouse model and the protective effect of PG545, a potent heparanase inhibitor...
March 25, 2017: Oncotarget
https://www.readbyqxmd.com/read/28361339/use-of-antihypertensive-drugs-in-neoplastic-patients
#8
Damiano Rizzoni, Carolina De Ciuceis, Enzo Porteri, Claudia Agabiti-Rosei, Enrico Agabiti-Rosei
The introduction of Vascular Endothelial Growth Factor (VEGF) signaling pathway inhibitor treatment has highlighted the role of the baseline activity of the VEFG system for blood pressure regulation. VEGF signaling pathway is associated with hypertension and proteinuria. Activation of the endothelin system, endothelial dysfunction and capillary rarefaction are among the underlying mechanisms possibly explaining the rise in blood pressure and, to some extent, also the renal injury. The hypertension induced by VEGF signaling pathway inhibition is, usually, responsive to treatment...
March 30, 2017: High Blood Pressure & Cardiovascular Prevention: the Official Journal of the Italian Society of Hypertension
https://www.readbyqxmd.com/read/28356404/medical-management-of-chronic-thromboembolic-pulmonary-hypertension
#9
REVIEW
Joanna Pepke-Zaba, Hossein-Ardeschir Ghofrani, Marius M Hoeper
Chronic thromboembolic pulmonary hypertension (CTEPH) results from incomplete resolution of acute pulmonary emboli, organised into fibrotic material that obstructs large pulmonary arteries, and distal small-vessel arteriopathy. Pulmonary endarterectomy (PEA) is the treatment of choice for eligible patients with CTEPH; in expert centres, PEA has low in-hospital mortality rates and excellent long-term survival. Supportive medical therapy consists of lifelong anticoagulation plus diuretics and oxygen, as needed...
March 31, 2017: European Respiratory Review: An Official Journal of the European Respiratory Society
https://www.readbyqxmd.com/read/28348727/steps-forward-in-the-treatment-of-pulmonary-arterial-hypertension-latest-developments-and-clinical-opportunities
#10
REVIEW
Jessica B Badlam, Todd M Bull
Pulmonary arterial hypertension (PAH) is a chronic disease that results in narrowing of the small pre-capillary pulmonary arteries leading to elevation of pulmonary artery pressure and pulmonary vascular resistance, subsequent right ventricular failure, and if unchecked, death. Advances in the treatment of PAH over the last two decades have markedly improved survival. These improvements reflect a combination of changes in treatments, improved patient care strategies, and varying disease phenotypes in the PAH population...
February 2017: Therapeutic Advances in Chronic Disease
https://www.readbyqxmd.com/read/28344594/articular-inflammation-induced-by-an-enzymatically-inactive-lys49-phospholipase-a2-activation-of-endogenous-phospholipases-contributes-to-the-pronociceptive-effect
#11
Renata Gonçalves Dias, Sandra Coccuzzo Sampaio, Morena Brazil Sant'Anna, Fernando Queiroz Cunha, José María Gutiérrez, Bruno Lomonte, Yara Cury, Gisele Picolo
BACKGROUND: Arthritis is a set of inflammatory conditions that induce aching, stiffness, swelling, pain and may cause functional disability with severe consequences to the patient's lives. These are multi-mediated pathologies that cannot be effectively protected and/or treated. Therefore, the aim of this study was to establish a new model of acute arthritis, using a Lys49-PLA2 (Bothrops asper myotoxin II; MT-II) to induce articular inflammation. METHODS: The articular inflammation was induced by MT-II (10 μg/joint) injection into the left tibio-tarsal or femoral-tibial-patellar joints...
2017: Journal of Venomous Animals and Toxins Including Tropical Diseases
https://www.readbyqxmd.com/read/28344559/cyclooxygenase-2-inhibition-limits-angiotensin-ii-induced-dna-oxidation-and-protein-nitration-in-humans
#12
Vincent Pialoux, Marc J Poulin, Brenda R Hemmelgarn, Daniel A Muruve, Erica N Chirico, Camille Faes, Darlene Y Sola, Sofia B Ahmed
Compared to other cyclooxygenase-2 inhibitors, celecoxib is associated with a lower cardiovascular risk, though the mechanism remains unclear. Angiotensin II is an important mediator of oxidative stress in the pathophysiology of vascular disease. Cyclooxygenase-2 may modify the effects of angiotensin II though this has never been studied in humans. The purpose of the study was to test the effects of selective cyclooxygenase-2 inhibition on plasma measures of oxidative stress, the vasoconstrictor endothelin-1, and nitric oxide metabolites, both at baseline and in respose to Angiotensin II challenge in healthy humans...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28326642/neprilysin-inhibition-in-heart-failure-mechanisms-and-substrates-beyond-modulating-natriuretic-peptides
#13
REVIEW
Emilia D'Elia, Attilio Iacovoni, Muthiah Vaduganathan, Ferdinando L Lorini, Stefano Perlini, Michele Senni
The autonomic nervous system, the renin-angiotensin-aldosterone system, and the natriuretic peptide system represent critical regulatory pathways in heart failure and as such have been the major targets of pharmacological development. The introduction and approval of angiotensin receptor neprilysin inhibitors (ARNi) have broadened the available drug treatments of patients with chronic heart failure with reduced ejection fraction. Neprilysin catalyses the degradation of a number of vasodilator peptides, including the natriuretic peptides, bradykinin, substance P, and adrenomedullin, as well as vasoconstrictor peptides, including endothelin-1 and angiotensin I and II...
March 21, 2017: European Journal of Heart Failure
https://www.readbyqxmd.com/read/28323857/myocardial-ischemia-reperfusion-enhances-transcriptional-expression-of-endothelin-1-and-vasoconstrictor-etb-receptors-via-the-protein-kinase-mek-erk1-2-signaling-pathway-in-rat
#14
Gry Freja Skovsted, Lars Schack Kruse, Lukas Adrian Berchtold, Anne-Sofie Grell, Karin Warfvinge, Lars Edvinsson
BACKGROUND: Coronary artery remodelling and vasospasm is a complication of acute myocardial ischemia and reperfusion. The underlying mechanisms are complex, but the vasoconstrictor peptide endothelin-1 is suggested to have an important role. This study aimed to determine whether the expression of endothelin-1 and its receptors are regulated in the myocardium and in coronary arteries after experimental ischemia-reperfusion. Furthermore, we evaluated whether treatment with a specific MEK1/2 inhibitor, U0126, modified the expression and function of these proteins...
2017: PloS One
https://www.readbyqxmd.com/read/28303689/non-healing-ischaemic-digital-ulcer-in-a-systemic-sclerosis-patient-a-challenging-clinical-case
#15
Sophie Blaise, Matthieu Roustit, Alexandra Forli, Bernard Imbert, Jean-Luc Cracowski
Ischaemic digital ulcers (DUs) are an indicator of the severity of the microangiopathy in patients with systemic sclerosis (SSc). DUs are a frequent complication, affecting about 50% of patients with SSc, and are often recurrent. In cross-sectional studies involving patients with SSc, the frequency of ischaemic DUs was 12-16% with a major impact on hand function and quality of life. Effective therapy for DUs remains elusive. Intravenous iloprost has been demonstrated to have a positive effect on healing of active DUs...
March 16, 2017: International Wound Journal
https://www.readbyqxmd.com/read/28298655/dual-nep-ece-inhibition-improves-endothelial-function-in-mesenteric-resistance-arteries-of-32-week-old-shr
#16
Pieter Lemkens, Leon Ja Spijkers, Merlijn J Meens, Jelly Nelissen, Ben Janssen, Stephan Lm Peters, Paul Mh Schiffers, Jo Gr De Mey
Endothelin 1 (ET-1), a potent vasoconstrictor, pro-mitogenic and pro-inflammatory peptide, may promote development of endothelial dysfunction and arterial remodeling. ET-1 can be formed through cleavage of big-ET-1 by endothelin-converting enzyme (ECE) or neutral endopeptidase (NEP). We investigated whether chronic treatment with the novel dual NEP/ECE inhibitor SOL1 improves functional and structural properties of resistance-sized arteries of 32-week-old male spontaneously hypertensive rats (SHR). SHR received a chronic 4-week treatment with SOL1, losartan or hydralazine...
March 16, 2017: Hypertension Research: Official Journal of the Japanese Society of Hypertension
https://www.readbyqxmd.com/read/28287881/renin-angiotensin-system-blockade-alone-or-combined-with-eta-receptor-blockade-effects-on-the-course-of-chronic-kidney-disease-in-5-6-nephrectomized-ren-2-transgenic-hypertensive-rats
#17
Lenka Sedláková, Věra Čertíková Chábová, Šárka Doleželová, Petra Škaroupková, Libor Kopkan, Zuzana Husková, Lenka Červenková, Soňa Kikerlová, Ivana Vaněčková, Janusz Sadowski, Elzbieta Kompanowska-Jezierska, Petr Kujal, Herbert J Kramer, Luděk Červenka
BACKGROUND: Early addition of endothelin (ET) type A (ETA) receptor blockade to complex renin-angiotensin system (RAS) blockade has previously been shown to provide better renoprotection against progression of chronic kidney disease (CKD) in Ren-2 transgenic hypertensive rats (TGR) after 5/6 renal ablation (5/6 NX). In this study, we examined if additional protection is provided when ETA blockade is applied in rats with already developed CKD. METHODS: For complex RAS inhibition, an angiotensin-converting enzyme inhibitor along with angiotensin II type 1 receptor blocker was used...
2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/28286190/outcome-of-adults-with-eisenmenger-syndrome-treated-with-drugs-specific-to-pulmonary-arterial-hypertension-a-french-multicentre-study
#18
Sebastien Hascoet, Emmanuelle Fournier, Xavier Jaïs, Lauriane Le Gloan, Claire Dauphin, Ali Houeijeh, Francois Godart, Xavier Iriart, Adelaïde Richard, Jelena Radojevic, Pascal Amedro, Gilles Bosser, Nathalie Souletie, Yvette Bernard, Pamela Moceri, Hélène Bouvaist, Pierre Mauran, Elise Barre, Adeline Basquin, Clement Karsenty, Damien Bonnet, Laurence Iserin, Olivier Sitbon, Jérôme Petit, Elie Fadel, Marc Humbert, Magalie Ladouceur
BACKGROUND: The relationship between pulmonary arterial hypertension-specific drug therapy (PAH-SDT) and mortality in Eisenmenger syndrome (ES) is controversial. AIMS: To investigate outcomes in patients with ES, and their relationship with PAH-SDT. METHODS: Retrospective, observational, nationwide, multicentre cohort study. RESULTS: We included 340 patients with ES: genetic syndrome (n=119; 35.3%); pretricuspid defect (n=75; 22...
March 9, 2017: Archives of Cardiovascular Diseases
https://www.readbyqxmd.com/read/28283735/in-vitro-and-in-vivo-evaluation-of-dasatinib-and-imatinib-on-physiological-parameters-of-pulmonary-arterial-hypertension
#19
Bethany Baumgart, Mausumee Guha, James Hennan, Julia Li, Jochen Woicke, Damir Simic, Michael Graziano, Nicola Wallis, Thomas Sanderson, Roderick Todd Bunch
PURPOSE: Pulmonary arterial hypertension (PAH) results from occlusion or vasoconstriction of pulmonary vessels, leading to progressive right ventricular failure. Dasatinib, a BCR-ABL1 tyrosine kinase inhibitor (TKI) approved for the treatment of chronic myelogenous leukemia, has been associated with PAH. In contrast, the BCR-ABL1 TKI imatinib has demonstrated anti-vasoproliferative properties and has been investigated as a potential treatment for PAH. Here we describe studies evaluating the effects of dasatinib and imatinib on cardiovascular and pulmonary functions to understand the reported differential consequences of the two TKIs in a clinical setting...
March 10, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28283234/endothelin-inhibitors-lower-pulmonary-vascular-resistance-and-improve-functional-capacity-in-patients-with-fontan-circulation
#20
Gabriella Agnoletti, Simona Gala, Francesca Ferroni, Roberto Bordese, Lorenzo Appendini, Carlo Pace Napoleone, Laura Bergamasco
OBJECTIVES: To evaluate the effects of endothelin inhibitors (ERAs) on hemodynamic and functional parameters in patients post-Fontan procedure with high pulmonary vascular resistance (PVR). METHODS: Among our cohort of patients with Fontan circulation, 8 children, 8 adolescents, and 8 adults had PVR ≥2 WU*m(2). These patients were treated with ERAs (minors with bosentan, adults with macitentan) and reevaluated after 6 months. Pre- and posttreatment hemodynamic variables were assessed by cardiac catheterization...
February 10, 2017: Journal of Thoracic and Cardiovascular Surgery
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