Results 61 to 70 of about 2,334,067 (354)

Slow Receptor Dissociation Kinetics Differentiate Macitentan from Other Endothelin Receptor Antagonists in Pulmonary Arterial Smooth Muscle Cells

PLoS ONE, 2012
Two endothelin receptor antagonists (ERAs), bosentan and ambrisentan, are currently approved for the treatment of pulmonary arterial hypertension (PAH), a devastating disease involving an activated endothelin system and aberrant contraction and ...
J. Gatfield, Celia Mueller Grandjean, T. Sasse, M. Clozel, O. Nayler   +4 more
semanticscholar   +1 more source

Absence of Functional Autoantibodies Targeting Angiotensin II Receptor Type 1 and Endothelin‐1 Type A Receptor in Circulation and Purified IgG From Patients With Systemic Sclerosis

Arthritis &Rheumatology, EarlyView.
Objective Systemic sclerosis (SSc) is a rare but severe autoimmune disease characterized by immune dysregulation, fibrosis, and vasculopathy. Although previous studies have highlighted the presence of functional autoantibodies targeting the angiotensin II receptor type 1 (AT1) and endothelin‐1 type A receptor (ETAR), leading to autoantibody‐mediated ...
Wieke M. van Oostveen, Eva M. Hoekstra, E. W. Nivine Levarht, Ilana B. Kotliar, Thomas P. Sakmar, René E. M. Toes, Jeska K. de Vries‐Bouwstra, Laura H. Heitman, Cynthia M. Fehres   +8 more
wiley   +1 more source

Race and sex differences in response to endothelin receptor antagonists for pulmonary arterial hypertension.

Chest, 2012
BACKGROUND Recently studied therapies for pulmonary arterial hypertension (PAH) have improved outcomes among populations of patients, but little is known about which patients are most likely to respond to specific treatments.
Nicole B Gabler, B. French, B. Strom, Ziyue Liu, H. Palevsky, D. Taichman, S. Kawut, S. Halpern   +7 more
semanticscholar   +1 more source

Serum Type I Interferon Score for Prediction of Clinically Meaningful Disease Progression in Limited Cutaneous Systemic Sclerosis

Arthritis &Rheumatology, EarlyView.
Objective To assess the value of serum type I interferon (IFN) score in predicting clinically meaningful progression in limited cutaneous systemic sclerosis (lcSSc) using a novel composite endpoint adopted from the MINIMISE clinical trial. Methods A retrospective, longitudinal lcSSc cohort was identified within a national, multicenter observational ...
Stefano Di Donato, Rebecca Ross, Ranjitha Karanth, Vishal Kakkar, Enrico De Lorenzis, Lesley‐Anne Bissell, Kristina Clark, Philip Yee, Christopher P. Denton, Francesco Del Galdo   +9 more
wiley   +1 more source

Endothelin‐1 and Endothelin Receptor Antagonists in Cardiovascular Remodeling

Proceedings of the Society for Experimental Biology and Medicine, 1999
Endothelins build a peptide family composed of three isoforms, each of them containing 21 amino acids. Endothelin‐1 is the isoform mainly responsible for any cardiovascular action and therefore the sole scope of this review. Endothelin‐1 is the most potent endogenous vasoconstrictor known; in addition it acts as a potent (co)mitogen.
Klaus Münter, Michael Kirchengast
openaire   +3 more sources

Combinatorial targeting of early pathways profoundly inhibits neurodegeneration in a mouse model of glaucoma

Neurobiology of Disease, 2014
The endothelin system is implicated in various human and animal glaucomas. Targeting the endothelin system has great promise as a treatment for human glaucoma, but the cell types involved and the exact mechanisms of action are not clearly elucidated ...
Gareth R. Howell, Katharine H. MacNicoll, Catherine E. Braine, Ileana Soto, Danilo G. Macalinao, Gregory L. Sousa, Simon W.M. John   +6 more
doaj  

Therapeutic efficacy of TBC3711 in monocrotaline-induced pulmonary hypertension

Respiratory Research, 2011
Background Endothelin-1 signalling plays an important role in pathogenesis of pulmonary hypertension. Although different endothelin-A receptor antagonists are developed, a novel therapeutic option to cure the disease is still needed.
Brandes Ralf P, Janssen Wiebke, Cornitescu Teodora, Sydykov Akylbek, Dahal Bhola K, Luitel Himal, Kojonazarov Baktybek, Kosanovic Djuro, Davie Neil, Ghofrani Hossein A, Weissmann Norbert, Grimminger Friedrich, Seeger Werner, Schermuly Ralph T   +13 more
doaj   +1 more source

The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.

Journal of Medicinal Chemistry, 2012
Starting from the structure of bosentan (1), we embarked on a medicinal chemistry program aiming at the identification of novel potent dual endothelin receptor antagonists with high oral efficacy.
M. Bolli, C. Boss, C. Binkert, Stephan Buchmann, D. Bur, P. Hess, M. Iglarz, Solange Meyer, J. Rein, Markus Rey, A. Treiber, M. Clozel, W. Fischli, T. Weller   +13 more
semanticscholar   +1 more source

Activin A‐activated ALK4 induces pathogenic Th17 involved endothelial–mesenchymal transition in systemic lupus erythematosus‐associated pulmonary arterial hypertension

Arthritis &Rheumatology, Accepted Article.
Objective Autoimmune diseases, such as systemic lupus erythematosus (SLE), are associated with pulmonary arterial hypertension (PAH), a condition that can lead to heart failure. However, whether T cells also contribute to the occurrence of PAH in SLE, has not been clarified.
Shuliang Jing, Junyan Qian, Hongjie Ying, Pei Mao, Mingxin Yao, Zhihong Wu, Harm J Bogaard, Lie Wang, Mengtao Li, Jun Yang   +9 more
wiley   +1 more source

Fluorescence Correlation Spectroscopy in Drug Discovery: Study of Alexa532-Endothelin 1 Binding to the Endothelin ETA Receptor to Describe the Pharmacological Profile of Natural Products

The Scientific World Journal, 2012
Fluorescence correlation spectroscopy and the newly synthesized Alexa532-ET1 were used to study the dynamics of the endothelin ETA receptor-ligand complex alone and under the influence of a semisynthetic selective antagonist and a fungal extract on ...
Catherina Caballero-George, Thomas Sorkalla, Daniel Jakobs, Jessica Bolaños, Huzefa Raja, Carol Shearer, Eldredge Bermingham, Hanns Häberlein   +7 more
doaj   +1 more source