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Distinct ET(A) Receptor Binding Mode of Macitentan As Determined by Site Directed Mutagenesis
The competitive endothelin receptor antagonists (ERA) bosentan and ambrisentan, which have long been approved for the treatment of pulmonary arterial hypertension, are characterized by very short (1 min) occupancy half-lives at the ET(A) receptor. The novel ERA macitentan, displays a 20-fold increas...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Public Library of Science
2014
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4166607/ https://www.ncbi.nlm.nih.gov/pubmed/25226600 http://dx.doi.org/10.1371/journal.pone.0107809 |