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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...

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Detalles Bibliográficos
Autores principales: Gatfield, John, Mueller Grandjean, Celia, Bur, Daniel, Bolli, Martin H., Nayler, Oliver
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2014
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