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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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Autors principals: Gatfield, John, Mueller Grandjean, Celia, Bur, Daniel, Bolli, Martin H., Nayler, Oliver
Format: Artigo
Idioma:Inglês
Publicat: Public Library of Science 2014
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Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC4166607/
https://ncbi.nlm.nih.gov/pubmed/25226600
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1371/journal.pone.0107809
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