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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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Detalhes bibliográficos
Main Authors: Gatfield, John, Mueller Grandjean, Celia, Bur, Daniel, Bolli, Martin H., Nayler, Oliver
Formato: Artigo
Idioma:Inglês
Publicado em: Public Library of Science 2014
Assuntos:
Acesso em linha: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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