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Article

Distinct ETA receptor binding mode of macitentan as determined by site directed mutagenesis.

PloS one - 1 Jan 2014

Gatfield John, Mueller Grandjean Celia, Bur Daniel, Bolli Martin H, Nayler Oliver

Abstract excerpt

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 increased receptor occupancy half-life, causing insurmountable antagonism of ET-1-induced signaling in pulmonary arterial...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Share to Mutagenesis, Site-Directed

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Source

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Identifiers

PMID: 25226600
DOI: 10.1371/journal.pone.0107809
PMCID: PMC4166607

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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