Unique receptor dissociation kinetics of the novel endothelin receptor antagonist, macitentan

Characterizing a drug candidate for Gq coupled GPCR

This Poster summarizes a study from the Actelion Drug Discovery Department, characterizing the inhibitory potency of the drug candidate macitentan on ETA and ETB4,5, two GPCRs involved in pulmonary arterial hypertension (PAH).

Features:

  • Methodology followed by the authors
  • Key results of the study (antagonist potency and binding kinetics)
  • Conclusion suggesting the unique effectiveness of the macitentan compound

Dissociation-kinetics-of-endothelin-receptor-antagonist-macitentan-Mockup.jpg

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Inositol-Phosphate: a new era for Gq couple GPCR signaling

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