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Updated: Jun 21, 2026

Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
Published on: May 24, 2024
Therapeutic potential of endothelin receptor modulators: lessons from human clinical trials
John-David Aubert1, Lucienne Juillerat-Jeanneret
1University Institute of Pathology, University of Lausanne (UNIL), Centre Hospitalier Universitaire Vaudois (CHUV), Lausanne, Switzerland.
Abstract:
The endothelin system, and in particular endothelin receptors, are targets for therapeutic intervention in human diseases. Endothelin receptor antagonists have reached clinical use for treating pulmonary arterial hypertension, and are under clinical investigation for several other diseases, such as cancer, vasospasm or fibrogenic diseases. We review the molecules that have been evaluated in the main clinical trials, from the point of view of receptor selectivity and of their chemical characteristics which were important for efficacy in pulmonary hypertension. We will also discuss future use of antagonists to endothelin receptor(s) in several human diseases and what should be the necessary properties of the future molecules for efficacy in diseases where the presently tested molecules displayed suboptimal efficacy.
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