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Updated: Jun 12, 2026

Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
Published on: May 24, 2024
[Inhibitors of the receptor A for endothelin-1]
A Villers1, Y Neuzillet, P Beuzeboc
1Service d'urologie, Hôpital Huriez, CHRU Lille, 1 place de Verdun Lille cedex, France. arnauld.villers@wanadoo.fr
Abstract:
Endothelin-1 (ET-1) is a vasoactive peptide but also mitogenic and pro-angiogenic. ET-1 exerts its actions via two G protein-coupled receptors, ETA and ETB. ET-1 is involved in the progression of prostate cancer. Its actions affect the tumor cell proliferation, inhibition of apoptosis, angiogenesis, migration, invasion, metastasis to the bone growth. Inhibitors of receptors of ET-1 in clinical development are the atrasentan and ZD4054. This article reports on controlled, randomized, phase II and III studies on this new therapeutic class.
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