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L’endothéline : de la découverte aux avancées pharmacothérapeutiques

Abstract : Endothelin: From discovery to pharmacotherapeutic innovations Objectives > Endothelin (ET) is a major therapeutic target in cardiopulmonary diseases. The purpose of this review is to present the main concepts concerning ET biology, its patho-physiological roles and the major pharmacological and medical advances recently developed around the concept of ET receptor blockade. Methods > Analysis of PubMed database (keywords: endothe-lin, endothelin receptor antagonists, pulmonary hypertension, etc.), and of abstract originating from recent international meetings. Results > ET is a peptide produced by vascular endothelial cells as well as by many other tissues. Both its production and its effects are activated in pathological situations associated with endothelial dysfunction. ET is characterized by a strong tropism toward tissues because of its polarized release, the strong tissue receptor density and high affinity of the receptors for the peptide. ET exerts several vascular effects, including vasocons-triction, proliferation and hypertrophy, as well as non-vascular effects, notably stimulation of cardiac hypertrophy, tissue fibrosis and inflammation. Both vascular and non-vascular effects depend on the stimulation of two receptor subtypes, ET A and ET B. ET receptor antagonists (ERA) demonstrated Résumé
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Vincent Richard. L’endothéline : de la découverte aux avancées pharmacothérapeutiques. La Presse Médicale, Elsevier Masson, 2014, 43 (7-8), pp.742-755. ⟨10.1016/j.lpm.2014.01.015⟩. ⟨inserm-02296636⟩



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