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Endothelin 1

Endothelin 1 ( ET-1 ), also known as preproendothelin-1 (PPET1), is the most potent vasoconstrictor produced by the human body. [ 5 ] It is a peptide produced by vascular endoth...

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Endothelin 1 (ET-1), also known as preproendothelin-1 (PPET1), is the most potent vasoconstrictor produced by the human body.[5] It is a peptide produced by vascular endothelial cells,[6] as well as by cells in the heart (affecting contractility) and kidney (affecting sodium handling).[7] The protein encoded by this gene –EDN1– is proteolytically processed to release endothelin 1. Endothelin 1 is one of three isoforms of human endothelin.

Sources

Preproendothelin is precursor of the peptide ET-1. Endothelial cells convert preproendothelin to proendothelin and subsequently to mature endothelin, which the cells release.[6][8]

Clinical significance

Patients with salt-sensitive hypertension have higher plasma ET-1.[7]Endothelin-1 receptor antagonists (Bosentan) are used in the treatment of pulmonary hypertension.[6] Use of these antagonists prevents pulmonary arterial constriction and thus inhibits pulmonary hypertension.[6]

As of 2020, the role of endothelin-1 in affecting lipid metabolism and insulin resistance in obesity mechanisms was under clinical research.[9]

References

  1. 123GRCh38: Ensembl release 89: ENSG00000078401–Ensembl, May 2017
  2. 123GRCm38: Ensembl release 89: ENSMUSG00000021367–Ensembl, May 2017
  3. ↑"Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ↑"Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ↑ Dhaun N, Webb DJ (agosto de 2019). "Endotelinas en la biología y terapéutica cardiovascular". Nature Reviews. Cardiology . 16 (8): 491– 502. doi : 10.1038/s41569-019-0176-3 . hdl : 20.500.11820/70834c34-9404-4855-89c2-8a0fb1016ba8 . PMID 30867577 . 
  6. 1 2 3 4 Davenport AP, Hyndman KA, Dhaun N, Southan C, Kohan DE, Pollock JS, et al. (abril de 2016). " Endotelina" . Pharmacological Reviews . 68 (2): 357– 418. doi : 10.1124/pr.115.011833 . PMC 4815360. PMID 26956245 .   
  7. 1 2 Jankowich M, Choudhary G (2020). "Niveles de endotelina-1 y eventos cardiovasculares". Tendencias en Medicina Cardiovascular . 30 (1): 1– 8. doi : 10.1016/j.tcm.2019.01.007 . PMID 30765295 . 
  8. ↑ Boulpaep EL, Boron WF (2009). Fisiología médica: un enfoque celular y molecular . Saunders/Elsevier. ISBN 978-1-4160-3115-4.
  9. ↑ Jenkins HN, Rivera-Gonzalez O, Gibert Y, Speed ​​JS (diciembre de 2020). "Endotelina-1 en la fisiopatología de la obesidad y la resistencia a la insulina" . Obesity Reviews . 21 (12) e13086. doi : 10.1111/obr.13086 . PMC 7669671. PMID 32627269 .  
  • Resumen de toda la información estructural disponible en el PDB para UniProt : P05305 (Endotelina-1) en el PDBe-KB .

Este artículo incorpora texto de la Biblioteca Nacional de Medicina de los Estados Unidos , que es de dominio público .