Tips review
Molecular characterization of endothelin receptors

https://doi.org/10.1016/0165-6147(92)90038-8Get rights and content

Abstract

Following the first report on the identification of endothelin (ET), an increasing body of work has accumulated on this endothelium-derived 21-amino acid vasoconstrictor peptide. Subsequently, the existence of three distinct isoforms of ET, designated ET-1, ET-2 and ET-3, was predicted from the finding of three separate genes. The differential potencies of the three isoforms of the ET family have opened up the possibility of the existence of multiple ET receptor subtypes. Recently, molecular biological techniques provided direct evidence of at least two distinct subtypes of ET receptor. This article discusses the functions of the ETs, focusing especially on the molecular characteristics of their receptors.

References (41)

  • R. Ikegawa et al.

    Biochem. Biophys. Res. Commun.

    (1990)
  • C. Takasaki et al.

    Toxicon

    (1988)
  • S. Ohkubo

    FEBS Lett.

    (1990)
  • K.D. Bloch et al.

    J. Biol. Chem.

    (1989)
  • T. Sakurai

    Biochem. Biophys. Res. Commun.

    (1991)
  • T.D. Warner et al.

    Eur. J. Phamacol.

    (1989)
  • E.R. Martin et al.

    J. Biol. Chem.

    (1990)
  • H. Watanabe

    Biochem. Biophys. Res. Commun.

    (1989)
  • Y. Masuda

    FEBS Lett.

    (1989)
  • M. Sugiura et al.

    Biochem. Biophys. Res. Commun.

    (1989)
  • S. Nakajo et al.

    Biochem. Biophys. Res. Commun.

    (1989)
  • K. Hosoda

    FEBS Lett.

    (1991)
  • A. Sakamoto

    Biochem. Biophys. Res. Commun.

    (1991)
  • M. Nakamuta

    Biochem. Biophys. Res. Commun.

    (1991)
  • Y. Ogawa

    Biochem. Biophys. Res. Commun.

    (1991)
  • M. Kozuka et al.

    J. Biol. Chem.

    (1991)
  • S. Kimura

    Biochem. Biophys. Res. Commun.

    (1988)
  • K. Nakajima

    Biochem. Biophys. Res. Commun.

    (1989)
  • T. Saeki et al.

    Biochem. Biophys. Res. Commun.

    (1991)
  • M. Ihara

    Biochem. Biophys. Res. Commun.

    (1991)
  • Cited by (642)

    • ET<inf>A</inf> receptors are involved in the febrile response induced by high dose of bacterial endotoxin

      2021, Journal of Thermal Biology
      Citation Excerpt :

      These receptors have different selectivity to the ligand. ET-1 and ET-2 have greater affinity for the ETA receptor than ET-3, while the three ligands have similar affinity for the ETB receptor (Sakurai et al., 1992). ETA and ETB receptors share the same signaling pathway Gq/11 (Houde et al., 2016) although ETB receptors may also be associated with Gs and Gi, which promote activation or inhibition of adenylate cyclase, respectively, thus altering cyclic AMP levels (Davenport, 2002).

    • Endothelin and the heart in health and diseases

      2019, Peptides
      Citation Excerpt :

      The order of affinity of ETs for the first receptor type, designated ETA, is ET-1 > ET-2 > > ET-3. The second receptor type, designated ETB, shows equipotent affinity for all three ETs [41]. Exposure of cultured smooth muscle cells [42], Swiss 3T3 cells [43] and glomerular mesangial cells [44] to ET-1 for a long time causes a marked decrease in 125I-ET-1 binding sites, indicating an autologous down-regulation of ET receptors.

    • Neurobiology of opioid withdrawal: Role of the endothelin system

      2016, Life Sciences
      Citation Excerpt :

      The biological responses of ET-1 are mediated via the activation of two distinct G protein coupled receptors (GPCRs): endothelin-A (ETA) [47] and endothelin-B (ETB) receptors [129]. While all three ETs have equal affinity for the ETB receptor, ET-3 has a lower affinity for the ETA receptor compared with either ET-1 or ET-2 [115]. The global distribution of ET and its binding sites in the brain suggests that, in addition to being a vasoactive agent, ET acts as an important regulatory neuropeptide in the CNS and affects many other biological functions [54,85,128].

    View all citing articles on Scopus
    View full text