Decarboxylation of Ang-(1–7) to Ala 1 -Ang-(1–7) leads to significant changes in pharmacodynamics
作者: Anja TetznerMaura NaughtonKinga GebolysJenny EichhorstEsther SalaÓscar VillacañasThomas Walther
作者单位: 1Dept. Pharmacology and Therapeutics, School of Medicine and School of Pharmacy, University College Cork (UCC), Cork, Ireland
2Departments Obstetrics and Paediatric Surgery, University of Leipzig, Leipzig, Germany
3Leibniz-Forschungsinstitut for Molekulare Pharmakologie (FMP), Berlin, Germany
4Mind the Byte SL, Barcelona, Spain
5Institute of Medical Biochemistry and Molecular Biology, University Medicine Greifswald, Greifswald, Germany
刊名: European Journal of Pharmacology, 2018, Vol.833 , pp.116-123
来源数据库: Elsevier Journal
DOI: 10.1016/j.ejphar.2018.05.031
关键词: Ala 1 -Angiotensin-(1–7)Dose-response curveG-proteinsMas receptorMrgD receptorRenin-angiotensin system
原始语种摘要: Abstract(#br)The heptapeptide angiotensin (Ang)-(1–7) is part of the beneficial arm of the renin-angiotensin system. Ang-(1–7) has cardiovascular protective effects, stimulates regeneration, and opposes the often detrimental effects of AngII. We recently identified the G protein-coupled receptors Mas and MrgD as receptors for the heptapeptide. Ala 1 -Ang-(1–7) (Alamandine), a decarboxylated form of Ang-(1–7), has similar vasorelaxant effects, but has been described as only stimulating MrgD. Therefore, this study aimed to characterise the consequences of the lack of the carboxyl group in amino acid 1 on intracellular signalling and to identify the receptor fingerprint for Ala 1 -Ang-(1–7).(#br)In primary endothelial and mesangial cells, Ala 1 -Ang-(1–7) elevated cAMP concentration. Dose...
全文获取路径: Elsevier  (合作)
影响因子:2.592 (2012)

  • receptor 接受体
  • angiotensin 血管紧张肽
  • heptapeptide 七肽
  • leads 引线
  • concentration 浓度
  • cAMP 环腺苷酸
  • blocked 分块
  • beneficial 有利
  • protein 蛋白质
  • intervention