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A novel cyclic biased agonist of the apelin receptor, MM07, is disease modifying in the rat monocrotaline model of pulmonary arterial hypertension.

British journal of pharmacology | 2019

Apelin is an endogenous vasodilatory and inotropic peptide that is down-regulated in human pulmonary arterial hypertension, although the density of the apelin receptor is not significantly attenuated. We hypothesised that a G protein-biased apelin analogue MM07, which is more stable than the endogenous apelin peptide, may be beneficial in this condition with the advantage of reduced β-arrestin-mediated receptor internalisation with chronic use.

Pubmed ID: 30710493 RIS Download

Associated grants

  • Agency: Wellcome Trust, United Kingdom
    Id: 203814/Z/16/A
  • Agency: British Heart Foundation, United Kingdom
    Id: PG/13/91/30579
  • Agency: British Heart Foundation, United Kingdom
    Id: RG/13/4/30107
  • Agency: Medical Research Council, United Kingdom
    Id: MC_PC_14116
  • Agency: Wellcome Trust, United Kingdom
    Id: 107715/Z/15/Z
  • Agency: Wellcome Trust, United Kingdom
    Id: 096822/Z/11/Z
  • Agency: British Heart Foundation, United Kingdom
    Id: FS/14/59/31282

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