Peptide directoryHeart, vessels & kidneys

Apelin-17

A longer apelin that pulls its receptor into the cell harder.

Where it comes from

Made in
Brain, heart and kidney, cut from the same precursor
Sent out by
With the other apelins
Acts on
  • Vessels
  • Hypothalamus
  • Kidney

What it does

  • Lowers blood pressure more lastingly than apelin-13 in rats 1
  • Pulls the apelin receptor into the cell far more strongly than apelin-13 does, which is the clearest difference between the two 1
  • Stronger at water handling in animal studies, through the vasopressin neurons of the hypothalamus 1

In medicine

  • No medicine, no test and no human infusion study: it has stayed a laboratory peptide
  • It reaches the clinic only through what it taught about the receptor. Removing its last phenylalanine separates the signalling from the internalisation, and that is the design idea behind biased apelin agonists 2

Beyond the body’s own use

  • The work on it is about biased signalling rather than treatment: a ligand that drives the Gi pathway without dragging the receptor inside might lower blood pressure without the receptor going quiet 2
  • Nothing is in trials. Whether the longer apelins are present in human blood in meaningful amounts, or are largely an artefact of how tissue is extracted, is still argued 1
  • The practical reading is that the apelins are one hormone cut to several lengths, and the length decides how long the signal lasts rather than what it says 1

Sources

  1. El Messari et al., Functional dissociation of apelin receptor signalling and endocytosis, Journal of Neurochemistry 2004
  2. Ceraudo et al., Biased signalling favouring Gi over beta-arrestin promoted by an apelin fragment, Journal of Biological Chemistry 2014

This card describes what a medicine is for and what the evidence says; it recommends nothing. Talk to your clinician about anything you read here.