TR47 Opportunity in leaky vasculature

The vasculature, composed of vessels of different morphology and function, distributes blood to all tissues and maintains physiological tissue homeostasis. In pathologies, the vasculature is often affected by and engaged in, the disease process.  In resting conditions, the vasculature continuously leaks solute and small molecules but restricts extravasation of larger molecules and cells. In many diseases, including cancer and chronic inflammatory conditions, the vascular barrier disintegrates and leakage increases and may become chronic.

 

Animal data supports TR47 as a potential leaky vasculature therapy

  • In vitro and in vivo vascular permeability model – Mosnier and Griffin - www.ncbi.nlm.nih.gov/pmc/articles/PMC3537315/

  • 'A synthetic peptide composing PAR1 residues 47-66, TR47, stimulated protective signalling in endothelial cells’. When the TR47 peptide is given to mice that are subjected to VEGF-induced vascular leakage, this APC-mimetic peptide significantly reduces vascular leakage’.

  • 'Protection Against Vascular Leakage in Vivo by a Peptide Mimetic of the Novel Tethered Ligand Generated by Non-Canonical Cleavage of Protease Activated Receptor 1 by Activated Protein C'.