Azeliragon

Overview

Azeliragon (TTP488) is an orally bioavailable small molecule that inhibits the receptor for advanced glycation endproducts (RAGE).

Mechanism of Action

RAGE is a multiligand, transmembrane pattern recognition receptor of the immunoglobulin family.   Under normal physiologic states expression of RAGE is limited; however, with inflammatory processes and increased concentrations of RAGE ligands, there is upregulation of its expression in cells involved in immuno-inflammatory responses (e.g., monocytes/macrophages and T-cells), endothelial cells, and vascular smooth muscle cells.   Interaction between RAGE and ligands, such as AGEs, Aβ peptides, S100 proteins, HMGB1 (amphoterin) and oxLDL, promotes pro-inflammatory gene activation, thereby contributing to a diverse array of chronic immuno-inflammatory disorders. 

 

RAGE Mechanism Publications

 

  1. Bierhaus A, Humpert PM, Morcos M, Wendt T, Chavakis T, Arnold B, et al. Understanding RAGE, the receptor for advanced glycation end products. J Mol Med. 2005 Nov;83(11):876-86. Abstract link:  http://www.ncbi.nlm.nih.gov/pubmed/16133426
  2. Stern D, Yan SD, Yan SF, Schmidt AM. Receptor for advanced glycation endproducts: a multiligand receptor magnifying cell stress in diverse pathologic settings. Adv Drug Deliv Rev. 2002;54(12):1615-25. Abstract link: http://www.ncbi.nlm.nih.gov/pubmed/12453678

 

Publications

Links to the following publications and presentations, which are located on outside websites, are provided for informational purposes only and do not constitute the opinions or views of vTv Therapeutics

Presentations and Posters

Links to the following publications and presentations, which are located on outside websites, are provided for informational purposes only and do not constitute the opinions or views of vTv Therapeutics