Target intelligence / Profile preview

Advanced glycation end-product receptor (RAGE) (RAGE)

Target
RAGE
Molecular classification
Receptor, Immunoglobulin superfamily
01

Overview

The Advanced glycation end-product receptor (RAGE) is a multi-ligand transmembrane receptor belonging to the immunoglobulin superfamily (UniProt: Q15109). It is characterized by its ability to bind a diverse array of ligands, including advanced glycation end-products (AGEs), high-mobility group box 1 (HMGB1), S100/calgranulin proteins, and amyloid-beta peptides (PubMed: 22424582). Upon ligand binding, RAGE triggers sustained cellular signaling pathways, such as NF-κB activation, which leads to the production of pro-inflammatory cytokines and reactive oxygen species (PubMed: 30107159). This receptor plays a critical role in the pathogenesis of chronic inflammatory states, diabetic complications, neurodegenerative diseases like Alzheimer's, and various cancers (PubMed: 25132144). Therapeutic strategies primarily focus on small molecule antagonists, such as Azeliragon, or soluble RAGE decoys to prevent ligand-receptor interactions and mitigate downstream inflammatory damage (PubMed: 29150444).

Other names
AGERReceptor for advanced glycation end productsReceptor for AGEs
02

Mechanism of action

Antagonism of the receptor to prevent binding of pro-inflammatory ligands such as AGEs, HMGB1, and S100 proteins.

03

Biological functions

Signal transductionImmune responseInflammationCell migrationApoptosisCell proliferation
04

Disease associations

Diabetes mellitusAlzheimer's diseaseCardiovascular diseaseCancerChronic inflammationAtherosclerosis
05

Safety considerations

Potential impact on pulmonary homeostasisOff-target effects due to multi-ligand bindingInterference with normal tissue repair
06

Interacting drugs

Azeliragon

2 more in the full profile.

07

Biomarkers

Soluble RAGE (sRAGE)Endogenous secretory RAGE (esRAGE)High-mobility group box 1 (HMGB1)S100B

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