Drug intelligence / Profile preview

RAGE antagonist peptide

Development stage
Preclinical
Modality
Peptides
Administration
Intraperitoneal, Intravenous
01

Overview

RAGE antagonist peptide (RAP) is a synthetic, S100P-derived decapeptide (sequence: Ac-ELKVLMEKEL-NH2) that acts as a competitive antagonist of the Receptor for Advanced Glycation Endproducts (RAGE). Developed by researchers at the University of Texas MD Anderson Cancer Center and NYU Langone Medical Center, RAP mimics the RAGE-binding domain of S100P (amino acids 32–41) to competitively block the interaction of RAGE with its major pro-inflammatory and oncogenic ligands, including S100P, S100A4, and HMGB1. By preventing ligand-receptor binding, RAP inhibits downstream RAGE-mediated signaling pathways, such as the activation of NF-κB and MAPKs. It has demonstrated preclinical efficacy in reducing tumor growth, metastasis, and inflammation in models of pancreatic cancer, glioma, asthma, emphysema, and acute respiratory distress syndrome (ARDS).

Other names
Ac-ELKVLMEKEL-NH2Ac-ELKVLMEKEL-NH-2Ac-ELKVLMEKEL-NH 2RAGE antagonistic peptideS100P-derived RAGE antagonistic peptideS-100P-derived RAGE antagonistic peptideS 100P-derived RAGE antagonistic peptide
02

Targets

HMGB1 (High mobility group protein B1)S100A12 (S100 calcium-binding protein A12)S100A4 (Ferroptosis suppressor protein 1)S100P (S100 calcium-binding protein P)AGER (RAGE)

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