Drug intelligence / Profile preview

rgd-peptide

Development stage
Preclinical
Lead developer
Cleveland Clinic
Modality
Peptides
Administration
Intravenous, Intraperitoneal
01

Overview

RGD-peptides are a class of therapeutic and diagnostic agents characterized by the Arginine-Glycine-Aspartate (RGD) amino acid sequence. This motif is the minimal recognition sequence for several members of the integrin family, including integrin αvβ3, αvβ5, and α5β1, which are often overexpressed on tumor cells and angiogenic endothelial cells. By binding to these integrins, RGD-peptides can competitively inhibit cell adhesion to the extracellular matrix, disrupt pro-angiogenic signaling pathways (such as FAK and ERK), and induce apoptosis in endothelial cells. In glioblastoma research, RGD-peptides have been utilized to disrupt the perivascular niche interaction between cancer stem cells (CSCs) and endothelial cells, leading to reduced tumor growth and vascularization. Beyond direct therapeutic use, they are widely employed as targeting ligands for the delivery of nanoparticles, radiopharmaceuticals, and cytotoxic drugs to integrin-expressing tissues.

Other names
RGD peptideArg-Gly-Asp peptideRGD-containing peptide
02

Targets

ITGA5:ITGB1 (Integrin α5β1)αVβ3 (Integrin αVβ3)αVβ5 (Integrin αVβ5)

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