Related Experiment Video
Updated: Sep 6, 2025
Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
Published on: November 11, 2016
Therapeutic potential of targeting the receptor for advanced glycation end products (RAGE) by small molecule
Harbinder Singh1, Devendra K Agrawal1
1Department of Translational Research, College of Osteopathic Medicine of the Pacific Western University of Health Sciences, Pomona, California, USA.
Abstract:
Receptor for advanced glycation end products (RAGE) is a 45 kDa transmembrane receptor of immunoglobulin family that can bind to various endogenous and exogenous ligands and initiate the inflammatory downstream signaling pathways. RAGE is involved in various disorders including cardiovascular and neurodegenerative diseases, cancer, and diabetes. This review summarizes the structural features of RAGE and its various isoforms along with their pathological effects. Mainly, the article emphasized on the translational significance of antagonizing the interactions of RAGE with its ligands using small molecules reported in the last 5 years and discusses future approaches that could be employed to block the interactions in the treatment of chronic inflammatory ailments. The RAGE inhibitors described in this article could prove as a powerful approach in the management of immune-inflammatory diseases. A critical review of the literature suggests that there is a dire need to dive deeper into the molecular mechanism of action to resolve critical issues that must be addressed to understand RAGE-targeting therapy and long-term blockade of RAGE in human diseases.
Insights
The Receptor for Advanced Glycation End Products (RAGE) plays a key role in inflammation and diseases. Small molecule inhibitors targeting RAGE-ligand interactions show promise for treating chronic inflammatory conditions.
Area of Science:
- Immunology
- Molecular Biology
- Pharmacology
Background:
- Receptor for Advanced Glycation End Products (RAGE) is an immunoglobulin family transmembrane receptor.
- RAGE binds various ligands, initiating inflammatory signaling pathways.
- RAGE is implicated in cardiovascular diseases, neurodegeneration, cancer, and diabetes.
Purpose of the Study:
- To review the structural features and isoforms of RAGE.
- To summarize recent (5-year) small molecule inhibitors targeting RAGE-ligand interactions.
- To discuss future strategies for blocking RAGE in chronic inflammatory diseases.
Main Methods:
- Literature review focusing on RAGE structure, function, and inhibitors.
- Analysis of small molecules developed in the last five years.
- Discussion of translational significance and future therapeutic approaches.
Main Results:
- RAGE isoforms and their pathological roles are summarized.
- Small molecules targeting RAGE-ligand interactions demonstrate therapeutic potential.
- The review highlights the need for deeper mechanistic understanding.
Conclusions:
- RAGE inhibitors offer a promising therapeutic strategy for immune-inflammatory diseases.
- Further research into RAGE's molecular mechanisms is crucial for effective long-term blockade.
- Targeting RAGE interactions is a key area for managing chronic inflammatory ailments.
Related Concept Videos
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
01:27Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
01:12GPCR Desensitization
01:00Enzyme-linked Receptors
Neurotrophin (NT) receptors are a family of RTKs, including trkA, trkB, and trkC (tropomyosin-related kinase) receptors. TrkA is specific for nerve growth factor (NGF), neurotrophin-6, and neurotrophin-7. TrkB binds...