Targeting the Receptor for Advanced Glycation Endproducts (RAGE): A Medicinal Chemistry Perspective
Open accessAbstract
The receptor for advanced glycation endproducts (RAGE) is an ubiquitous, transmembrane, immunoglobulin-like receptor that exists in multiple isoforms and binds to a diverse range of endogenous extracellular ligands and intracellular effectors. Ligand binding at the extracellular domain of RAGE initiates a complex intracellular signaling cascade, resulting in the production of reactive oxygen species (ROS), immunoinflammatory effects, cellular proliferation, or apoptosis with concomitant upregulation of RAGE itself. To date, research has mainly focused on the correlation between RAGE activity and pathological conditions, such as cancer, diabetes, cardiovascular diseases, and neurodegeneration. Because RAGE plays a role in many pathological disorders, it has become an attractive target for the development of inhibitors at the extracellular and intracellular domains. This review describes the role of endogenous RAGE ligands/effectors in normo- and pathophysiological processes, summarizes the current status of exogenous small-molecule inhibitors of RAGE and concludes by identifying key strategies for future therapeutic intervention.
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The interaction of AGE-RAGE triggers intracellular and extracellular signaling pathways through activation of ERK1/2, MAPK, PI3K, AKT, NADPH oxidase, and NF-κB.
“The interaction of AGE-RAGE triggers intracellular and extracellular signaling pathways through the activation of extracellular signal-regulated kinases 1 and 2 (ERK1/2), mitogen-activated protein kinases (MAPK), phosphoinositide 3-kinase (PI3K), protein kinase B (AKT), NADPH oxidase, and nuclear factor-κB (NF-κB).”
From Advanced glycation end products (AGEs) and other adducts in aging-related diseases and alcohol-mediated tissue injury (2021) · cites this paper as [41]
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Rungratanawanich, W., Qu, Y., Wang, X., Essa, M. M., & Song, B.-J. (2021) · Experimental & Molecular Medicine · doi:10.1038/s12276-021-00561-7 · Cited by 411 · see citing works
Defective mitophagy in Alzheimer’s disease
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The Role of Dietary Advanced Glycation End Products in Metabolic Dysfunction
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Fernando, D. H., Forbes, J. M., Angus, P. W., & Herath, C. B. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms20205037 · Cited by 184 · see citing works
Can Metformin Exert as an Active Drug on Endothelial Dysfunction in Diabetic Subjects
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RAGE Signaling in Skeletal Biology
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- Authors
- Bongarzone, S., Savickas, V., Luzi, F., & Gee, A. D.
- Affiliations
- St Thomas' Hospital (GB)
- Corresponding author
- Bongarzone, Salvatore
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2017-05-08
- Volume
- 60
- Issue
- 17
- Pages
- 7213-7232
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- PMC
- PMC5601361
- OpenAlex
- W2613211673
- Cited by
- 313
- References
- 138
- Citations by year
- 2026: 15 · 2025: 31 · 2024: 40 · 2023: 41 · 2022: 40 · 2021: 53 · 2020: 50 · 2019: 21 · 2018: 20 · 2017: 2
- FWCI
- 3.32
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Locations
- Journal of Medicinal Chemistry (publishedVersion, cc-by)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Research Portal (King's College London) (submittedVersion, cc-by)
- UEA Digital Repository (University of East Anglia) (submittedVersion)
- Funders
- Wellcome Trust (WT 088641/Z/09/Z)
- King's College Hospital NHS Foundation Trust (NA)
- Medical Research Council (MR/K022733/1)
- Engineering and Physical Sciences Research Council (NA)
- National Institute for Health Research (NA)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Clinical Biochemistry › Advanced Glycation End Products research
- Life Sciences › Immunology and Microbiology › Immunology › Galectins and Cancer Biology
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › Aldose Reductase and Taurine
- Keywords
- receptor for advanced glycation end products, RAGE, RAGE inhibitors, small molecule inhibitors, RAGE ligands, intracellular signaling, reactive oxygen species, inflammation, apoptosis, cancer, diabetes mellitus, cardiovascular disease, neurodegeneration, therapeutic target
- MeSH terms
- Receptor for Advanced Glycation End Products, Protein Domains, Animals, Cardiovascular Diseases, Diabetes Mellitus, Humans, Neoplasms, Glycation End Products, Advanced, Reactive Oxygen Species, Neurodegenerative Diseases, Protein Isoforms, Small Molecule Libraries, Drug Discovery, Molecular Targeted Therapy
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