Targeting the receptor for advanced glycation endproducts (RAGE): A medicinal chemistry perspective

Bongarzone, Salvatore, Savickas, Vilius ORCID: https://orcid.org/0000-0002-8059-5619, Luzi, Federico and Gee, Antony D. (2017) Targeting the receptor for advanced glycation endproducts (RAGE): A medicinal chemistry perspective. Journal of Medicinal Chemistry, 60 (17). pp. 7213-7232. ISSN 0022-2623

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Abstract

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.

Item Type: Article
Uncontrolled Keywords: sdg 3 - good health and well-being ,/dk/atira/pure/sustainabledevelopmentgoals/good_health_and_well_being
Faculty \ School: Faculty of Science > School of Chemistry, Pharmacy and Pharmacology
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Depositing User: LivePure Connector
Date Deposited: 21 Nov 2024 09:30
Last Modified: 27 Nov 2024 10:46
URI: https://ueaeprints.uea.ac.uk/id/eprint/97736
DOI: 10.1021/acs.jmedchem.7b00058

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