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Targeting the Receptor for Advanced Glycation Endproducts (RAGE): A Medicinal Chemistry Perspective
[Image: see text] 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 do...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical
Society
2017
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5601361/ https://www.ncbi.nlm.nih.gov/pubmed/28482155 http://dx.doi.org/10.1021/acs.jmedchem.7b00058 |
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author | Bongarzone, Salvatore Savickas, Vilius Luzi, Federico Gee, Antony D. |
author_facet | Bongarzone, Salvatore Savickas, Vilius Luzi, Federico Gee, Antony D. |
author_sort | Bongarzone, Salvatore |
collection | PubMed |
description | [Image: see text] 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. |
format | Online Article Text |
id | pubmed-5601361 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | American Chemical
Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-56013612017-09-19 Targeting the Receptor for Advanced Glycation Endproducts (RAGE): A Medicinal Chemistry Perspective Bongarzone, Salvatore Savickas, Vilius Luzi, Federico Gee, Antony D. J Med Chem [Image: see text] 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. American Chemical Society 2017-05-08 2017-09-14 /pmc/articles/PMC5601361/ /pubmed/28482155 http://dx.doi.org/10.1021/acs.jmedchem.7b00058 Text en Copyright © 2017 American Chemical Society This is an open access article published under a Creative Commons Attribution (CC-BY) License (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) , which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited. |
spellingShingle | Bongarzone, Salvatore Savickas, Vilius Luzi, Federico Gee, Antony D. Targeting the Receptor for Advanced Glycation Endproducts (RAGE): A Medicinal Chemistry Perspective |
title | Targeting the Receptor
for Advanced Glycation Endproducts
(RAGE): A Medicinal Chemistry Perspective |
title_full | Targeting the Receptor
for Advanced Glycation Endproducts
(RAGE): A Medicinal Chemistry Perspective |
title_fullStr | Targeting the Receptor
for Advanced Glycation Endproducts
(RAGE): A Medicinal Chemistry Perspective |
title_full_unstemmed | Targeting the Receptor
for Advanced Glycation Endproducts
(RAGE): A Medicinal Chemistry Perspective |
title_short | Targeting the Receptor
for Advanced Glycation Endproducts
(RAGE): A Medicinal Chemistry Perspective |
title_sort | targeting the receptor
for advanced glycation endproducts
(rage): a medicinal chemistry perspective |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5601361/ https://www.ncbi.nlm.nih.gov/pubmed/28482155 http://dx.doi.org/10.1021/acs.jmedchem.7b00058 |
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