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10.1021/acs.jmedchem.7b00058

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suck abstract from ncbi


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pmid28482155
      J+Med+Chem 2017 ; 60 (17 ): 7213-7232
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  • Targeting the Receptor for Advanced Glycation Endproducts (RAGE): A Medicinal Chemistry Perspective #MMPMID28482155
  • Bongarzone S ; Savickas V ; Luzi F ; Gee AD
  • J Med Chem 2017[Sep]; 60 (17 ): 7213-7232 PMID28482155 show ga
  • 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.
  • |Animals [MESH]
  • |Cardiovascular Diseases/drug therapy/metabolism [MESH]
  • |Diabetes Mellitus/drug therapy/metabolism [MESH]
  • |Drug Discovery/*methods [MESH]
  • |Glycation End Products, Advanced/metabolism [MESH]
  • |Humans [MESH]
  • |Molecular Targeted Therapy/methods [MESH]
  • |Neoplasms/drug therapy/metabolism [MESH]
  • |Neurodegenerative Diseases/drug therapy/metabolism [MESH]
  • |Protein Domains/drug effects [MESH]
  • |Protein Isoforms/antagonists & inhibitors/chemistry/metabolism [MESH]
  • |Reactive Oxygen Species/metabolism [MESH]
  • |Receptor for Advanced Glycation End Products/*antagonists & inhibitors/chemistry/*metabolism [MESH]


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