ArticleACS chemical neuroscience2016
Synthesis and Evaluation of [(18)F]RAGER: A First Generation Small-Molecule PET Radioligand Targeting the Receptor for Advanced Glycation Endproducts.
Article in ACS chemical neuroscience, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 35 citations in OpenAlex.
- Protein glycoxidation in neuropsychiatric disorders-from basic research to clinical practice.Redox biology · 2026Review
- Endosome-phagophore linking assemblies for the degradation of membrane/extracellular proteins.Nature communications · 2025Article
- Advance and Prospect of Positron Emission Tomography in Alzheimer's disease research.Molecular psychiatry · 2025Review
- Identifying RAGE inhibitors as potential therapeutics for Alzheimer's disease via integrated in-silico approaches.Scientific reports · 2025Article
- Modulating the RAGE-Induced Inflammatory Response: Peptoids as RAGE Antagonists.Chembiochem : a European journal of chemical biology · 2023Article
- RAGE Inhibitors in Neurodegenerative Diseases.Biomedicines · 2023Review
- Therapeutic potential of targeting the receptor for advanced glycation end products (RAGE) by small molecule inhibitors.Drug development research · 2022Review
- The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.Journal of medicinal chemistry · 2021Review
- Positron Emission Tomography in Animal Models of Alzheimer's Disease Amyloidosis: Translational Implications.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Positron Emission Tomography in Animal Models of Tauopathies.Frontiers in aging neuroscience · 2021Review
- PET Imaging of Neuroinflammation in Alzheimer's Disease.Frontiers in immunology · 2021Review
- Strategies for PET imaging of the receptor for advanced glycation endproducts (RAGE).Journal of pharmaceutical analysis · 2020Article
- Quantitative imaging of the receptor for advanced glycation end-products in prostate cancer.European journal of nuclear medicine and molecular imaging · 2020Article
- Positron Emission Tomography in the Inflamed Cerebellum: Addressing Novel Targets among G Protein-Coupled Receptors and Immune Receptors.Pharmaceutics · 2020Review
- Progress of RAGE Molecular Imaging in Alzheimer's Disease.Frontiers in aging neuroscience · 2020Review
- Microenvironment Remodeling Micelles for Alzheimer's Disease Therapy by Early Modulation of Activated Microglia.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2019Article
- Glycation in Huntington's Disease: A Possible Modifier and Target for Intervention.Journal of Huntington's disease · 2019Review
- Gray matter structural networks are associated with cardiovascular risk factors in healthy older adults.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2018 · on this mapArticle
- Multimodal imaging of the receptor for advanced glycation end-products with molecularly targeted nanoparticles.Theranostics · 2018Article
- Targeted nanoparticles for multimodal imaging of the receptor for advanced glycation end-products.Theranostics · 2018Article
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
The receptor for advanced glycation endproducts (RAGE) is a 35 kDa transmembrane receptor that belongs to the immunoglobulin superfamily of cell surface molecules. Its role in Alzheimer's disease (AD) is complex, but it is thought to mediate influx of circulating amyloid-β into the brain as well as amplify Aβ-induced pathogenic responses. RAGE is therefore of considerable interest as both a diagnostic and a therapeutic target in AD. Herein we report the synthesis and preliminary preclinical evaluation of [(18)F]RAGER, the first small molecule PET radiotracer for RAGE (Kd = 15 nM). Docking studies proposed a likely binding interaction between RAGE and RAGER, [(18)F]RAGER autoradiography showed colocalization with RAGE identified by immunohistochemistry in AD brain samples, and [(18)F]RAGER microPET confirmed CNS penetration and increased uptake in areas of the brain known to express RAGE. This first generation radiotracer represents initial proof-of-concept and a promising first step toward quantifying CNS RAGE activity using PET. However, there were high levels of nonspecific [(18)F]RAGER binding in vitro, likely due to its high log P (experimental log P = 3.5), and rapid metabolism of [(18)F]RAGER in rat liver microsome studies. Therefore, development of second generation ligands with improved imaging properties would be advantageous prior to anticipated translation into clinical PET imaging studies.
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