ArticleProceedings of the National Academy of Sciences of the United States of America2008
Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers.
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Who cites it
46 citing papers in PubMed, 111 citations in OpenAlex.
- One-Step Photoreduction of Nitroarenes to Nitrosoarenes.Organic letters · 2026Article
- Rapamycin Treatment Reduces Brain Pericyte Constriction in Ischemic Stroke.Translational stroke research · 2025Article
- The molecular genetics of PI3K/PTEN/AKT/mTOR pathway in the malformations of cortical development.Genes & diseases · 2024Review
- Local blockade of tacrolimus promotes T-cell-mediated tumor regression in systemically immunosuppressed hosts.Journal for immunotherapy of cancer · 2023Article
- Survival of intracellular pathogens in response to mTORC1- or TRPML1-TFEB-induced xenophagy.Autophagy reports · 2023Article
- Structural mechanism of allosteric activation of TRPML1 by PI(3,5)PProceedings of the National Academy of Sciences of the United States of America · 2022Article
- Alleviation of cisplatin-induced neuropathic pain, neuronal apoptosis, and systemic inflammation in mice by rapamycin.Frontiers in aging neuroscience · 2022Article
- In Silico Strategy for Targeting the mTOR Kinase at Rapamycin Binding Site by Small Molecules.Molecules (Basel, Switzerland) · 2021Article
- The Resurrection of Phenotypic Drug Discovery.ACS medicinal chemistry letters · 2020Article
- Development of Non-Immunosuppressive FK506 Derivatives as Antifungal and Neurotrophic Agents.Journal of microbiology and biotechnology · 2020Review
- Immortalized Dorsal Root Ganglion Neuron Cell Lines.Frontiers in cellular neuroscience · 2020Review
- Construction and Validation of a 13-Gene Signature for Prognosis Prediction in Medulloblastoma.Frontiers in genetics · 2020Article
- High-throughput microscopy exposes a pharmacological window in which dual leucine zipper kinase inhibition preserves neuronal network connectivity.Acta neuropathologica communications · 2019Article
- Rapamycin directly activates lysosomal mucolipin TRP channels independent of mTOR.PLoS biology · 2019Article
- Rapamycin and FK506 derivative TH2849 could ameliorate neurodegenerative diseases through autophagy with low immunosuppressive effect.CNS neuroscience & therapeutics · 2019Article
- Endogenous TRPV4 Expression of a Hybrid Neuronal Cell Line N18D3 and Its Utilization to Find a Novel Synthetic Ligand.Journal of molecular neuroscience : MN · 2017Article
- Applications of Nonenzymatic Catalysts to the Alteration of Natural Products.Chemical reviews · 2017Review
- An overview of rapamycin: from discovery to future perspectives.Journal of industrial microbiology & biotechnology · 2017Review
- Rapamycin ameliorates cadmium-induced activation of MAPK pathway and neuronal apoptosis by preventing mitochondrial ROS inactivation of PP2A.Neuropharmacology · 2016Article
- How longevity research can lead to therapies for Alzheimer's disease: The rapamycin story.Experimental gerontology · 2015Review
Corrections and comments
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Authors and funding
23 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Rapamycin is an immunosuppressive immunophilin ligand reported as having neurotrophic activity. We show that modification of rapamycin at the mammalian target of rapamycin (mTOR) binding region yields immunophilin ligands, WYE-592 and ILS-920, with potent neurotrophic activities in cortical neuronal cultures, efficacy in a rodent model for ischemic stroke, and significantly reduced immunosuppressive activity. Surprisingly, both compounds showed higher binding selectivity for FKBP52 versus FKBP12, in contrast to previously reported immunophilin ligands. Affinity purification revealed two key binding proteins, the immunophilin FKBP52 and the beta1-subunit of L-type voltage-dependent Ca(2+) channels (CACNB1). Electrophysiological analysis indicated that both compounds can inhibit L-type Ca(2+) channels in rat hippocampal neurons and F-11 dorsal root ganglia (DRG)/neuroblastoma cells. We propose that these immunophilin ligands can protect neurons from Ca(2+)-induced cell death by modulating Ca(2+) channels and promote neurite outgrowth via FKBP52 binding.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.