Targeting the CSF-1/CSF-1R Axis: Exploring the Potential of CSF1R Inhibitors in Neurodegenerative Diseases
DC Field | Value | Language |
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dc.contributor.author | Baek, Jihyun | - |
dc.contributor.author | Jun, Joonhong | - |
dc.contributor.author | Kim, Hyejin | - |
dc.contributor.author | Bae, Hyunah | - |
dc.contributor.author | Park, Haebeen | - |
dc.contributor.author | Cho, Hyunwook | - |
dc.contributor.author | Han, Songhee | - |
dc.contributor.author | Shin, Ho Chul | - |
dc.contributor.author | Hah, Jung-Mi | - |
dc.date.accessioned | 2024-04-12T05:30:26Z | - |
dc.date.available | 2024-04-12T05:30:26Z | - |
dc.date.issued | 2024-03 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.issn | 1520-4804 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/118726 | - |
dc.description.abstract | We report herein the potential of colony-stimulating factor-1 receptor (CSF1R) inhibitors as therapeutic agents in neuroinflammatory diseases, with a focus on Alzheimer's disease (AD). Employing a carefully modified scaffold, N-(4-heterocycloalkyl-2-cycloalkylphenyl)-5-methylisoxazole-3-carboxamide, we identify highly selective and potent CSF1R inhibitors & horbar;7dr(i) and 7ds(i). Molecular docking studies shed light on the binding modes of these key compounds within the CSF1R binding site. Remarkably, kinome-wide selectivity assessment underscores the impressive specificity of 7dr(i) for CSF-1R. Notably, 7dr(i) emerges as a potent CSF-1R inhibitor with favorable cellular activity and minimal cytotoxicity among the synthesized compounds. Demonstrating efficacy in inhibiting CSF1R phosphorylation in microglial cells and successfully mitigating neuroinflammation in an in vivo LPS-induced model, 7dr(i) establishes itself as a promising antineuroinflammatory agent. | - |
dc.format.extent | 22 | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | American Chemical Society | - |
dc.title | Targeting the CSF-1/CSF-1R Axis: Exploring the Potential of CSF1R Inhibitors in Neurodegenerative Diseases | - |
dc.type | Article | - |
dc.publisher.location | 미국 | - |
dc.identifier.doi | 10.1021/acs.jmedchem.3c02366 | - |
dc.identifier.scopusid | 2-s2.0-85188990746 | - |
dc.identifier.wosid | 001191233700001 | - |
dc.identifier.bibliographicCitation | Journal of Medicinal Chemistry, v.67, no.7, pp 1 - 22 | - |
dc.citation.title | Journal of Medicinal Chemistry | - |
dc.citation.volume | 67 | - |
dc.citation.number | 7 | - |
dc.citation.startPage | 1 | - |
dc.citation.endPage | 22 | - |
dc.type.docType | Article | - |
dc.description.isOpenAccess | N | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.subject.keywordPlus | NEUROINFLAMMATION | - |
dc.subject.keywordPlus | ISOXAZOLE | - |
dc.subject.keywordPlus | FMS | - |
dc.identifier.url | https://pubs.acs.org/doi/10.1021/acs.jmedchem.3c02366 | - |
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