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DOI: 10.1016/j.ejmech.2025.117600

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Medicinal Research Reviews, 2024, 44, 2291
DOI: 10.1002/med.22043

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DOI: 10.1042/BST20230358

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Cell Commun Signal, 2024, 22
DOI: 10.1186/s12964-023-01460-2

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J. Med. Chem., 2023, 66, 9916
DOI: 10.1021/acs.jmedchem.3c00769

Small molecules in the treatment of COVID-19

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Sig Transduct Target Ther, 2022, 7
DOI: 10.1038/s41392-022-01249-8

Design, molecular characterization and therapeutic investigation of a novel CCR8 peptide antagonist that attenuates acute liver injury by inhibiting infiltration and activation of macrophages

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Acta Pharmaceutica Sinica B, 2025, 15, 2114
DOI: 10.1016/j.apsb.2025.02.018

Mechanistic insights into inhibition of CCL2-guided leukocyte recruitment by oxyresveratrol and its derivatives

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DOI: 10.1016/j.molliq.2024.124218

Ethanol-Extracted Acorn Induces Anti-Inflammatory Effects in Human Keratinocyte and Production of Hyaluronic Acid in Human Fibroblasts

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Journal of Medicinal Food, 2023, 26, 595
DOI: 10.1089/jmf.2022.K.0128

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Chemistry A European J, 2023, 29
DOI: 10.1002/chem.202202565

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DOI: 10.1080/07391102.2023.2171136

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ChemMedChem, 2024, 19
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