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Traditional treatments can only delay the progression of osteoarthritis, and patients may need joint replacement eventually. As a class of organic compound molecules weighing less than 1000 daltons, small molecule inhibitors can target proteins as the main components of most drugs clinically. Small molecule inhibitors for osteoarthritis are under constant research. In this regard, by reviewing relevant manuscripts, small molecule inhibitors targeting MMPs, ADAMTS, IL-1, TNF, WNT, NF-\u03baB, and other proteins were reviewed. We summarized these small molecule inhibitors with different targets and discussed disease-modifying osteoarthritis drugs based on them. These small molecule inhibitors have good inhibitory effects on osteoarthritis, and this review will provide a reference for the treatment of osteoarthritis.<\/jats:p>","DOI":"10.3390\/jcm12051986","type":"journal-article","created":{"date-parts":[[2023,3,2]],"date-time":"2023-03-02T04:57:38Z","timestamp":1677733058000},"page":"1986","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":25,"title":["Recent Advances in Small Molecule Inhibitors for the Treatment of Osteoarthritis"],"prefix":"10.3390","volume":"12","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-1586-1415","authenticated-orcid":false,"given":"Jianjing","family":"Lin","sequence":"first","affiliation":[{"name":"Department of Sports Medicine and Rehabilitation, Peking University Shenzhen Hospital, Shenzhen 518036, 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