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Review Article

选择性MMP-13抑制剂:有望治疗骨性关节炎的药物

卷 27, 期 22, 2020

页: [3753 - 3769] 页: 17

弟呕挨: 10.2174/0929867326666181217153118

价格: $65

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摘要

骨关节炎(OA)是一种年龄相关性退行性疾病，以慢性关节疼痛、炎症和关节软骨损伤为特征。目前，甾体类药物和非甾体类抗炎药(NSAIDS)、选择性环氧合酶-2 (COX-2)抑制剂是治疗OA的一线药物。然而，这些药物可能会导致一些心血管副作用。因此，开发新的治疗OA的药物已成为当务之急。基质金属蛋白酶-13 (Matrix metalloproteinase, MMP-13)是基质金属蛋白酶家族(Matrix metalloproteinases, MMPs)的重要成员，通过降解关节软骨和骨组织中的II型胶原而发挥重要作用。值得注意的是，MMP-13在OA患者中异常表达，而在正常成人中不表达。此外，广谱MMP抑制剂可能会导致一些疼痛和关节僵硬的副作用，在临床试验中称为肌肉骨骼综合征(MSS)。因此，开发选择性MMP-13抑制剂是治疗OA的一个潜在策略。本文综述了选择性MMP-13抑制剂的研究进展，包括锌结合和非锌结合选择性MMP-13抑制剂两个亚家族。

关键词: 骨关节炎，关节软骨，MMP-13，锌结合基，构效关系，选择性抑制剂。

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