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摘要
新出现的证据支持一种相互交织的框架,在一个共同的病理背景下不同的炎症途径参与许多疾病。花生四烯酸通过环氧合酶-2 (COX-2)和15-脂氧合酶(15-LOX)代谢的途径是重要的。酶活性及其产物涉及一系列病理生理过程,包括代谢损伤导致脂肪炎症和随后的血管和神经疾病,以及各种促肿瘤和抗肿瘤作用。更复杂的是,COX-2和15-LOX活性和代谢产物相互作用或作用于其他细胞靶点,其中最突出的是过氧化物酶体增殖物激活受体γ (PPARγ)。因此,有效的治疗干预,这类多面障碍需要同时调节多个靶点。在这里,我们描述了COX-2、15-LOX和PPARγ在癌症和代谢紊乱并发症中的作用,强调了设计多靶点定向配体(mtdl)修饰其活性的价值,并对这些配体设计和合成的原理、可行性及其已知的生物学效应进行了综述。我们推测MTDL在这些疾病中的潜在影响,并强调需要结构化的未来努力来转化这些早期结果,促进这些和类似的分子在临床研究中的采用。
关键词: 多靶点定向配体,环氧化酶-2
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