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首页> 外文期刊>Current medicinal chemistry >Qin, J.-J.a , Nag, S.a , Voruganti, S.a , Wang, W.a , Zhang, R.a b Natural product MDM2 inhibitors: Anticancer activity and mechanisms of action
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Qin, J.-J.a , Nag, S.a , Voruganti, S.a , Wang, W.a , Zhang, R.a b Natural product MDM2 inhibitors: Anticancer activity and mechanisms of action

机译：Qin，J.-J.a，Nag，S.a，Voruganti，S.a，Wang，W.a，Zhang，R.a b天然产物MDM2抑制剂：抗癌活性和作用机理

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摘要

The mdm2 oncogene has recently been suggested to be a valuable target for cancer therapy and prevention. Overexpression of mdm2 is often seen in various human cancers and correlates with high-grade, late-stage, and more treatment-resistant tumors. The MDM2-p53 auto-regulatory loop has been extensively investigated and is an attractive cancer target, which indeed has been the main focus of anti-MDM2 drug discovery. Much effort has been expended in the development of small molecule MDM2 antagonists targeting the MDM2-p53 interaction, and a few of these have advanced into clinical trials. However, MDM2 exerts its oncogenic activity through both p53-dependent and-independent mechanisms. Recently, there is an increasing interest in identifying natural MDM2 inhibitors; some of them have been shown to decrease MDM2 expression and activity in vitro and in vivo. These identified natural MDM2 inhibitors include a plethora of diverse chemical frameworks, ranging from flavonoids, steroids, and sesquiterpenes to alkaloids. In addition to a brief review of synthetic MDM2 inhibitors, this review focuses on natural product MDM2 inhibitors, summarizing their biological activities in vitro and in vivo and the underlying molecular mechanisms of action, targeting MDM2 itself, regulators of MDM2, and/or the MDM2-p53 interaction. These MDM2 inhibitors can be used alone or in combination with conventional treatments, improving the prospects for cancer therapy and prevention. Their complex and unique molecular architectures may provide a stimulus for developing synthetic analogs in the future.
机译：最近有人提出，mdm2癌基因是癌症治疗和预防的重要靶标。 mdm2的过表达常在各种人类癌症中发现，并与高级别，晚期和更具治疗抵抗力的肿瘤有关。 MDM2-p53的自动调节回路已被广泛研究，并且是有吸引力的癌症靶标，确实是抗MDM2药物发现的主要焦点。在开发靶向MDM2-p53相互作用的小分子MDM2拮抗剂方面已经付出了很多努力，其中一些已进入临床试验。但是，MDM2通过p53依赖性和非依赖性机制发挥其致癌活性。最近，人们越来越关注鉴定天然MDM2抑制剂。已显示其中一些在体外和体内会降低MDM2的表达和活性。这些已鉴定的天然MDM2抑制剂包括多种多样的化学框架，从类黄酮，类固醇和倍半萜到生物碱。除了简要概述合成MDM2抑制剂外，本综述重点关注天然产物MDM2抑制剂，总结了它们在体外和体内的生物学活性以及潜在的分子作用机制，这些药物针对MDM2本身，MDM2和/或MDM2的调节剂。 -p53互动。这些MDM2抑制剂可单独使用或与常规治疗结合使用，从而改善癌症治疗和预防的前景。它们复杂而独特的分子结构可能会刺激未来开发合成类似物。

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