天然热休克蛋白90抑制剂可治疗癌症和炎症。,European Journal of Medicinal Chemistry

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天然热休克蛋白90抑制剂可治疗癌症和炎症。
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-01-11 , DOI: 10.1016/j.ejmech.2020.112063
Thadeu E M M Costa ₁ , Nulgumnalli Manjunathaiah Raghavendra ₂ , Carmen Penido ₁

Affiliation

热休克蛋白（HSP）90是最丰富的HSP，它们是分子伴侣分子，其主要作用是通过协助多种蛋白的折叠，稳定和重塑来保护和维持细胞。数百种蛋白质依赖于HSP90伴侣的活性，包括在癌症和炎症中起重要作用的激酶和转录因子，因此以HSP90为靶点的疗法已被认为是治疗癌症和炎症相关疾病的潜在策略。在不同类型的癌症和炎症的临床前研究和临床试验中，天然，半合成和合成化合物对HSP90的抑制作用已产生令人鼓舞的结果。天然产物是广泛用于药物开发的生物活性化合物的巨大来源，这是由于其代谢产物的多样性能够调节多种蛋白质功能。HSP90抑制剂已从细菌，真菌和植物种类中分离出来。这些天然化合物具有调节HSP90活性的显着能力，并可用作开发新型合成或半合成抑制剂的支架。一百多项临床试验评估了HSP90抑制剂作为针对不同类型肿瘤的辅助治疗的效果，目前，正在开展新的研究以寻求新颖的，更有前景的，更有效的癌症治疗方法。在这篇综述中，我们介绍了天然存在的HSP90抑制剂和类似物，

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Natural heat shock protein 90 inhibitors in cancer and inflammation.

Heat shock protein (HSP)90 is the most abundant HSPs, which are chaperone molecules whose major roles are cell protection and maintenance by means of aiding the folding, the stabilization and the remodeling of a wide range of proteins. A few hundreds of proteins depend on HSP90 chaperone activity, including kinases and transcriptional factors that play essential roles in cancer and inflammation, so that HSP90-targeted therapies have been considered as a potential strategy for the treatment of cancer and inflammatory-associated diseases. HSP90 inhibition by natural, semi-synthetic and synthetic compounds have yield promising results in pre-clinical studies and clinical trials for different types of cancers and inflammation. Natural products are a huge source of biologically active compounds widely used in drug development due to the great diversity of their metabolites which are capable to modulate several protein functions. HSP90 inhibitors have been isolated from bacteria, fungi and vegetal species. These natural compounds have a noteworthy ability to modulate HSP90 activity as well as serve as scaffolds for the development of novel synthetic or semi-synthetic inhibitors. Over a hundred clinical trials have evaluated the effect of HSP90 inhibitors as adjuvant treatment against different types of tumors and, currently, new studies are being developed to gain sight on novel promising and more effective approaches for cancer treatment. In this review, we present the naturally occurring HSP90 inhibitors and analogues, discussing their anti-cancer and anti-inflammatory effects.

更新日期：2020-01-13

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