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天然 STAT3 抑制剂:一个小视角。

Natural STAT3 inhibitors: A mini perspective.

机构信息

Southern University of Science and Technology, School of Medicine, Shenzhen 518055, People's Republic of China.

Division of Life Science, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China.

出版信息

Bioorg Chem. 2021 Oct;115:105169. doi: 10.1016/j.bioorg.2021.105169. Epub 2021 Jul 16.

Abstract

Signal transducer and activator of transcription 3 (STAT3) plays pivotal role in several cellular processes such as cell proliferation and survival and has been found to be aberrantly activated in many cancers. STAT3 is largely believed to be one of the key oncogenes and crucial therapeutic targets. Much research has suggested the leading mechanisms for regulating the STAT3 pathway and its role in promoting tumorigenesis. Therefore, intensive efforts have been devoted to develop potent STAT3 inhibitors and several of them are currently undergoing clinical trials. Nevertheless, many natural products were identified as STAT3 inhibitors but attract less attention compared to the small molecule counterpart. In this review, the development of natural STAT3 inhibitors with an emphasis on their biological profile and chemical synthesis are detailed. The current state of STAT3 inhibitors and the future directions and opportunities for STAT3 inhibitor are discussed.

摘要

信号转导子和转录激活因子 3(STAT3)在细胞增殖和存活等多种细胞过程中发挥关键作用,并且已在许多癌症中发现异常激活。STAT3 被广泛认为是关键致癌基因之一和关键治疗靶点。大量研究表明,调节 STAT3 途径的主要机制及其在促进肿瘤发生中的作用。因此,人们致力于开发有效的 STAT3 抑制剂,其中几种抑制剂目前正在进行临床试验。然而,许多天然产物被鉴定为 STAT3 抑制剂,但与小分子对应物相比,它们的关注度较低。在这篇综述中,详细介绍了天然 STAT3 抑制剂的开发,重点介绍了它们的生物学特性和化学合成。讨论了 STAT3 抑制剂的现状以及 STAT3 抑制剂的未来方向和机会。

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