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非激酶靶向致癌性 c-Jun N-末端激酶 (JNK) 信号转导:具有临床应用潜力的癌症治疗方法的未来。

Non-kinase targeting of oncogenic c-Jun N-terminal kinase (JNK) signaling: the future of clinically viable cancer treatments.

机构信息

The Kinghorn Cancer Centre, Garvan Institute of Medical Research, Sydney, Australia.

St Vincent's Hospital Clinical School, UNSW, Sydney, Australia.

出版信息

Biochem Soc Trans. 2022 Dec 16;50(6):1823-1836. doi: 10.1042/BST20220808.

Abstract

c-Jun N-terminal Kinases (JNKs) have been identified as key disease drivers in a number of pathophysiological settings and central oncogenic signaling nodes in various cancers. Their roles in driving primary tumor growth, positively regulating cancer stem cell populations, promoting invasion and facilitating metastatic outgrowth have led JNKs to be considered attractive targets for anti-cancer therapies. However, the homeostatic, apoptotic and tumor-suppressive activities of JNK proteins limit the use of direct JNK inhibitors in a clinical setting. In this review, we will provide an overview of the different JNK targeting strategies developed to date, which include various ATP-competitive, non-kinase and substrate-competitive inhibitors. We aim to summarize their distinct mechanisms of action, review some of the insights they have provided regarding JNK-targeting in cancer, and outline the limitations as well as challenges of all strategies that target JNKs directly. Furthermore, we will highlight alternate drug targets within JNK signaling complexes, including recently identified scaffold proteins, and discuss how these findings may open up novel therapeutic options for targeting discrete oncogenic JNK signaling complexes in specific cancer settings.

摘要

c-Jun N-末端激酶(JNKs)已被确定为许多生理病理环境中的关键疾病驱动因素,也是多种癌症中重要的致癌信号节点。它们在驱动原发性肿瘤生长、正向调节癌症干细胞群体、促进侵袭以及促进转移生长中的作用,使得 JNK 成为癌症治疗的有吸引力的靶点。然而,JNK 蛋白的稳态、凋亡和肿瘤抑制活性限制了直接 JNK 抑制剂在临床环境中的应用。在这篇综述中,我们将概述迄今为止开发的不同 JNK 靶向策略,包括各种 ATP 竞争性、非激酶和底物竞争性抑制剂。我们旨在总结它们不同的作用机制,回顾它们在癌症中针对 JNK 靶向治疗提供的一些见解,并概述所有直接靶向 JNK 的策略的局限性和挑战。此外,我们将突出 JNK 信号复合物中的其他药物靶点,包括最近发现的支架蛋白,并讨论这些发现如何为针对特定癌症环境中特定致癌 JNK 信号复合物开辟新的治疗选择。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/325d/9788565/4709b1b20d0f/BST-50-1823-g0001.jpg

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