摘要
有丝分裂激酶在负责所有肿瘤类型的癌症发展和进展的细胞过程中具有不可或缺的作用,并且是治疗的常见靶点。然而,人类激酶组的很大一部分在癌症系统的功能方面仍未得到探索。在有丝分裂激酶中,永不进入有丝分裂激酶 (NEK) 家族正在成为各种癌症类型中的新型激酶靶标。 NEK5 是 NEK 家族中一个未被充分研究的成员。虽然最近有更多研究描述了 NEK5 的生理功能,但其在癌症生物学中的作用仍未得到广泛研究。然而,新兴研究表明 NEK5 在各种实体瘤中具有潜在的关键功能。在这篇综述中,我们讨论了关于 NEK5 在癌症中的作用以及 NEK5 表达和活性在肿瘤发展和转移中的影响的当前知识。我们总结了当前检查 NEK5 在不同癌症系统和细胞过程中的活性的研究。作为一种研究不足的激酶,目前没有选择性 NEK5 靶向剂来测试药物抑制对癌症的影响,尽管该领域最近取得了进展。在这里,我们还介绍了开发 NEK5 选择性药理学抑制的最新进展,并讨论了 NEK5 靶向治疗开发的当前方向。选择性 NEK5 抑制剂的产生有望用于癌症生长和转移的新靶向疗法。
关键词: Never-in-有丝分裂激酶家族、有丝分裂、NEK5、治疗靶点、乳腺癌、转移。
Current Medicinal Chemistry
Title:Targeting Never-In-Mitosis-A Related Kinase 5 in Cancer: A Review
Volume: 28 Issue: 30
关键词: Never-in-有丝分裂激酶家族、有丝分裂、NEK5、治疗靶点、乳腺癌、转移。
摘要: Mitotic kinases have integral roles in cell processes responsible for cancer development and progression in all tumor types and are common targets for therapeutics. However, a large subset of the human kinome remains unexplored with respect to functionality in cancer systems. Within the mitotic kinases, the never-in-mitosis kinase (NEK) family is emerging as novel kinase targets in various cancer types. NEK5 is an understudied member of the NEK family. While there are more recent studies describing the physiologic function of NEK5, its role in cancer biology remains widely understudied. However, emerging studies implicate that NEK5 has potentially crucial functions in various solid tumors. In this review, we discuss current knowledge regarding the role of NEK5 in cancer and the implications of NEK5 expression and activity in tumor development and metastasis. We summarize current studies that examine NEK5 activity in diverse cancer systems and cellular processes. As an understudied kinase, there are currently no selective NEK5-targeting agents to test the effects of pharmacologic inhibition on cancer, although there exist recent advancements in this area. Here we also include an update on efforts to develop selective pharmacologic inhibition of NEK5, and we discuss the current direction of NEK5-targeting therapeutic development. The generation of selective NEK5 inhibitors is promising new targeted therapies for cancer growth and metastasis.
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Targeting Never-In-Mitosis-A Related Kinase 5 in Cancer: A Review, Current Medicinal Chemistry 2021; 28 (30) . https://dx.doi.org/10.2174/0929867328666210322101749
DOI https://dx.doi.org/10.2174/0929867328666210322101749 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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