Comprehensive Insights that Targeting PIM for Cancer Therapy: Prospects and Obstacles,Journal of Medicinal Chemistry

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Comprehensive Insights that Targeting PIM for Cancer Therapy: Prospects and Obstacles
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2024-01-02 , DOI: 10.1021/acs.jmedchem.3c01802
Li Chen _{1,

2,

3} , Wuyu Mao ₁ , Changyu Ren ₄ , Jinqi Li _{2,

3} , Jifa Zhang ₁

Affiliation

Proviral integration sitea for Moloney-murine leukemia virus (PIM) kinases are a family of highly conserved serine/tyrosine kinases consisting of three members, PIM-1, PIM-2, and PIM-3. These kinases regulate a wide range of substrates through phosphorylation and affect key cellular processes such as transcription, translation, proliferation, apoptosis, and energy metabolism. Several PIM inhibitors are currently undergoing clinical trials, such as a phase I clinical trial of Uzanserti (5) for the treatment of relapsed diffuse large B-cell lymphoma that has been completed. The current focus encompasses the structural and biological characterization of PIM, ongoing research progress on small-molecule inhibitors undergoing clinical trials, and evaluation analysis of persisting challenges in this field. Additionally, the design and discovery of small-molecule inhibitors targeting PIM in recent years have been explored, with a particular emphasis on medicinal chemistry, aiming to provide valuable insights for the future development of PIM inhibitors.

中文翻译：

针对 PIM 癌症治疗的综合见解：前景和障碍

莫洛尼鼠白血病病毒 (PIM) 激酶的前病毒整合位点是高度保守的丝氨酸/酪氨酸激酶家族，由三个成员组成：PIM-1、PIM-2 和 PIM-3。这些激酶通过磷酸化调节多种底物，并影响转录、翻译、增殖、细胞凋亡和能量代谢等关键细胞过程。目前有几种PIM抑制剂正在进行临床试验，例如Uzanserti （ 5 ）治疗复发性弥漫性大B细胞淋巴瘤的I期临床试验已经完成。目前的重点包括PIM的结构和生物学表征、正在进行临床试验的小分子抑制剂的研究进展以及该领域持续挑战的评估分析。此外，近年来针对PIM的小分子抑制剂的设计和发现也得到了探索，特别是药物化学，旨在为PIM抑制剂的未来发展提供有价值的见解。

更新日期：2024-01-02

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