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Fyn, Blk, and Lyn kinase inhibitors: A mini-review on medicinal attributes, research progress, and future insights
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2024-02-24 , DOI: 10.1016/j.bmcl.2024.129674
Rupali Kohal , Bhavana , Preety Kumari , Arun Kumar Sharma , Ghanshyam Das Gupta , Sant Kumar Verma

Fyn, Blk, and Lyn are part of a group of proteins called Src family kinases. They are crucial in controlling cell communication and their response to the growth, changes, and immune system. Blocking these proteins with inhibitors can be a way to treat diseases where these proteins are too active. The primary mode of action of these inhibitors is to inhibit the phosphorylation of Fyn, Blk, and Lyn receptors, which in turn affects how signals pass within the cells. This review shows the structural and functional aspects of Fyn, Blk, and Lyn kinases, highlighting the significance of their dysregulation in diseases such as cancer and autoimmune disorders. The discussion encompasses the design strategies, SAR analysis, and chemical characteristics of effective inhibitors, shedding light on their specificity and potency. Furthermore, it explores the progress of clinical trials of these inhibitors, emphasizing their potential therapeutic applications.

中文翻译:

Fyn、Blk 和 Lyn 激酶抑制剂:医学属性、研究进展和未来见解的小型回顾

Fyn、Blk 和 Lyn 是一组称为 Src 家族激酶的蛋白质的一部分。它们对于控制细胞通讯及其对生长、变化和免疫系统的反应至关重要。用抑制剂阻断这些蛋白质可能是治疗这些蛋白质过于活跃的疾病的一种方法。这些抑制剂的主要作用方式是抑制 Fyn、Blk 和 Lyn 受体的磷酸化,从而影响信号在细胞内传递的方式。这篇综述展示了 Fyn、Blk 和 Lyn 激酶的结构和功能方面,强调了它们的失调在癌症和自身免疫性疾病等疾病中的重要性。讨论内容包括有效抑制剂的设计策略、SAR 分析和化学特性,阐明其特异性和效力。此外,它还探讨了这些抑制剂的临床试验进展,强调了它们潜在的治疗应用。
更新日期:2024-02-24
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