当前位置: X-MOL 学术J. Enzyme Inhib. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
New horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011–2021) focussing on structure–activity relationship (SAR) and docking insights
Journal of Enzyme inhibition and Medicinal Chemistry ( IF 5.6 ) Pub Date : 2021-07-07 , DOI: 10.1080/14756366.2021.1937143
Ahmed Elkamhawy 1, 2 , Eslam M H Ali 3, 4, 5 , Kyeong Lee 1
Affiliation  

Abstract

Lymphocyte-specific protein tyrosine kinase (Lck), a non-receptor Src family kinase, has a vital role in various cellular processes such as cell cycle control, cell adhesion, motility, proliferation, and differentiation. Lck is reported as a key factor regulating the functions of T-cell including the initiation of TCR signalling, T-cell development, in addition to T-cell homeostasis. Alteration in expression and activity of Lck results in numerous disorders such as cancer, asthma, diabetes, rheumatoid arthritis, atherosclerosis, and neuronal diseases. Accordingly, Lck has emerged as a novel target against different diseases. Herein, we amass the research efforts in literature and pharmaceutical patents during the last decade to develop new Lck inhibitors. Additionally, structure-activity relationship studies (SAR) and docking models of these new inhibitors within the active site of Lck were demonstrated offering deep insights into their different binding modes in a step towards the identification of more potent, selective, and safe Lck inhibitors.



中文翻译:

淋巴细胞特异性蛋白酪氨酸激酶 (Lck) 抑制剂药物发现的新视野:十年回顾 (2011-2021) 侧重于结构活性关系 (SAR) 和对接见解

摘要

淋巴细胞特异性蛋白酪氨酸激酶 (Lck) 是一种非受体 Src 家族激酶,在细胞周期控制、细胞粘附、运动、增殖和分化等各种细胞过程中起着至关重要的作用。据报道,Lck 是调节 T 细胞功能的关键因素,包括 TCR 信号传导的启动、T 细胞发育以及 T 细胞稳态。Lck 表达和活性的改变导致多种疾病,例如癌症、哮喘、糖尿病、类风湿性关节炎、动脉粥样硬化和神经元疾病。因此,Lck 已成为针对不同疾病的新靶点。在此,我们在过去十年中积累了文献和药物专利的研究成果,以开发新的 Lck 抑制剂。此外,

更新日期:2021-07-08
down
wechat
bug