ABL1酪氨酸激酶的结构和动力学及其在慢性髓性白血病中的重要作用

IF 3.6 3区 医学 Q2 CHEMISTRY, MEDICINAL
Ayca Irgit, Reyhan Kamıs, Belgin Sever, Amaç Fatih Tuyun, Masami Otsuka, Mikako Fujita, Hasan Demirci, Halilibrahim Ciftci
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引用次数: 0

摘要

Abelson (ABL1)酪氨酸激酶是非受体酪氨酸激酶的重要组成部分,与许多细胞过程有关,包括分化和增殖。ABL1的结构特征包括一个独特的n端帽区,一个c端尾,一个双叶激酶,SH2和SH3结构域。这些域使其能够参与多个信号级联和动态控制。慢性髓性白血病(CML)的病理生理主要由BCR-ABL1癌蛋白驱动,由ABL1激酶的失调引起,即通过其与断点簇区(BCR)基因的融合。ABL1是治疗CML的关键靶点,因为BCR-ABL1融合会导致不受控制的细胞增殖和细胞凋亡抵抗。靶向ABL1酪氨酸激酶的酪氨酸激酶抑制剂(TKIs)通过抑制BCR-ABL1融合蛋白介导的持续激活的信号通路,在CML的治疗中发挥着关键作用。本文研究了ABL1的结构特征,它们与CML的关系,以及ABL1与目前fda批准的TKIs之间的相互作用,强调了该激酶在癌变中的关键功能及其酪氨酸激酶抑制剂的可能靶标状态。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Structure and Dynamics of the ABL1 Tyrosine Kinase and Its Important Role in Chronic Myeloid Leukemia

Structure and Dynamics of the ABL1 Tyrosine Kinase and Its Important Role in Chronic Myeloid Leukemia

Abelson (ABL1) tyrosine kinase is an essential component of non-receptor tyrosine kinases and is associated with numerous cellular processes, including differentiation and proliferation. The structural features of ABL1 include a distinct N-terminal cap region, a C-terminal tail, a bilobed kinase, SH2, and SH3 domains. These domains enable its engagement in several signaling cascades and dynamic control. The pathophysiology of chronic myeloid leukemia (CML) is mainly driven by the BCR-ABL1 oncoprotein, arising from dysregulation of ABL1 kinase, namely through its fusion to the breakpoint cluster region (BCR) gene. ABL1 is a crucial target in the treatment of CML as the BCR-ABL1 fusion causes uncontrolled cellular proliferation and resistance to apoptosis. Tyrosine kinase inhibitors (TKIs) targeting the ABL1 tyrosine kinase are playing a critical role in the treatment of CML through the inhibition of persistently activated signaling pathways mediated by the BCR-ABL1 fusion protein. The article examines the structural characteristics of ABL1, how they relate to CML, and the interactions between ABL1 and the current FDA-approved TKIs, emphasizing the kinase's critical function in carcinogenesis and its possible target status for tyrosine kinase inhibitors.

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来源期刊
Archiv der Pharmazie
Archiv der Pharmazie 医学-化学综合
CiteScore
7.90
自引率
5.90%
发文量
176
审稿时长
3.0 months
期刊介绍: Archiv der Pharmazie - Chemistry in Life Sciences is an international journal devoted to research and development in all fields of pharmaceutical and medicinal chemistry. Emphasis is put on papers combining synthetic organic chemistry, structural biology, molecular modelling, bioorganic chemistry, natural products chemistry, biochemistry or analytical methods with pharmaceutical or medicinal aspects such as biological activity. The focus of this journal is put on original research papers, but other scientifically valuable contributions (e.g. reviews, minireviews, highlights, symposia contributions, discussions, and essays) are also welcome.
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