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双皮质素样激酶 1 基因异构体的表观遗传景观及其对癌症干细胞的治疗意义。

Epigenetic Landscape and Therapeutic Implication of Gene Isoforms of Doublecortin-Like Kinase 1 for Cancer Stem Cells.

机构信息

Department of Medicine, The University of Oklahoma Health Sciences Center, Oklahoma City, OK 73104, USA.

Department of Veterans Affairs Medical Center, Oklahoma City, OK 73104, USA.

出版信息

Int J Mol Sci. 2023 Nov 16;24(22):16407. doi: 10.3390/ijms242216407.

Abstract

While significant strides have been made in understanding cancer biology, the enhancement in patient survival is limited, underscoring the urgency for innovative strategies. Epigenetic modifications characterized by hereditary shifts in gene expression without changes to the DNA sequence play a critical role in producing alternative gene isoforms. When these processes go awry, they influence cancer onset, growth, spread, and cancer stemness. In this review, we delve into the epigenetic and isoform nuances of the protein kinase, doublecortin-like kinase 1 (DCLK1). Recognized as a hallmark of tumor stemness, DCLK1 plays a pivotal role in tumorigenesis, and DCLK1 isoforms, shaped by alternative promoter usage and splicing, can reveal potential therapeutic touchpoints. Our discussion centers on recent findings pertaining to the specific functions of DCLK1 isoforms and the prevailing understanding of its epigenetic regulation via its two distinct promoters. It is noteworthy that all DCLK1 isoforms retain their kinase domain, suggesting that their unique functionalities arise from non-kinase mechanisms. Consequently, our research has pivoted to drugs that specifically influence the epigenetic generation of these DCLK1 isoforms. We posit that a combined therapeutic approach, harnessing both the epigenetic regulators of specific DCLK1 isoforms and DCLK1-targeted drugs, may prove more effective than therapies that solely target DCLK1.

摘要

尽管在理解癌症生物学方面已经取得了重大进展,但患者的生存率提高有限,这突显了创新策略的紧迫性。表观遗传修饰的特征是基因表达的遗传改变,而 DNA 序列不变,在产生替代基因异构体方面发挥着关键作用。当这些过程出现异常时,它们会影响癌症的发生、生长、扩散和癌症干细胞特性。在这篇综述中,我们深入探讨了蛋白激酶、双皮质激酶 1(DCLK1)的表观遗传和异构体细微差别。DCLK1 被认为是肿瘤干细胞的标志,它在肿瘤发生中起着关键作用,并且通过不同的启动子使用和剪接形成的 DCLK1 异构体可以揭示潜在的治疗靶点。我们的讨论集中在最近关于 DCLK1 异构体的特定功能的发现,以及通过其两个不同的启动子对其表观遗传调控的现有理解。值得注意的是,所有 DCLK1 异构体都保留其激酶结构域,这表明它们独特的功能是由非激酶机制产生的。因此,我们的研究已经转向专门影响这些 DCLK1 异构体表观遗传生成的药物。我们假设,结合使用特定的 DCLK1 异构体的表观遗传调节剂和 DCLK1 靶向药物的治疗方法可能比仅靶向 DCLK1 的治疗方法更有效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5826/10671580/18cfc9fee726/ijms-24-16407-g001.jpg

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