CDK8/19 inhibition attenuates G1 arrest induced by BCR-ABL antagonists and accelerates death of chronic myelogenous leukemia cells.

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Tác giả: Iaroslav E Abramenko, Eugenia V Broude, Alexandra V Bruter, Mengqian Chen, Ekaterina S Ivanova, Alvina I Khamidullina, Anastasia M Khrustaleva, Jing Li, Chang-Uk Lim, Julia V Nuzhina, Igor B Roninson, Alexander A Shtil, Victor V Tatarskiy, Alexander V Tyakht, Ekaterina A Varlamova, Nadezhda E Vorobyeva, Margarita A Yastrebova, Maria A Zamkova

Ngôn ngữ: eng

Ký hiệu phân loại: 616.99419 Other diseases

Thông tin xuất bản: United States : Cell death discovery , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 142746

Imatinib mesylate (IM) and other BCR-ABL tyrosine kinase inhibitors (BCR-ABLi) are the mainstay of chronic myelogenous leukemia (CML) treatment. However, activation of circumventing signaling pathways and quiescence may limit BCR-ABLi efficacy. CDK8/19 Mediator kinases have been implicated in the emergence of non-genetic drug resistance. Dissecting the effects of pharmacological CDK8/19 inhibition on CML survival in response to BCR-ABLi, we found that a selective, non-toxic CDK8/19 inhibitor (CDK8/19i) Senexin B (SenB) and other CDK8/19i sensitized K562 cells to different BCR-ABLi via attenuation of cell cycle arrest. In particular, SenB prevented IM-induced upregulation of genes that negatively regulate cell cycle progression. SenB also antagonized IM-activated p27
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