CDK6 kinase inhibition unmasks metabolic dependencies in BCR::ABL1+ leukemia.

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Tác giả: Florian Bellutti, Eszter Doma, Gerwin Heller, Thorsten Klampfl, Karoline Kollmann, Sofie Nebenfuehr, Lisa Scheiblecker, Alessia Schirripa, Veronika Sexl, Eduard Stefan, Sophie Strich, Omar Torres-Quesada, Waltraud Tschulenk, Peter Valent, Ingrid Walter, Daniela Werdenich, Sabine Zöchbauer-Müller, Markus Zojer

Ngôn ngữ: eng

Ký hiệu phân loại: 297.1248 Sources of Islam

Thông tin xuất bản: England : Cell death & disease , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 203108

Metabolic reprogramming and cell cycle deregulation are hallmarks of cancer cells. The cell cycle kinase CDK6 has recently been implicated in a wide range of hematopoietic malignancies. We here investigate the role of CDK6 in the regulation of cellular metabolism in BCR::ABL1+ leukemic cells. Our study, using gene expression data and ChIP-Seq analysis, highlights the contribution of CDK6 kinase activity in the regulation of oxidative phosphorylation. Our findings imply a competition for promoter interaction of CDK6 with the master regulator of mitochondrial respiration, NRF-1. In line, cells lacking kinase active CDK6 display altered mitochondria morphology with a defective electron transport chain. The enhanced cytoplasm/mitochondria ATP ratio paralleled by high pyruvate and lactate levels indicate a metabolic switch to glycolysis. Accordingly, combinatorial treatment of leukemic cells including imatinib resistant cells with the CDK4/6 inhibitor palbociclib and the glycolysis inhibitor 2-deoxyglucose (2-DG) enhanced apoptosis, while blocking cell proliferation in leukemic cells. These data may open a new therapeutic avenue for hematologic malignancies with high CDK6 expression by exploiting metabolic vulnerabilities unmasked by blocking CDK6 kinase activity that might even be able to overcome imatinib resistance.
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