4.8 Review

DNA-PKcs: A Targetable Protumorigenic Protein Kinase

Journal

CANCER RESEARCH
Volume 82, Issue 4, Pages 523-533

Publisher

AMER ASSOC CANCER RESEARCH
DOI: 10.1158/0008-5472.CAN-21-1756

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Funding

  1. NIH/NCI [5R01CA17640105, 5R01CA18256905]

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DNA-PKcs is a crucial protein kinase involved in cancer development and progression, with its deregulation frequently associated with poor outcomes in various types of tumors. Therapeutic targeting of DNA-PKcs is currently being tested in preclinical and clinical settings for cancer therapy.
DNA-dependent protein kinase catalytic subunit (DNA-PKcs) is a pleiotropic protein kinase that plays critical roles in cellular processes fundamental to cancer. DNA-PKcs expression and activity are frequently deregulated in multiple hematologic and solid tumors and have been tightly linked to poor outcome. Given the potentially influential role of DNA-PKcs in cancer develop-ment and progression, therapeutic targeting of this kinase is being tested in preclinical and clinical settings. This review summarizes the latest advances in the field, providing a com-prehensive discussion of DNA-PKcs functions in cancer and an update on the clinical assessment of DNA-PK inhibitors in cancer therapy.

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