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Updated: Jul 26, 2025

Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay
Published on: May 3, 2018
Targeting CDK1 in cancer: mechanisms and implications
Qiushi Wang1, Ann M Bode2, Tianshun Zhang3
1The Hormel Institute, University of Minnesota, 801 16th Ave NE, Austin, MN, 55912, USA.
Abstract:
Cyclin dependent kinases (CDKs) are serine/threonine kinases that are proposed as promising candidate targets for cancer treatment. These proteins complexed with cyclins play a critical role in cell cycle progression. Most CDKs demonstrate substantially higher expression in cancer tissues compared with normal tissues and, according to the TCGA database, correlate with survival rate in multiple cancer types. Deregulation of CDK1 has been shown to be closely associated with tumorigenesis. CDK1 activation plays a critical role in a wide range of cancer types; and CDK1 phosphorylation of its many substrates greatly influences their function in tumorigenesis. Enrichment of CDK1 interacting proteins with Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis was conducted to demonstrate that the associated proteins participate in multiple oncogenic pathways. This abundance of evidence clearly supports CDK1 as a promising target for cancer therapy. A number of small molecules targeting CDK1 or multiple CDKs have been developed and evaluated in preclinical studies. Notably, some of these small molecules have also been subjected to human clinical trials. This review evaluates the mechanisms and implications of targeting CDK1 in tumorigenesis and cancer therapy.
Insights
Cyclin dependent kinases (CDKs), particularly CDK1, are crucial for cell cycle progression and are highly expressed in cancers, indicating their potential as therapeutic targets. Targeting CDK1 shows promise for effective cancer treatment strategies.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Cyclin-dependent kinases (CDKs) are key regulators of the cell cycle.
- CDKs, especially CDK1, are frequently overexpressed in various cancer types.
- Elevated CDK expression often correlates with poorer patient survival rates.
Purpose of the Study:
- To review the role of CDK1 in tumorigenesis.
- To evaluate CDK1 as a therapeutic target for cancer.
- To discuss small molecules targeting CDK1 in preclinical and clinical studies.
Main Methods:
- Literature review of CDK1 function in cancer.
- Analysis of CDK1 expression data and its correlation with survival.
- KEGG pathway analysis of CDK1 interacting proteins.
- Evaluation of preclinical and clinical data for CDK1 inhibitors.
Main Results:
- CDK1 deregulation is closely linked to cancer development.
- CDK1 substrates and interacting proteins are involved in multiple oncogenic pathways.
- Numerous small molecules targeting CDK1 have shown promise in preclinical and clinical settings.
Conclusions:
- CDK1 is a validated and promising target for cancer therapy.
- Targeting CDK1 offers a viable strategy for developing novel cancer treatments.
- Further investigation into CDK1-targeting agents is warranted for clinical application.
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