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Updated: Jun 22, 2026

Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay
Published on: May 3, 2018
Cell cycle kinases as therapeutic targets for cancer
Silvia Lapenna1, Antonio Giordano
1Oncology Research Centre of Mercogliano, Mercogliano, Avellino, Italy. slapenna@gmail.com
Abstract:
Several families of protein kinases orchestrate the complex events that drive the cell cycle, and their activity is frequently deregulated in hyperproliferative cancer cells. Although several molecules that inhibit cell cycle kinases have been developed and clinically screened as potential anticancer agents, none of these has been approved for commercial use and an effective strategy to specifically control malignant cell proliferation has yet to be established. However, recent genetic and biochemical studies have provided information about the requirement for certain cell cycle kinases by specific tumours and specialized tissue types. Here, we discuss the potential and limitations of established cell cycle kinases as targets in anticancer drug discovery as well as novel strategies for the design of new agents.
Insights
Protein kinases regulate cell division, but their targeting for cancer therapy remains challenging. New strategies are needed to effectively control cancer cell proliferation by targeting specific kinases.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Protein kinases are crucial regulators of the cell cycle.
- Deregulation of cell cycle kinases is common in hyperproliferative cancers.
- Current kinase inhibitors have not yet achieved clinical approval for cancer treatment.
Purpose of the Study:
- To review established cell cycle kinases as targets for anticancer drug discovery.
- To discuss the potential and limitations of targeting these kinases.
- To explore novel strategies for designing new anticancer agents.
Main Methods:
- Literature review of genetic and biochemical studies.
- Analysis of established cell cycle kinases as drug targets.
- Discussion of novel therapeutic strategies.
Main Results:
- Several protein kinase families regulate cell cycle progression.
- Kinase activity is frequently dysregulated in cancer cells.
- No cell cycle kinase inhibitors have been approved for clinical use.
Conclusions:
- Targeting cell cycle kinases holds promise for cancer therapy.
- Understanding tumor-specific kinase requirements is crucial.
- Novel strategies are essential for effective anticancer drug development.
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