The CDK inhibitors in cancer research and therapy
Jonas Cicenas1, Mindaugas Valius
1Department of Medicine, Institute of Anatomy, University of Fribourg, Rte. Albert- Gockel 1, 1700, Fribourg, Switzerland. j.cicenas@mapkinases.eu
Abstract:
Chemical compounds that interfere with an enzymatic function of kinases are useful for gaining insight into the complicated biochemical processes in mammalian cells. Cyclin-dependent kinases (CDK) play an essential role in the control of the cell cycle and/or proliferation. These kinases as well as their regulators are frequently deregulated in different human tumors. Aberrations in CDK activity have also been observed in viral infections, Alzheimer's, Parkinson's diseases, ischemia and some proliferative disorders. This led to an intensive search for small-molecule CDK inhibitors not only for research purposes, but also for therapeutic applications. Here, we discuss seventeen CDK inhibitors and their use in cancer research or therapy. This review should help researchers to decide which inhibitor is best suited for the specific purpose of their research. For this purpose, the targets, commercial availability and IC(50) values are provided for each inhibitor. The review will also provide an overview of the clinical studies performed with some of these inhibitors.
Insights
This review discusses seventeen small-molecule cyclin-dependent kinase (CDK) inhibitors, detailing their targets, availability, and efficacy. It aids researchers in selecting appropriate CDK inhibitors for cancer research and therapeutic applications.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Kinase inhibitors are crucial tools for understanding mammalian cell biochemical processes.
- Cyclin-dependent kinases (CDKs) regulate cell cycle and proliferation, with deregulation implicated in human tumors and various diseases.
Purpose of the Study:
- To review seventeen small-molecule CDK inhibitors for their utility in cancer research and therapy.
- To guide researchers in selecting the most suitable CDK inhibitor for their specific research needs.
Main Methods:
- Compilation and discussion of seventeen CDK inhibitors.
- Inclusion of inhibitor targets, commercial availability, and IC(50) values.
- Overview of clinical studies involving selected CDK inhibitors.
Main Results:
- Detailed information on seventeen CDK inhibitors is presented.
- Data on targets, IC(50) values, and commercial availability are provided for each inhibitor.
- Clinical study data for some inhibitors are summarized.
Conclusions:
- The review provides a comprehensive resource for researchers investigating CDK inhibitors.
- Informed selection of CDK inhibitors is facilitated for both research and therapeutic development.
- Understanding inhibitor profiles aids in advancing cancer research and treatment strategies.
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