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Updated: Aug 12, 2025

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Exploring the chemotherapeutic potential of currently used kinase inhibitors: An update
Rajashri R Naik1, Ashok K Shakya2
1Faculty of Allied Medical Sciences, Pharmacological and Diagnostic Research Center, Al-Ahliyya Amman University, Amman, Jordan.
Abstract:
Protein kinases are enzymes that transfer phosphate to protein, resulting in the modification of the protein. The human genome encodes approximately 538 kinases. Kinases play a role in maintaining a number of cellular processes, including control of the cell cycle, metabolism, survival, and differentiation. Protein kinase dysregulation causes several diseases, and it has been shown that numerous kinases are deregulated in cancer. The oncogenic potential of these kinases is increased by a number of processes, including overexpression, relocation, fusion point mutations, and the disruption of upstream signaling. Understanding of the mechanism or role played by kinases has led to the development of a large number of kinase inhibitors with promising clinical benefits. In this review, we discuss FDA-approved kinase inhibitors and their mechanism, clinical benefits, and side effects, as well as the challenges of overcoming some of their side effects and future prospects for new kinase inhibitor discovery.
Insights
Protein kinases regulate cell functions, but their dysregulation drives cancer. This review details FDA-approved kinase inhibitors, their benefits, side effects, and future directions in cancer therapy.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Protein kinases are crucial enzymes regulating cellular processes like cell cycle and metabolism.
- Dysregulation of protein kinases, through mechanisms like overexpression or mutations, is implicated in various diseases, particularly cancer.
- The human genome encodes approximately 538 kinases, highlighting their widespread importance.
Purpose of the Study:
- To review FDA-approved kinase inhibitors.
- To discuss their mechanisms of action, clinical benefits, and associated side effects.
- To explore challenges in managing side effects and future prospects for novel kinase inhibitor development.
Main Methods:
- Literature review of FDA-approved kinase inhibitors.
- Analysis of mechanisms, clinical efficacy, and adverse events.
- Discussion of therapeutic challenges and future research directions.
Main Results:
- Kinase inhibitors have shown significant clinical benefits in treating various cancers.
- Understanding kinase function has enabled targeted therapeutic strategies.
- Side effects associated with kinase inhibitors present challenges that require management.
Conclusions:
- Kinase inhibitors represent a vital class of targeted cancer therapies.
- Continued research is essential to overcome treatment-related toxicities and discover next-generation inhibitors.
- Future efforts will focus on improving efficacy and patient outcomes through advanced kinase inhibitor design.
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