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Published on: February 21, 2019
Protein kinases: Role of their dysregulation in carcinogenesis, identification and inhibition
Niloy Sarkar1,2, Amit Singh1,3, Pankaj Kumar1,3
1Nano-Bioconjugate Chemistry Lab, Cluster Innovation Centre, University of Delhi, Delhi, India.
Abstract:
Protein kinases belong to the phosphor-transferases superfamily of enzymes, which "activate" enzymes via phosphorylation. The kinome of an organism is the total set of genes in the genome, which encode for all the protein kinases. Certain mutations in the kinome have been linked to dysregulation of protein kinases, which in turn can lead to several diseases and disorders including cancer. In this review, we have briefly discussed the role of protein kinases in various biochemical processes by categorizing cancer associated phenotypes and giving their protein kinase examples. Various techniques have also been discussed, which are being used to analyze the structure of protein kinases, and associate their roles in the oncogenesis. We have also discussed protein kinase inhibitors and United States Federal Drug Administration (USFDA) approved drugs, which target protein kinases and can serve as a counter to protein kinase dysregulation and mitigate the effects of oncogenesis. Overall, this review briefs about the importance of protein kinases, their roles in oncogenesis on dysregulation and how their inhibition via various drugs can be used to mitigate their effects.
Insights
Protein kinases regulate cell functions via phosphorylation. Dysregulation of these kinases is linked to cancer, but inhibitors offer therapeutic potential.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Protein kinases, part of the phosphor-transferases superfamily, regulate cellular processes through phosphorylation.
- The kinome, encompassing all protein kinase genes, is crucial for cellular function.
- Mutations in the kinome can lead to protein kinase dysregulation, contributing to diseases like cancer.
Approach:
- This review categorizes cancer-associated phenotypes and provides protein kinase examples.
- It discusses techniques for analyzing protein kinase structure and their role in oncogenesis.
- The review examines protein kinase inhibitors and FDA-approved drugs for cancer therapy.
Key Points:
- Protein kinases play vital roles in numerous biochemical pathways.
- Dysregulation of protein kinases is a significant factor in oncogenesis.
- Targeting protein kinases with inhibitors is a key strategy in cancer treatment.
Conclusions:
- Understanding protein kinase function and dysregulation is essential for cancer research.
- Protein kinase inhibitors represent a promising therapeutic avenue for mitigating oncogenesis.
- This review highlights the importance of protein kinases and their therapeutic targeting.
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