Related Experiment Video
Updated: Feb 4, 2026
Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
A comprehensive review of protein kinase inhibitors for cancer therapy
Radhamani Kannaiyan1, Daruka Mahadevan2
1a Department of Internal Medicine , University of Arizona College of Medicine at South Campus , Tucson , AZ , USA.
Introduction:
Protein kinases are involved in various cellular functions. About 2% of the human genome encodes for protein kinases. Dysregulation of protein kinases is implicated in various processes of carcinogenesis. The advent of protein kinase inhibitors in cancer therapy has led to a paradigm shift in cancer therapy. Several protein kinase inhibitors have been approved by FDA in the last few decades. Areas covered: This article provides a review of the FDA approved protein kinase inhibitors as of December 2017 for the well-known oncogenic protein kinases. A list of FDA approved protein kinase inhibitors and their FDA approved clinical indications were cataloged. The role of the respective oncogenic protein kinases in carcinogenesis and cancer progression and the relevant landmark clinical trials of respective protein kinase inhibitors leading up to the FDA approval were PubMed searched and discussed. Expert commentary: Further understanding of the molecular origin of various cancers would help identify new targets. Use of biomarker profiling might select the patient population that would benefit better from kinase inhibitors. Clinical trials should be designed to identify the appropriate sequence of the available kinase inhibitors. It would prove to be useful to test these drugs in the adjuvant setting.
Insights
This review covers FDA-approved protein kinase inhibitors for oncogenic kinases as of December 2017. It details their clinical indications, roles in cancer, and landmark trials, offering insights for future cancer therapy.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Protein kinases regulate cellular functions, and their dysregulation is linked to carcinogenesis.
- Approximately 2% of the human genome encodes protein kinases.
- Protein kinase inhibitors represent a significant advancement in cancer therapy.
Purpose of the Study:
- To review FDA-approved protein kinase inhibitors targeting well-known oncogenic kinases as of December 2017.
- To catalog approved inhibitors and their clinical indications.
- To discuss the role of these kinases in cancer and landmark clinical trials.
Main Methods:
- PubMed search for relevant clinical trials and FDA-approved protein kinase inhibitors.
- Cataloging of approved inhibitors and their indications.
- Review of literature on oncogenic protein kinases and their inhibitors.
Main Results:
- A comprehensive list of FDA-approved protein kinase inhibitors and their clinical indications up to December 2017.
- Discussion of the role of specific oncogenic kinases in cancer progression.
- Summary of landmark clinical trials that led to drug approvals.
Conclusions:
- Further research into cancer's molecular origins can identify novel therapeutic targets.
- Biomarker profiling can optimize patient selection for kinase inhibitor therapy.
- Future clinical trials should explore optimal sequencing and adjuvant use of kinase inhibitors.
Related Concept Videos
02:54Protein Kinases and Phosphatases
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
02:54Protein Kinases and Phosphatases
02:49Cancer Therapies
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
01:25cAMP-dependent Protein Kinase Pathways
01:10Review and Preview
Percentiles are a type of fractile that partition data into...