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Updated: May 15, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
Kinase drug discovery--what's next in the field?
1MRC Protein Phosphorylation Unit, University of Dundee, Dundee DD1 5EH, United Kingdom. p.cohen@dundee.ac.uk
Abstract:
Over the past 15 years protein kinases have become the pharmaceutical industry's most important class of drug target in the field of cancer. Some 20 drugs that target kinases have been approved for clinical use over the past decade, and hundreds more are undergoing clinical trials. However, the recent approval of the first protein kinase inhibitors for the treatment of inflammatory diseases, coupled with an enhanced understanding of the signaling networks that control the immune system, suggests that there will be a surge of interest in this area over the next 10 years. In this connection, we discuss opportunities for targeting protein kinases in the MyD88 signaling network for the development of drugs to treat chronic inflammatory and autoimmune diseases. Activating mutations in protein kinases underlie many other diseases and conditions, and we also discuss why the protein kinases SPAK/OSR1 and LRRK2 have recently become interesting targets for the treatment of hypertension and Parkinson's disease, respectively, and the progress that has been made in developing LRRK2 inhibitors. Finally we suggest that more focus on the identification of inhibitors of kinase activation, rather than kinase activity, may pay dividends in identifying exquisitely specific inhibitors of signal transduction cascades, and we also highlight "pseudo-kinases" as an attractive and unexplored area for drug development that merits much more attention in the years to come.
Insights
Protein kinases are crucial drug targets for cancer and inflammation. New research explores targeting the MyD88 pathway for autoimmune diseases and highlights pseudo-kinases as promising drug targets.
Area of Science:
- Biochemistry
- Pharmacology
- Immunology
Background:
- Protein kinases are a major focus for drug development, particularly in oncology.
- Recent approvals for inflammatory diseases and advances in immunology signal growing interest in kinase inhibitors for immune-related conditions.
Purpose of the Study:
- To explore targeting the MyD88 signaling network for treating chronic inflammatory and autoimmune diseases.
- To discuss the potential of SPAK/OSR1 and LRRK2 kinases as therapeutic targets for hypertension and Parkinson's disease, respectively.
- To highlight pseudo-kinases as a novel and underexplored area for drug discovery.
Main Methods:
- Review of current literature on protein kinase inhibitors and signaling pathways.
- Analysis of MyD88 signaling network in the context of inflammation and autoimmune diseases.
- Discussion of drug development strategies, including targeting kinase activation and pseudo-kinases.
Main Results:
- Protein kinase inhibitors are increasingly important in treating cancer and inflammatory diseases.
- The MyD88 signaling network presents opportunities for novel anti-inflammatory and autoimmune drug development.
- SPAK/OSR1 and LRRK2 kinases are identified as promising targets for hypertension and Parkinson's disease.
Conclusions:
- Targeting protein kinases offers significant therapeutic potential beyond cancer, particularly in inflammatory and autoimmune diseases.
- Developing inhibitors that target kinase activation and exploring pseudo-kinases could lead to more specific and effective treatments for various diseases.
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