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A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Are MAP kinases drug targets? Yes, but difficult ones
Simona Margutti1, Stefan A Laufer
1Institute of Pharmacy, Department of Pharmaceutical and Medicinal Chemistry; Eberhard Karls University of Tuebingen, Auf der Morgenstelle 8, 72076 Tuebingen, Germany.
Chemmedchem
|June 2, 2007
Summary
Protein kinase inhibitors are crucial in drug discovery, with recent successes driving further research. Challenges remain in target selection due to kinase similarity and unclear pathway-disease links, particularly for MAPK pathways.
Area of Science:
- Biochemistry
- Pharmacology
- Drug Discovery
Background:
- Pharmaceutical companies increasingly focus on novel target identification and validation.
- Protein kinase inhibitors represent a significant area of research and development in drug discovery.
- Recent successful drug launches have spurred further interest in kinase inhibitors.
Purpose of the Study:
- To provide a comprehensive overview of protein kinase inhibition.
- To highlight successful examples and clinical candidates, with a focus on the MAPK pathway.
- To address the challenges in kinase target selection and validation.
Main Methods:
- Review of current literature on protein kinase inhibitors.
- Analysis of successful kinase inhibitor drugs and clinical candidates.
- Focus on the Mitogen-Activated Protein Kinase (MAPK) pathway.
Main Results:
- The field of protein kinase inhibitors has advanced significantly, altering perceptions of kinases as drug targets.
- Several protein kinase inhibitors have achieved market success, with many more in clinical development.
- Challenges persist regarding kinase similarity, functional redundancy, and pathway-disease associations.
Conclusions:
- Protein kinase inhibition is a vital strategy in modern drug discovery.
- Despite challenges, kinase inhibitors, especially targeting MAPK pathways, hold significant therapeutic potential.
- Continued research is needed to overcome hurdles in target selection and fully elucidate pathway-disease connections.
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