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Novel approaches for targeting kinases

Jacob, Sandra, Jahnke, Wolfgang and Knapp, Stefan (2014) Novel approaches for targeting kinases. Future Medicinal Chemistry, 6 (5). pp. 541-561. ISSN 1756-89191756-8927


Protein kinases are involved in many essential cellular processes and their deregulation can lead to a variety of diseases, including cancer. The pharmaceutical industry has invested heavily in the identification of kinase inhibitors to modulate these disease promoting pathways, resulting in several successful drugs. However, the field is challenging as it is difficult to identify novel selective inhibitors with good PK/PD properties. In addition, resistance to kinase inhibitor treatment frequently arises. The identification of non-ATP site targeting (“allosteric”) modulators, and the expansion of kinase target space to include the less studied members of the family, including atypical and pseudokinases, are potential avenues to overcome these challenges. In this perspective we will discuss the opportunities and challenges of following these approaches and others.

Item Type: Article
Date Deposited: 26 Apr 2016 23:46
Last Modified: 26 Apr 2016 23:46


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