Targeting protein kinases in central nervous system disorders

Laura K. Chico, Linda J. Van Eldik, D. Martin Watterson

Research output: Contribution to journalReview articlepeer-review

232 Scopus citations


Protein kinases are a growing drug target class in disorders in peripheral tissues, but the development of kinase-targeted therapies for central nervous system (CNS) diseases remains a challenge, largely owing to issues associated specifically with CNS drug discovery. However, several candidate therapeutics that target CNS protein kinases are now in various stages of preclinical and clinical development. We review candidate compounds and discuss selected CNS protein kinases that are emerging as important therapeutic targets. In addition, we analyse trends in small-molecule properties that correlate with key challenges in CNS drug discovery, such as blood-brain barrier penetrance and cytochrome P450-mediated metabolism, and discuss the potential of future approaches that will integrate molecular-fragment expansion with pharmacoinformatics to address these challenges.

Original languageEnglish
Pages (from-to)892-909
Number of pages18
JournalNature Reviews Drug Discovery
Issue number11
StatePublished - 2009

Bibliographical note

Funding Information:
The authors acknowledge funding from the National Institutes of Health (AG031311, NS056051 and AG013939).

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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