The Clinical Kinase Index: A Method to Prioritize Understudied Kinases as Drug Targets for the Treatment of Cancer

Derek Essegian, Rimpi Khurana, Vasileios Stathias, Stephan C. Schürer

Research output: Contribution to journalArticlepeer-review

2 Scopus citations

Abstract

The approval of the first kinase inhibitor, Gleevec, ushered in a paradigm shift for oncological treatment—the use of genomic data for targeted, efficacious therapies. Since then, over 48 additional small-molecule kinase inhibitors have been approved, solidifying the case for kinases as a highly druggable and attractive target class. Despite the role deregulated kinase activity plays in cancer, only 8% of the kinome has been effectively “drugged.” Moreover, 24% of the 634 human kinases are understudied. We have developed a comprehensive scoring system that utilizes differential gene expression, pathological parameters, overall survival, and mutational hotspot analysis to rank and prioritize clinically relevant kinases across 17 solid tumor cancers from The Cancer Genome Atlas. We have developed the clinical kinase index (CKI) app (http://cki.ccs.miami.edu) to facilitate interactive analysis of all kinases in each cancer. Collectively, we report that understudied kinases have potential clinical value as biomarkers or drug targets that warrant further study.

Original languageEnglish (US)
Article number100128
JournalCell Reports Medicine
Volume1
Issue number7
DOIs
StatePublished - Oct 20 2020

Keywords

  • cancer drug target
  • clinical scoring system
  • data integration
  • differential gene expression
  • druggable genome
  • human kinome
  • Kaplan-Meier survival analysis
  • target validation
  • TNM score
  • understudied kinase

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Medicine(all)

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