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Targeting kinases with precision.

Alexandra K Gardino1, Erica K Evans1, Joseph L Kim1

  • 1Blueprint Medicines, Cambridge, MA, USA.

Molecular & Cellular Oncology
|September 26, 2018
PubMed
Summary
This summary is machine-generated.

Cancer genomics reveals diverse kinase mutations, posing challenges for drug discovery. Tailored strategies are needed to develop precise cancer therapies based on tumor molecular profiles.

Keywords:
BLU-285avapritinibgastrointestinal stromal tumorprecision medicinesystemic mastocytosis

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Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Cancer genomics has identified heterogeneous mutations in kinases, leading to varied activation mechanisms.
  • Developing potent and selective drugs against these mutated kinases presents a significant challenge.

Purpose of the Study:

  • To bridge the gap between cancer genomic insights and drug discovery strategies.
  • To enable the development of precision cancer medicines tailored to individual tumor genotypes.

Main Methods:

  • Analysis of cancer genomics data.
  • Mechanistic studies of kinase activation.
  • Drug discovery and optimization strategies.

Main Results:

  • Identification of diverse kinase activation mechanisms driven by heterogeneous mutations.
  • Development of strategies for creating potent and selective kinase inhibitors.

Conclusions:

  • Optimized drugs can facilitate personalized medicine approaches.
  • Precision treatment based on molecular tumor genotype is achievable with advanced therapeutic options.