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Updated: Aug 13, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
12:40

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors

Published on: December 7, 2014

Therapeutic modulation of inflammatory gene transcription by kinase inhibitors

Gordon Alton1, Klaus Schwamborn, Yoshi Satoh

  • 1Biochemistry Department, Pfizer Global Research and Development, La Jolla Laboratories, 4215 Sorrento Valley Boulevard, San Diego, CA 92121, USA. galton@pfizer.com

Expert Opinion on Biological Therapy
|August 13, 2002
PubMed

Insights

Altered gene expression drives inflammatory diseases. Targeting protein kinases, enzymes regulating gene activity, offers a promising therapeutic strategy for inflammation treatment.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Altered gene expression and protein levels are central to inflammatory disease aetiology.
  • Transcription factors control inflammatory gene expression, with their activity regulated by signal transduction networks.
  • Protein kinases are key signal transducers, modulating transcription factor activity through phosphorylation.

Purpose of the Study:

  • To review kinase inhibitors in development for inflammatory diseases.
  • To highlight the role of transcription factors in inflammation.
  • To explore targeted small molecule inhibitors for selective therapies.

Main Methods:

  • Review of current literature on protein kinase inhibitors.
  • Analysis of signal transduction pathways in inflammation.
  • Examination of transcription factor involvement in inflammatory gene regulation.

Main Results:

  • Protein kinases are crucial in pro-inflammatory signaling cascades.
  • Pharmacological inhibition of protein kinases presents a viable therapeutic approach for inflammation.
  • Imatinib exemplifies successful tyrosine kinase inhibition in medicine.

Conclusions:

  • Targeted kinase inhibitors offer potential for selective, tissue-specific therapies for inflammatory conditions.
  • Understanding kinase-transcription factor interactions is key to developing novel anti-inflammatory drugs.

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