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Updated: Sep 2, 2025

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

Published on: December 7, 2014

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Recent advances in targeting protein kinases and pseudokinases in cancer biology

Kristina Riegel1, Parthiban Vijayarangakannan2, Petros Kechagioglou1

  • 1Cell Biology Unit, University Medical Center Mainz, JGU-Mainz, Mainz, Germany.

Frontiers in Cell and Developmental Biology
|August 8, 2022
PubMed

Insights

Kinase inhibitors are FDA-approved cancer drugs, but many kinases and pseudokinases remain understudied. This review highlights recent advances in targeting these proteins for cancer therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Kinases are crucial drug targets in oncology, with numerous FDA-approved inhibitors for cancer treatment.
  • Despite successes, a significant portion of the kinome (the complete set of kinases) remains underexplored.
  • Pseudokinases, a related class of proteins, are increasingly recognized for their role in cancer.

Purpose of the Study:

  • To summarize recent advancements in targeting kinases and pseudokinases in cancer.
  • To highlight successful strategies, such as targeting cell cycle machinery.
  • To discuss emerging approaches for effectively targeting pseudokinases in oncological applications.

Main Methods:

  • Literature review of recent developments in kinase and pseudokinase research.
  • Analysis of successful kinase inhibitor therapies.
  • Exploration of strategies for targeting understudied kinases and pseudokinases.

Main Results:

  • The review covers recent progress in understanding and targeting kinases and pseudokinases.
  • Examples of successful targeting strategies are provided.
  • The importance of exploring understudied kinome regions is emphasized.

Conclusions:

  • Kinases remain a highly druggable target class for cancer therapy.
  • Further research into understudied kinases and pseudokinases is essential for developing novel cancer treatments.
  • Effective targeting strategies for pseudokinases hold promise for future cancer drug development.
Keywords:
CDK4/6MAPKRAFallosteric regulationcancerinhibitorskinomemolecular switch

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