Innovative strategies for measuring kinase activity to accelerate the next wave of novel kinase inhibitors

Tim S. Veth, Nynke M. Kannegieter, Erik L. de Graaf, Rob Ruijtenbeek, Jos Joore, Anna Ressa, Maarten Altelaar*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

Abstract

The development of protein kinase inhibitors (PKIs) has gained significance owing to their therapeutic potential for diseases like cancer. In addition, there has been a rise in refining kinase activity assays, each possessing unique biological and analytical characteristics crucial for PKI development. However, the PKI development pipeline experiences high attrition rates and approved PKIs exhibit unexploited potential because of variable patient responses. Enhancing PKI development efficiency involves addressing challenges related to understanding the PKI mechanism of action and employing biomarkers for precision medicine. Selecting appropriate kinase activity assays for these challenges can overcome these attrition rate issues. This review delves into the current obstacles in kinase inhibitor development and elucidates kinase activity assays that can provide solutions.

Original languageEnglish
Article number103907
Pages (from-to)1-11
Number of pages11
JournalDrug Discovery Today
Volume29
Issue number3
DOIs
Publication statusPublished - Mar 2024

Bibliographical note

Publisher Copyright:
© 2024 The Authors

Funding

We thank Nick Veringmeier (JustPushPlay) for proofreading and improving the manuscript's readability. This work has been supported by EPIC-XS, project number 823839, funded by the Horizon 2020 programme of the European Union and the NWO funded Netherlands Proteomics Centre through the National Road Map for Large-scale Infrastructures program X- Omics, Project 184.034.019.

FundersFunder number
EPIC-XS - Horizon 2020 programme of the European Union823839
NWO funded Netherlands Proteomics Centre through the National Road Map for Large-scale Infrastructures program X- Omics184.034.019

    Keywords

    • biomarkers
    • inhibitor development
    • kinase activity assays
    • Kinases
    • mechanism of action
    • phosphorylation
    • protein kinase inhibitors

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