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

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. Teaser: Kinase activity assays hold the potential to accelerate effective PKI development by addressing a multitude of challenges. Here, we explore how these kinase activity assays solve these challenges and improve PKI development.

Informations de copyright

Copyright © 2024. Published by Elsevier Ltd.

Déclaration de conflit d'intérêts

Conflicts of interest Maarten Altelaar is one of the patent holders of the described T-loop kinase activity assay QuantaKinome™. Nynke Kannegieter, Erik de Graaf, Jos Joore and Anna Ressa are former employees of Pepscope, which offered the kinase activity assay QuantaKinome™. All other authors have no conflicts of interest to declare.