KINAXO Launches KinAffinity® Services for Efficient Profiling of Kinase Inhibitors in Cells or Tissue

KINAXO Biotechnologies GmbH announced today that it added KinAffinity® to its service portfolio. KinAffinity® provides invaluable information about a kinase inhibitor’s selectivity in a cell or tissue of interest. It simultaneously determines affinities for native kinases expressed within a cellular proteome and thus overcomes the limitations of traditional biochemical assays that only use recombinant proteins.

Kinase inhibitors with favorable pharmaceutical properties are extensively pursued as therapeutics in numerous oncological, neurological and inflammatory indications. However, their development faces significant challenges such as target specificity for the disease-relevant target proteins. Here, KinAffinity® provides critical information to select the right lead compound for clinical development.
KinAffinity® combines proprietary chemical proteomics methods with state-of-the-art quantitative mass spectrometry (see Sharma et al., Nature Methods 2009).

Endogenously expressed, post-translationally modified kinases are enriched by a ready-to-use affinity matrix in the presence of native binding partners and competed with the kinase inhibitor of interest. Subsequently, bioinformatic methods are used to reveal the inhibitor’s quantitative cellular target profile. The inhibitor’s targets are ranked by their affinities and reported to the customer.

KinAffinity® is applicable for type I and type II kinase inhibitors. It facilitates selectivity analysis on an organism level that accounts for differences in protein expression between different cells, as well as their mutational and modification status that might affect drug binding.