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KinaTor

Together with scientists at the Max Planck Institute for Biochemistry in Martinsried, GPC Biotech AG and Kinaxo Biotechnologies GmbH we have developed a sophisticated chemical derivatization based affinity chromatography technology for selectivity profiling and off-target identification of kinase inhibitors. The strategic relevance of the KinaTor technology in the area of lead finding and optimization is twofold. Firstly, it provides the ultimate selectivity panel for a lead of any ongoing optimization program on distinct kinase targets, and secondly, it identifies novel and unexpected kinase targets for an investigated compound series templated on a privileged structure. The KinaTor-technology is offered on a service basis by Kinaxo (Martinsried, Germany) which helds exclusive worldwide licenses from the Max-Planck Society and GPC Biotech AG. Vichem is generating the functional derivatives, which are being used for immobilization. The derivatization service combines structural and synthetic know how and can be offered to interested partners on a non-exclusive basis.

The KinaTor technology relies on the coupling of small molecule kinase inhibitors via a linker to a matrix with the aim to generate an affinity chromatography material, which exploits the strong binding affinities between kinase inhibitors and their molecular targets. A key element of the technology is the proper chemical modification of the kinase inhibitor on such a way that it maintains its kinase inhibitory activity. Once coupled and proven active, immobilized ligands are processed in an affinity chromatography approach to identify all the relevant targets and off-targets from a crude extract, which bind to this matrix. MS analysis of the identified protein spots and a parallel LC-MS/MS analysis permit detection of all the bound proteins (see Kinaxo homepage).

Until today, we have developed >40 KinaTor molecules (properly derivatized kinase inhibitors) for our partners (Kinaxo, MPI, GPC Biotech, EPFL, KU Leuven, Johnson & Johnson etc.) to enable selectivity profiling and off-target identifications of selected kinase inhibitors.