January 2007

Boehinger Ingelheim R&D and Kinasource publish results of a successful collaboration

Why would a large pharmaceutical company want to do KESTREL experimentation?

Well, protein kinases are important drug targets and only 25% of the exisiting 520 protein kinases are well understood. For a good number of the kinases very few physiological substrates are known and the existing kinase assays are poor. Phosphorylated substrates in blood cells may be useful as biomarkers for inhibitor efficacy. For these and other reasons Kinasource collaborates with several pharmaceutical companies.

Boehringer Ingelheim Ridgefield has collaborated with Kinasource in order to identify novel substrates for Pim-2, a member of only three kinases in the Pim-family. We have identified a number of substrates from rat thymus, one of which, eukaryotic translation initiation factor 4B (eIF4B), became phosphorylated by Pim-2 at Ser406 in a RERHPSWRSE motif. The team at Boehringer Ingelheim used this information to generate a 20 times better peptide substrate, a useful tool for inhibitor screening (Peng et al., 2007 Journal of Biochemistry 141:353-362).