s new NanoBRET Target Engagement Intracellular Kinase
Assay (NanoBRET TE) is the first assay to quantify inhibitor drug binding to kinase
proteins inside live human cells, and shows greater predictive potential compared to traditional approaches that use purified kinase
domains in non-cell-based assays, the company said.
Firstly, high level of PIM-1 kinase
was discovered in lymphoma tumours and leukaemia .
M2 EQUITYBITES-October 10, 2016-Nexus BioPharma to license TransChem's transition state chemistry technology for kinase
Inhibitors are specific enzymes which oppose the process of cell division and growth in cancerous cells.
In cases in which tyrosine kinase
inhibitors are effective they reduce signaling via both the PI3K/AKT and MEK/ERK signaling pathways.
Molecular biologists, biochemists, pharmaceutical chemists, and other researchers highlight the therapeutic potential of kinase
inhibitors to disrupt the role they play in tumor progression and several other diseases.
In this work, Matthews (executive director of oncology discovery at Exelixis, "an integrated drug discovery and development company") and Gerritsen (vice president of molecular and cellular pharmacology also at Exelixis) provide a broad, if necessarily selective, treatment of kinase
cancer targets and the drugs that inhibit them, with a focus on small molecule inhibitors.
The study, led by University of Iowa scientists, demonstrated in theory, that it might be possible to use drugs that maintain the positive effects on heart function of a known enzyme called calmodulin kinase
II (CaM kinase
) while reducing its negative effects.
Available for both purchase and as part of the proprietary KinaseProfiler service, the expanded PI3 kinase
line now offers 17 lipid kinases
, which are a new class of potential drug targets.
These effects are regulated by complex intracellular signaling pathways including MAPKs, phospholipase C, protein kinase
C, and phospholipase A2.
Since receptor-binding Fn peptides decrease focal contacts, disturb cytoskeletal elements such as actin and decrease Fn receptor aggregation in fibroblasts, we have proposed that Fn-fs have similar effects in chondrocytes and that these changes in receptor and cytoskeletal elements alter the location of upstream kinases
near receptors which leads to altered signal transduction and emergence of inflammatory MAP kinase
Kinexus Bioinformatics Corporation, Vancouver, a Canadian proteomics company, has announced the validation of its unique approach for protein kinase
drug target discovery with the publication of its latest research findings in the September printed issue of the Journal of Biological Chemistry.