Kinases

Protein kinases are a group of enzymes with the basic biochemical function of phosphorylation of other proteins. Protein kinases represent one of the most important classes of cellular proteins. As the principle components of cell signal transduction pathways, the activity of kinases often controls the activities of “effector” proteins, which in turn affect the profiles of cellular gene expression. Kinase signaling pathways play a primary role in regulating cell proliferation, cell metabolism and cell death. Research has shown that changes in protein kinase activity within a cell can lead to several disease states, most notably cancer. With this knowledge base, scientists have been investigating the ability of drugs to block various protein kinases as a cancer therapy. This approach has proved successful with the discovery of several kinase inhibitor drugs for the treatment of various cancers such as Gleevec^®, Iressa^® and Tarceva^®.  In addition to their involvement in cancer, protein kinases are implicated in diabetes, inflammation and neurological development and degeneration.

KinaseScreen™ PROFILEing
Kinase selectivity profiling is a mainstay of modern drug discovery as target selectivity and specificity are common problems in the identification and development of candidate kinase inhibitors. CDAS' KinaseAdvisor and RapidKinaseProfiling services have been developed to answer specific needs for both large and highly customizable assay panels and for quick (less than a week turnaround time) kinase profiling.

KinaseScreen™ HTS
Screen your library of compounds in any kinase assay developed as part of the CDAS KinaseScreen program. All screening projects are highly customized to meet our clients’ expectations of throughput, process & workflow and screening data reporting.

KinaseScreen™ IC₅₀
Determine compound inhibitor potency in selected kinase assays developed as part of the CDAS KinaseScreen program.

KinaseScreen™ Mechanism of Action (MoA)
Mechanism of Action studies provide researchers with detailed information about the manner in which their compounds interact with enzymatic targets and are important for characterizing allosteric inhibitors and assessing kinetic on and off rates.

Learn more about the procedure developed by CDAS to determine your compounds mechanisms of actions using unique Caliper LabChip® technology features.

Technology platform
CDAS conducts KinaseScreen in vitro kinase profiling, high throughput screening and compound Mechanism of Actions services using the LabChip® 3000 and EZ Reader microfluidic technology platforms and ProfilerPro™ Kinase Selectivity Assay Kits developed by Caliper Life Sciences.

   Key features and benefits of the technology:
     •  No monoclonal antibodies or radioisotopes are required
     •  Detection of biochemical inhibition in a direct, ratiometric, high quality format in which both substrate 
        and product are measured in every well
     •  Wide range of kinase assays: Serine/Threonine, Receptor and Cytoplasmic Tyrosine kinases but
        also inhibitors of Lipid  kinases such as PI3 kinase(e.g. PI3K-alpha) and Sphingosine kinase are easily 
        detected

   The separation and direct measurement of substrates and products allowing:
     •  Higher signal-to-noise ratios
     •  Fewer false positive and negative results
     •  The identification and elimination of enzymatic activities that are not associated with the kinase 
         reaction of interest
     •  The ability to read over time (kinetic format)

   A small reaction volume is used for the detecttion of substrate and product:
     •  Minimum sample requirements (100 ug is enough for profiling a compound in a broad panel of assays
     •  Profile your new lead compounds and other chemicals faster and at a lower cost
     •  Due to minimal sample requirements you save your compound for additional CDAS in vitro studies