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Protein kinases are involved in many cellular signaling pathways and comprise one of the largest families of homologous proteins. They play an extensive role in signal transduction and regulation of the complex cellular processes necessary to maintain life. Overexpression and/or dysregulation of protein kinases lead to a variety of diseases, thus providing numerous targets for drug development. Currently, approximately 24% of all research spending on drug discovery and development is focused on kinases. In view of the huge demand for small molecules that target this class of proteins, many technologies and platforms have been developed for the discovery of kinase inhibitors, including biochemical-based functional assays and compound-binding competition assays.

The critical role of kinases in human biology:

  1. Important components of cell signal transduction
  2. Regulation of many cellular processes through phosphorylation of diverse substrates (proteins, lipids, sugars)
  3. About 518 protein kinase in human genome (388 S/T, 90 Tyr, 40 atypical) & more
  4. More than third of all human proteins are phosphorylated

Protein kinases represent one of the most promising groups of drug targets owing to their involvement in such pathological conditions such as cancer, neural disorders, inflammatory diseases, and metabolism problems. Classical methods to analyze kinase activity involve the quantification of phosphoryl transfer by detecting the production of the phosphorylated product or the changes in the ratio of ATP to ADP. To assist the efforts in kinase drug discovery, Creative Bioarray offers high quality, time efficient and cost effective kinase solution for assay development, high throughput screening (HTS) and selectivity profiling.

Radiometric-based Assays

  • Filtration binding assay
  • Scintillation proximity assay

Fluorescence-based Detection Assays

  • Fluorescence intensity (FI) assay
  • Fluorescence polarization (FP) assay
  • Fluorescence resonance energy transfer (FRET)
  • Time-resolved fluorescence (TRF)
  • Time-resolved fluorescence resonance energy transfer (TR-FRET)
  • Enzyme-linked immunosorbent assay
  • Luminescence detection
  • Mobility shift assay
  • Ligand-kinase binding assay

Features of the Kinase Assay in Creative Bioarray

  • Homogeneous, nonradioactive, robust
  • Universal (any enzyme substrate combinations)
  • Applicable for different kinases and diverse substrates
  • Use multi-phosphorylated substrates
  • Minimal false hits
  • Distinguish between ATP competitive and noncompetitive inhibitors

Creative Bioarray has decades of experience in providing kinase products and services to meet a variety of drug discovery research needs. Whether you need a high quality, active protein for your internal research and drug discovery screening, or you are looking to outsource your custom protein production, assay development, and kinase selectivity profiling, our team can help support your projects.

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