Kinases are an important target class in drug development, not only due to their etiology in disease, but also because they are considered to be highly ‘druggable’, as they are a target that can be chemically modulated by small molecules yet purified in large amounts. To date, the crystal structures of over forty different kinases have been published.
Protein kinases are a large and diverse enzyme family that catalyzes the transfer of γ phosphate groups from adenosine triphosphate (ATP) to hydroxyl groups on serine, threonine (ser, thr kinases; STKs) or tyrosine residues (tyrosine kinase; TKs). There are over 500 genes encoding protein kinases, of which at least 30% are phosphorylated themselves by other kinases, often arranging in coordinated and cascading cellular pathways. Protein phosphorylation, therefore, acts a critical ‘switching’ mechanism in many cellular responses. Conversely, disregulation of cellular phosphorylation is now implicated in a large number of diseases.
Check the Kinase Pathway Map for a graphical representation of Kinase pathways detectible with PerkinElmer assays. For additional details on drug discovery and assay strategies please refer to our technical library.
Assay platforms include:
- The versatile Alpha Technology provides a platform for measurement of phosphorylated peptides and full-length protein substrates. Perform optimized cellular kinase assays that require no wash steps with Alpha SureFire and capture endogenous phosphorylated proteins with ease.
- LANCE and LANCE Ultra TR-FRET assays are ideal for Tyrosine (Tyr) and Serine/Threonine (Ser/Thr) kinases. For a specific Tyrosine or Serine/Threonine target, try our optimized LANCE Ultra reagents with ULight-substrate and Eu-anti-phospho-antibody pairs. If you are unsure of your Ser/Thr kinase substrate target, try our KinaSelect kit for optimizing your kinase to its target sequence.
- A proven performer, DELFIA® technology is a robust, established time-resolved fluorometric (TRF) assay method for secondary screening and hit confirmation.
- The gold standard for traditional filter binding assays 33P-labeled or 32P-labeled NEN® Radionucleotides deliver unmatched assay performance and quality.
- FlashPlate Plus is a robust homogeneous radioactive platform, Kinase assays can be quickly developed on 96- or 384-well FlashPlates.
- OnPoint reagent services give you access to expertise when you need it most. Our team of scientists can assist you with assay development, custom labeling and custom membrane and cell line development.