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lymphocyte-specific protein tyrosine kinase - LCK

Target Class Kinases FamilyTK
SpeciesHuman   
Background
This gene is a member of the Src family of protein tyrosine kinases (PTKs). The encoded protein is a key signaling molecule in the selection and maturation of developing T-cells. It contains N-terminal sites for myristylation and palmitylation, a PTK domain, and SH2 and SH3 domains which are involved in mediating protein-protein interactions with phosphotyrosine-containing and proline-rich motifs, respectively. The protein localizes to the plasma membrane and pericentrosomal vesicles, and binds to cell surface receptors, including CD4 and CD8, and other signaling molecules. Multiple alternatively spliced variants, encoding the same protein, have been described. [provided by RefSeq, Jul 2008]

Protein Source
Human(recombinant):Expressed in E. coli
Readout
KINOMEscan
Method
Detect kinase displacment by competitor compounds from an immobilized ligand using qPCR
Substrate
Arachidonic Acid
Agonist Effect (Activation)
T cell activation
Antagonist Effect (Inhibition)
T cell inhibition; SCID-like immunodeficiency
Ref.
Bowes et. al. 2012
AntagonistIC50(nM)
Dasatinib0.2
Vandetanib17
Imatinib40
Binding reactions are assembled by combining kinases, liganded affinity beads, and test compounds in 384-well plates. The assay plates are incubated at room temperature with shaking for 1 hour. Affinity beads are washed and then re-suspended in elution buffer. The kinase concentration in the eluates was measured by qPCR.
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