Activating Compound | Comment | Organism | Structure |
---|---|---|---|
additional information | JAK2 activation loop structure, residues 994-1023, with phosphorylation sites Y1007 and Y1008, JAK2 switches between active and inactive forms involving the switch motif Asp994-Phe2995-Gly996 proximal to the active site, overview | Homo sapiens |
Application | Comment | Organism |
---|---|---|
drug development | JAK2 is a target for drug development, specific inhibitors are of tremendous clinical relevance | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expression of JAK2 kinase domain, comprisine residues 835-1132, as GST-fusion protein in Spodoptera frugiperda Sf9 cells using baculovirus transfection system | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
purified recombinant detagged JAK2 kinase domain bound to inhibitor CMP6, hanging drop vapour diffusion method, 20°C, mixing of equal volumes of protein solution, containing 10 mg/ml protein in 20 mM Tris, pH 8.5, 250 mM NaCl, and 1 mM DTT, and reservoir solution, containing 28% PEG 4000, 0.2 M ammonium acetate, and 0.1 M citrate, pH 6.0, 1-3 days, X-ray diffraction structure determination and analysis at 2.0 A | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
CMP6 | i.e. 2-tert-butyl-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinoline-7-1, specific for JAK2, kinase domain binding structure and mechanism | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | JAK2 is an important intracellular mediator of cytokine signalling, JAK2 deficiency may lead to hematologic cancers, and a number of immune diseases | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
phosphoprotein | activation of JAK2 by phosphorylation at sites Y1007 and Y1008 of the activation loop structure | Homo sapiens |
Purification (Comment) | Organism |
---|---|
recombinant GST-fusion JAK2 kinase domain from Sf9 insect cells, glutathione affinity chromatography, afterwards the JAK2 protein is treated with inhibitor CMP6 and the GST-tag is cleaved off by thrombin, followed by gel filtration | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | JAK2 is an important intracellular mediator of cytokine signalling, JAK2 deficiency may lead to hematologic cancers, and a number of immune diseases | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
JAK2 | - |
Homo sapiens |
Janus kinase 2 | - |
Homo sapiens |
More | JAK2 is a member of the Janus kinase family of PTKs | Homo sapiens |
Protein tyrosine kinase | - |
Homo sapiens |
PTK | - |
Homo sapiens |