TargetNet


P52333

Tyrosine-protein kinase JAK3


Function

Non-receptor tyrosine kinase involved in various processes such as cell growth, development, or differentiation. Mediates essential signaling events in both innate and adaptive immunity and plays a crucial role in hematopoiesis during T-cells development. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors sharing the common subunit gamma such as IL2R, IL4R, IL7R, IL9R, IL15R and IL21R. Following ligand binding to cell surface receptors, phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins. Subsequently, phosphorylates the STATs proteins once they are recruited to the receptor. Phosphorylated STATs then form homodimer or heterodimers and translocate to the nucleus to activate gene transcription. For example, upon IL2R activation by IL2, JAK1 and JAK3 molecules bind to IL2R beta (IL2RB) and gamma chain (IL2RG) subunits inducing the tyrosine phosphorylation of both receptor subunits on their cytoplasmic domain. Then, STAT5A AND STAT5B are recruited, phosphorylated and activated by JAK1 and JAK3. Once activated, dimerized STAT5 translocates to the nucleus and promotes the transcription of specific target genes in a cytokine-specific fashion.


Database Links

Database Links
UniProt P52333
PDB 1YVJ, 3LXK, 3LXL, 3PJC, 3ZC6, 3ZEP, 4HVD, 4HVG, 4HVH, 4HVI, 4I6Q
BioGrid 109921
BindingDB P52333
DrugBank Not available
Guide to PHARMACOLOGY 2049
PharmGKB PA29990
KEGG hsa:3718
BioCyc Not available
Entrez Gene (GeneID) 3718

Chemical Space of the Positive Compounds


Model Performance Metrics

Metric Mean Value Standard Deviation
AUC 0.9736 0.0012
Accuracy 0.9207 0.0037
Sensitivity 0.9004 0.0058
Specificity 0.9394 0.0048
BEDROC 0.9977 0.0017
MCC Threshold 0.512 N/A
MCC 0.8434 N/A
F-score Threshold 0.414 N/A
F-score 0.9167 N/A

Downloads

R Model Object

Random Forest model object (.RData)

Download RData

Positive Set

SMILES string + affinity value (.tsv)

Download TSV


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Page generated on: 2014-04-29 14:39:42