Tclin ITK Tyrosine-protein kinase ITK/TSK

Protein Summary

Description

Tyrosine kinase that plays an essential role in regulation of the adaptive immune response. Regulates the development, function and differentiation of conventional T-cells and nonconventional NKT-cells. When antigen presenting cells (APC) activate T-cell receptor (TCR), a series of phosphorylation lead to the recruitment of ITK to the cell membrane, in the vicinity of the stimulated TCR receptor, where it is phosphorylated by LCK. Phosphorylation leads to ITK autophosphorylation and full activation. Once activated, phosphorylates PLCG1, leading to the activation of this lipase and subsequent cleavage of its substrates. In turn, the endoplasmic reticulum releases calcium in the cytoplasm and the nuclear activator of activated T-cells (NFAT) translocates into the nucleus to perform its transcriptional duty. Phosphorylates 2 essential adapter proteins: the linker for activation of T-cells/LAT protein and LCP2. Then, a large number of signaling molecules such as VAV1 are recruited and ultimately lead to lymphokine production, T-cell proliferation and differentiation (PubMed:12186560, PubMed:12682224, PubMed:21725281). Phosphorylates TBX21 at 'Tyr-530' and mediates its interaction with GATA3 (By similarity). This gene encodes an intracellular tyrosine kinase expressed in T-cells. The protein contains both SH2 and SH3 domains which are often found in intracellular kinases. It is thought to play a role in T-cell proliferation and differentiation. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• Q08881
• B2R752
• Q32ML7

Gene Name

• ITK

Ensembl ID

• ENST00000422843
• ENSP00000398655
• ENSG00000113263

Symbol

• EMT
• LYK
• EMT
• LYK
• LPFS1
• PSCTK2

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
protein domain	1
molecular function	0.96
hub protein	0.88
biological process	0.73
kinase	0.71

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Tk Group / Tec Family / Tyrosine-protein Kinase Itk/tsk

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 2864.42   (req: < 5)

Gene RIFs: 59   (req: <= 3)

Antibodies: 465   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 2864.42   (req: >= 5)

Gene RIFs: 59   (req: > 3)

Antibodies: 465   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 17

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 305

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 4