Details of the Target
General Information of Target
Target ID | LDTP05576 | |||||
---|---|---|---|---|---|---|
Target Name | Tyrosine-protein kinase ITK/TSK (ITK) | |||||
Gene Name | ITK | |||||
Gene ID | 3702 | |||||
Synonyms |
EMT; LYK; Tyrosine-protein kinase ITK/TSK; EC 2.7.10.2; Interleukin-2-inducible T-cell kinase; IL-2-inducible T-cell kinase; Kinase EMT; T-cell-specific kinase; Tyrosine-protein kinase Lyk |
|||||
3D Structure | ||||||
Sequence |
MNNFILLEEQLIKKSQQKRRTSPSNFKVRFFVLTKASLAYFEDRHGKKRTLKGSIELSRI
KCVEIVKSDISIPCHYKYPFQVVHDNYLLYVFAPDRESRQRWVLALKEETRNNNSLVPKY HPNFWMDGKWRCCSQLEKLATGCAQYDPTKNASKKPLPPTPEDNRRPLWEPEETVVIALY DYQTNDPQELALRRNEEYCLLDSSEIHWWRVQDRNGHEGYVPSSYLVEKSPNNLETYEWY NKSISRDKAEKLLLDTGKEGAFMVRDSRTAGTYTVSVFTKAVVSENNPCIKHYHIKETND NPKRYYVAEKYVFDSIPLLINYHQHNGGGLVTRLRYPVCFGRQKAPVTAGLRYGKWVIDP SELTFVQEIGSGQFGLVHLGYWLNKDKVAIKTIREGAMSEEDFIEEAEVMMKLSHPKLVQ LYGVCLEQAPICLVFEFMEHGCLSDYLRTQRGLFAAETLLGMCLDVCEGMAYLEEACVIH RDLAARNCLVGENQVIKVSDFGMTRFVLDDQYTSSTGTKFPVKWASPEVFSFSRYSSKSD VWSFGVLMWEVFSEGKIPYENRSNSEVVEDISTGFRLYKPRLASTHVYQIMNHCWKERPE DRPAFSRLLRQLAEIAESGL |
|||||
Target Type |
Clinical trial
|
|||||
Target Bioclass |
Enzyme
|
|||||
Family |
Protein kinase superfamily, Tyr protein kinase family, TEC subfamily
|
|||||
Subcellular location |
Cytoplasm
|
|||||
Function |
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. Required for TCR-mediated calcium response in gamma-delta T-cells, may also be involved in the modulation of the transcriptomic signature in the Vgamma2-positive subset of immature gamma-delta T-cells. Phosphorylates TBX21 at 'Tyr-530' and mediates its interaction with GATA3.
|
|||||
TTD ID | ||||||
Uniprot ID | ||||||
DrugMap ID | ||||||
Ensemble ID | ||||||
HGNC ID | ||||||
ChEMBL ID |
Probe(s) Labeling This Target
ABPP Probe
Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
---|---|---|---|---|---|
IPM Probe Info |
![]() |
N.A. | LDD0241 | [1] | |
4-Iodoacetamidophenylacetylene Probe Info |
![]() |
C289(0.00); C143(0.00); C488(0.00); C199(0.00) | LDD0038 | [2] | |
IA-alkyne Probe Info |
![]() |
C289(0.00); C143(0.00); C339(0.00); C488(0.00) | LDD0036 | [2] | |
Lodoacetamide azide Probe Info |
![]() |
C289(0.00); C594(0.00); C143(0.00); C488(0.00) | LDD0037 | [2] | |
Compound 10 Probe Info |
![]() |
C143(0.00); C289(0.00); C488(0.00) | LDD2216 | [3] | |
Compound 11 Probe Info |
![]() |
N.A. | LDD2213 | [3] |
Competitor(s) Related to This Target
The Interaction Atlas With This Target
The Protein(s) Related To This Target
Enzyme
Protein name | Family | Uniprot ID | |||
---|---|---|---|---|---|
Receptor tyrosine-protein kinase erbB-2 (ERBB2) | Tyr protein kinase family | P04626 |
Transporter and channel
Protein name | Family | Uniprot ID | |||
---|---|---|---|---|---|
Heat shock protein HSP 90-beta (HSP90AB1) | Heat shock protein 90 family | P08238 |
Cytokine and receptor
Protein name | Family | Uniprot ID | |||
---|---|---|---|---|---|
Tumor necrosis factor ligand superfamily member 6 (FASLG) | Tumor necrosis factor family | P48023 |
Other
Protein name | Family | Uniprot ID | |||
---|---|---|---|---|---|
Lymphocyte cytosolic protein 2 (LCP2) | . | Q13094 |
The Drug(s) Related To This Target
Approved
Drug Name | Drug Type | External ID | |||
---|---|---|---|---|---|
Fostamatinib | Small molecular drug | DB12010 | |||
Pazopanib | Small molecular drug | DB06589 | |||
Zanubrutinib | . | DB15035 |
Phase 2
Drug Name | Drug Type | External ID | |||
---|---|---|---|---|---|
Jte-051 | . | D01EJJ |
Phase 1
Drug Name | Drug Type | External ID | |||
---|---|---|---|---|---|
Cpi-818 | Small molecular drug | D1YZ5O |
Investigative
Drug Name | Drug Type | External ID | |||
---|---|---|---|---|---|
Bms-509744 | Small molecular drug | D04PEI | |||
Staurosporine | Small molecular drug | DB02010 | |||
Bms-488516 | . | D05RPN |
Patented
Drug Name | Drug Type | External ID | |||
---|---|---|---|---|---|
Pmid27774824-compound-figure3example7 | Small molecular drug | D02IET | |||
Pyrazolo[4,3-c]Pyridine Derivative 2 | . | D09PIS |
References