Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T91761
|
||||
Former ID |
TTDR00858
|
||||
Target Name |
Tyrosine-protein kinase itk/tsk
|
||||
Gene Name |
ITK
|
||||
Synonyms |
Inducible T cell kinase; Kinase EMT; T-cell-specific kinase; Tyrosine kinase ITK; Tyrosine-protein kinase Lyk; ITK
|
||||
Target Type |
Clinical Trial
|
||||
Disease | Allergy [ICD9: 995.3; ICD10: T78.4] | ||||
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.
|
||||
BioChemical Class |
Kinase
|
||||
UniProt ID | |||||
EC Number |
EC 2.7.10.2
|
||||
Sequence |
MNNFILLEEQLIKKSQQKRRTSPSNFKVRFFVLTKASLAYFEDRHGKKRTLKGSIELSRI
KCVEIVKSDISIPCHYKYPFQVVHDNYLLYVFAPDRESRQRWVLALKEETRNNNSLVPKY HPNFWMDGKWRCCSQLEKLATGCAQYDPTKNASKKPLPPTPEDNRRPLWEPEETVVIALY DYQTNDPQELALRRNEEYCLLDSSEIHWWRVQDRNGHEGYVPSSYLVEKSPNNLETYEWY NKSISRDKAEKLLLDTGKEGAFMVRDSRTAGTYTVSVFTKAVVSENNPCIKHYHIKETND NPKRYYVAEKYVFDSIPLLINYHQHNGGGLVTRLRYPVCFGRQKAPVTAGLRYGKWVIDP SELTFVQEIGSGQFGLVHLGYWLNKDKVAIKTIREGAMSEEDFIEEAEVMMKLSHPKLVQ LYGVCLEQAPICLVFEFMEHGCLSDYLRTQRGLFAAETLLGMCLDVCEGMAYLEEACVIH RDLAARNCLVGENQVIKVSDFGMTRFVLDDQYTSSTGTKFPVKWASPEVFSFSRYSSKSD VWSFGVLMWEVFSEGKIPYENRSNSEVVEDISTGFRLYKPRLASTHVYQIMNHCWKERPE DRPAFSRLLRQLAEIAESGL |
||||
Drugs and Mode of Action | |||||
Pathways | |||||
KEGG Pathway | Chemokine signaling pathway | ||||
T cell receptor signaling pathway | |||||
Leukocyte transendothelial migration | |||||
NetPath Pathway | IL2 Signaling Pathway | ||||
Pathway Interaction Database | Fc-epsilon receptor I signaling in mast cells | ||||
TCR signaling in na& | |||||
#xef | |||||
ve CD4+ T cells | |||||
Class I PI3K signaling events | |||||
Reactome | Generation of second messenger molecules | ||||
FCERI mediated Ca+2 mobilization | |||||
WikiPathways | TCR Signaling Pathway | ||||
T-Cell Receptor and Co-stimulatory Signaling | |||||
TCR signaling | |||||
References | |||||
Ref 531363 | Optimisation of ITK inhibitors through successive iterative design cycles. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1852-6. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.