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ITK (Tyrosine-protein kinase ITK/TSK) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Renal cell carcinoma and Sarcomas.
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.
Open Targets scores its association with cancer at 0.68 (direct and indirect evidence; datatypes clinical 0.97, literature 0.90, genetic association 0.00, somatic mutation 0.50, animal model 0.34). In OnCo, 3 product records name it (Ibrutinib, Acalabrutinib and Soquelitinib).
In plain words · ITK (Tyrosine-protein kinase ITK/TSK) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Renal cell carcinoma and Sarcomas.
ITK (Tyrosine-protein kinase ITK/TSK) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Renal cell carcinoma and Sarcomas.
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.
No product in this corpus aims at ITK yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Lineage antigen shared with normal NK-cells and T-cells and lymphoid tissue cells: HPA finds the gene tissue enriched in lymphoid tissue, and the 3 medicines aimed at it (Acalabrutinib, Ibrutinib, Soquelitinib) act on the wild-type protein, so the normal lineage is hit too. HPA ITK: RNA tissue enriched (lymphoid tissue 54 nTPM); blood lineage group enriched (NK-cells 29 nTPM, T-cells 78 nTPM); no normal tissue stained high. Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Renal cell carcinoma, Sarcomas (soft tissue, bone, GIST)); approvals of single-target medicines aimed at it also list Leukaemia, Lymphoma, not counted; Open Targets associates it with 1 specific cancer type at or above 0.5 (renal cell carcinoma). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas ITK tissue; Human Protein Atlas ITK pathology; Open Targets ENSG00000113263 associations
First described 1993. Earliest sequence paper UniProt cites for the protein: Tanaka et al, FEBS Lett, 1993, "A novel human tyrosine kinase gene inducible in T cells by interleukin 2". Source.
Sources: HGNC HGNC:6171 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt Q08881 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000113263 (association with cancer (MONDO_0004992) 0.68; per-cancer scores at or above 0.5: renal cell carcinoma 0.63, sarcoma 0.62 (GraphQL API, CC0))
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. Location: Cytoplasm; Nucleus (UniProt). Locus 5q33.3 (HGNC).
RNA: tissue enriched (lymphoid tissue 54 nTPM), detected in some normal tissues. Blood: group enriched (NK-cells 29 nTPM, T-cells 78 nTPM).
No normal tissue stained high.
No cancer sample stained medium or high.
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
Query for this target: (TITLE:"ITK" OR ABSTRACT:"ITK" OR TITLE:"IL2 inducible T cell kinase" OR ABSTRACT:"IL2 inducible T cell kinase" OR TITLE:"Tyrosine-protein kinase ITK/TSK" OR ABSTRACT:"Tyrosine-protein kinase ITK/TSK" OR TITLE:"PSCTK2" OR ABSTRACT:"PSCTK2") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about ITK, not a curated reading list.
Shares Acalabrutinib, Ibrutinib.
Shares Acalabrutinib, Ibrutinib.
Shares Acalabrutinib, Ibrutinib.
Shares Acalabrutinib, Ibrutinib.
Shares Acalabrutinib, Ibrutinib.
Shares Acalabrutinib, Ibrutinib, Sarcomas (soft tissue, bone, GIST).
Shares Acalabrutinib, Ibrutinib.
Shares Acalabrutinib, Ibrutinib.