ITK
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.
Overview
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).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
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.
- 3 · How drugs use it
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.
External identifiers
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))
Biology
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).
- Renal cell carcinoma: Open Targets association 0.63 with renal cell carcinoma (MONDO_0005086)
- Sarcomas: Open Targets association 0.62 with sarcoma (MONDO_0005089)
Notes
top- Written by scripts/fetch-cancer-genes.ts from CIViC, Open Targets, IntOGen, HGNC and UniProt; the function text is UniProt's, condensed and in UK spelling. Roles: Open Targets known-drug datatype score 0.97. Evidence tier "approved-drug" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery 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.
Similar pages
not linked directly; found by shared links- TargetTEC
Shares Acalabrutinib, Ibrutinib.
- TrialStudy of Acalabrutinib (ACP-196) Versus Ibrutinib in Previously Treated Participants With High Risk Chronic Lymphocytic Leukemia (CLL)
Shares Acalabrutinib, Ibrutinib.
- TrialStudy of BTK Inhibitor LOXO-305 Versus Approved BTK Inhibitor Drugs in Patients With Mantle Cell Lymphoma (MCL)
Shares Acalabrutinib, Ibrutinib.
- PairingCaution: ibrutinib in patients with cardiac risk
Shares Acalabrutinib, Ibrutinib.
- TrialBELLWAVE-011
Shares Acalabrutinib, Ibrutinib.
- InstitutionThe Ohio State University Comprehensive Cancer Center, James Cancer Hospital and Solove Research Institute
Shares Acalabrutinib, Ibrutinib, Sarcomas (soft tissue, bone, GIST).
- TermCLL-IPI (chronic lymphocytic leukaemia prognostic index)
Shares Acalabrutinib, Ibrutinib.
- TermMYD88 L265P and CXCR4 mutations
Shares Acalabrutinib, Ibrutinib.