PRKCQ
PRKCQ (Protein kinase C theta type) 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 Leukaemia, Myeloproliferative neoplasms, Systemic mastocytosis and 1 more.
Overview
Calcium-independent, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that mediates non-redundant functions in T-cell receptor (TCR) signalling, including T-cells activation, proliferation, differentiation and survival, by mediating activation of multiple transcription factors such as NF-kappa-B, JUN, NFATC1 and NFATC2. In TCR-CD3/CD28-co-stimulated T-cells, is required for the activation of NF-kappa-B and JUN, which in turn are essential for IL2 production, and participates in the calcium-dependent NFATC1 and NFATC2 transactivation. Mediates the activation of the canonical NF-kappa-B pathway (NFKB1) by direct phosphorylation of CARD11 on several serine residues, inducing CARD11 association with lipid rafts and recruitment of the BCL10-MALT1 complex, which then activates IKK complex, resulting in nuclear translocation and activation of NFKB1.
Open Targets scores its association with cancer at 0.61 (direct and indirect evidence; datatypes literature 0.93, animal model 0.80, genetic association 0.17, clinical 0.92).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · PRKCQ (Protein kinase C theta type) 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 Leukaemia, Myeloproliferative neoplasms, Systemic mastocytosis and 1 more.
- 1 · What it is
PRKCQ (Protein kinase C theta type) 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 Leukaemia, Myeloproliferative neoplasms, Systemic mastocytosis and 1 more.
- 2 · What goes wrong in cancer
Calcium-independent, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that mediates non-redundant functions in T-cell receptor (TCR) signalling, including T-cells activation, proliferation, differentiation and survival, by mediating activation of multiple transcription factors such as NF-kappa-B, JUN, NFATC1 and NFATC2.
- 3 · How drugs use it
No product in this corpus aims at PRKCQ 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:9410 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt Q04759 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000065675 (association with cancer (MONDO_0004992) 0.61; per-cancer scores at or above 0.5: acute myeloid leukaemia 0.56, myeloproliferative neoplasm 0.56, systemic mastocytosis 0.54, leukaemia 0.57 (GraphQL API, CC0))
Biology
Calcium-independent, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that mediates non-redundant functions in T-cell receptor (TCR) signalling, including T-cells activation, proliferation, differentiation and survival, by mediating activation of multiple transcription factors such as NF-kappa-B, JUN, NFATC1 and NFATC2. In TCR-CD3/CD28-co-stimulated T-cells, is required for the activation of NF-kappa-B and JUN, which in turn are essential for IL2 production, and participates in the calcium-dependent NFATC1 and NFATC2 transactivation. Mediates the activation of the canonical NF-kappa-B pathway (NFKB1) by direct phosphorylation of CARD11 on several serine residues, inducing CARD11 association with lipid rafts and recruitment of the BCL10-MALT1 complex, which then activates IKK complex, resulting in nuclear translocation and activation of NFKB1. May also play an indirect role in activation of the non-canonical NF-kappa-B (NFKB2) pathway. In the signalling pathway leading to JUN activation, acts by phosphorylating the mediator STK39/SPAK and may not act through MAP kinases signalling. Plays a critical role in TCR/CD28-induced NFATC1 and NFATC2 transactivation by participating in the regulation of reduced inositol 1,4,5-trisphosphate generation and intracellular calcium mobilisation. Location: Cytoplasm; Cell membrane (UniProt). Locus 10p15.1 (HGNC).
- Leukaemia: Open Targets association 0.57 with leukaemia (MONDO_0005059)
- Myeloproliferative neoplasms: Open Targets association 0.56 with myeloproliferative neoplasm (MONDO_0020076)
- Systemic mastocytosis: Open Targets association 0.54 with systemic mastocytosis (MONDO_0016586)
- Acute myeloid leukaemia: Open Targets association 0.56 with acute myeloid leukaemia (MONDO_0018874)
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 0.94. 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:"PRKCQ" OR ABSTRACT:"PRKCQ" OR TITLE:"protein kinase C theta" OR ABSTRACT:"protein kinase C theta" OR TITLE:"Protein kinase C theta type" OR ABSTRACT:"Protein kinase C theta type") 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 PRKCQ, not a curated reading list.
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