PRKCB
PRKCB (Protein kinase C beta 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, an oncogene driver and a biomarker, and an approved or late-stage drug is recorded against it. Tied to Leukaemia, Myeloproliferative neoplasms, Head and neck squamous cell carcinoma and 5 more.
Overview
Calcium-activated, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase involved in various cellular processes such as regulation of the B-cell receptor (BCR) signalosome, oxidative stress-induced apoptosis, androgen receptor-dependent transcription regulation, insulin signalling and endothelial cells proliferation. Plays a key role in B-cell activation by regulating BCR-induced NF-kappa-B activation. Mediates the activation of the canonical NF-kappa-B pathway (NFKB1) by direct phosphorylation of CARD11/CARMA1 at 'Ser-559', 'Ser-644' and 'Ser-652'.
CIViC holds 3 clinical evidence items and 0 assertions across 2 variants. Open Targets scores its association with cancer at 0.66 (direct and indirect evidence; datatypes literature 0.86, genetic association 0.00, somatic mutation 0.45, clinical 0.92). IntOGen calls it a driver in 4 cohorts (4 activating, 0 loss-of-function), covering Diffuse Large B-Cell Lymphoma, NOS, Head and Neck Squamous Cell Carcinoma, Prostate Adenocarcinoma, Stomach Adenocarcinoma.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · PRKCB (Protein kinase C beta 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, an oncogene driver and a biomarker, and an approved or late-stage drug is recorded against it. Tied to Leukaemia, Myeloproliferative neoplasms, Head and neck squamous cell carcinoma and 5 more.
- 1 · What it is
PRKCB (Protein kinase C beta 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, an oncogene driver and a biomarker, and an approved or late-stage drug is recorded against it. Tied to Leukaemia, Myeloproliferative neoplasms, Head and neck squamous cell carcinoma and 5 more.
- 2 · What goes wrong in cancer
Calcium-activated, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase involved in various cellular processes such as regulation of the B-cell receptor (BCR) signalosome, oxidative stress-induced apoptosis, androgen receptor-dependent transcription regulation, insulin signalling and endothelial cells proliferation.
- 3 · How drugs use it
No product in this corpus aims at PRKCB 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:9395 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P05771 (protein name, function text, keywords and locations (REST API)); CIViC gene PRKCB (3 evidence items, 0 assertions, 2 variants; diseases: Adult T-cell Leukaemia/lymphoma, Diffuse Large B-cell Lymphoma (GraphQL API, CC0)); Open Targets ENSG00000166501 (association with cancer (MONDO_0004992) 0.66; per-cancer scores at or above 0.5: acute myeloid leukaemia 0.60, myeloproliferative neoplasm 0.60, systemic mastocytosis 0.54, leukaemia 0.65 (GraphQL API, CC0)); IntOGen PRKCB (driver in 4 cohorts (Act 4, LoF 0); Compendium_Cancer_Genes.tsv release 20240920, CC0 1.0)
Biology
Calcium-activated, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase involved in various cellular processes such as regulation of the B-cell receptor (BCR) signalosome, oxidative stress-induced apoptosis, androgen receptor-dependent transcription regulation, insulin signalling and endothelial cells proliferation. Plays a key role in B-cell activation by regulating BCR-induced NF-kappa-B activation. Mediates the activation of the canonical NF-kappa-B pathway (NFKB1) by direct phosphorylation of CARD11/CARMA1 at 'Ser-559', 'Ser-644' and 'Ser-652'. Phosphorylation induces CARD11/CARMA1 association with lipid rafts and recruitment of the BCL10-MALT1 complex as well as MAP3K7/TAK1, which then activates IKK complex, resulting in nuclear translocation and activation of NFKB1. Plays a direct role in the negative feedback regulation of the BCR signalling, by down-modulating BTK function via direct phosphorylation of BTK at 'Ser-180', which results in the alteration of BTK plasma membrane localisation and in turn inhibition of BTK activity. Involved in apoptosis following oxidative damage: in case of oxidative conditions, specifically phosphorylates 'Ser-36' of isoform p66Shc of SHC1, leading to mitochondrial accumulation of p66Shc, where p66Shc acts as a reactive oxygen species producer. Location: Cytoplasm; Nucleus; Membrane (UniProt). Locus 16p12.2-p12.1 (HGNC).
- Leukaemia: Open Targets association 0.65 with leukaemia (MONDO_0005059)
- Myeloproliferative neoplasms: Open Targets association 0.60 with myeloproliferative neoplasm (MONDO_0020076)
- Head and neck squamous cell carcinoma: IntOGen driver in 1 cohort (HNSC)
- Prostate cancer: IntOGen driver in 1 cohort (PRAD)
- Gastric & gastro-oesophageal junction cancer: IntOGen driver in 1 cohort (STAD)
- Systemic mastocytosis: Open Targets association 0.54 with systemic mastocytosis (MONDO_0016586)
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; IntOGen calls it an activating (Act) driver in 4 cohorts; CIViC holds 3 clinical evidence items on its variants. Evidence tier "approved-drug" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
- Diseases the sources name that have no OnCo cancer page yet, so they are not linked: Adult T-cell Leukaemia/lymphoma.
Latest papers
topQuery for this target: (TITLE:"PRKCB" OR ABSTRACT:"PRKCB" OR TITLE:"protein kinase C beta" OR ABSTRACT:"protein kinase C beta" OR TITLE:"Protein kinase C beta type" OR ABSTRACT:"Protein kinase C beta type" OR TITLE:"PKCβ" OR ABSTRACT:"PKCβ" OR TITLE:"PRKCB2" OR ABSTRACT:"PRKCB2" OR TITLE:"PRKCB1" OR ABSTRACT:"PRKCB1") 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 PRKCB, not a curated reading list.
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