PRKCZ
PRKCZ (Protein kinase C zeta 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- and diacylglycerol-independent serine/threonine-protein kinase that functions in phosphatidylinositol 3-kinase (PI3K) pathway and mitogen-activated protein (MAP) kinase cascade, and is involved in NF-kappa-B activation, mitogenic signalling, cell proliferation, cell polarity, inflammatory response and maintenance of long-term potentiation (LTP). Upon lipopolysaccharide (LPS) treatment in macrophages, or following mitogenic stimuli, functions downstream of PI3K to activate MAP2K1/MEK1-MAPK1/ERK2 signalling cascade independently of RAF1 activation. Required for insulin-dependent activation of AKT3, but may function as an adapter rather than a direct activator.
Open Targets scores its association with cancer at 0.64 (direct and indirect evidence; datatypes literature 0.93, animal model 0.32, genetic association 0.37, 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 · PRKCZ (Protein kinase C zeta 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
PRKCZ (Protein kinase C zeta 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- and diacylglycerol-independent serine/threonine-protein kinase that functions in phosphatidylinositol 3-kinase (PI3K) pathway and mitogen-activated protein (MAP) kinase cascade, and is involved in NF-kappa-B activation, mitogenic signalling, cell proliferation, cell polarity, inflammatory response and maintenance of long-term potentiation (LTP).
- 3 · How drugs use it
No product in this corpus aims at PRKCZ 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:9412 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt Q05513 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000067606 (association with cancer (MONDO_0004992) 0.64; 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- and diacylglycerol-independent serine/threonine-protein kinase that functions in phosphatidylinositol 3-kinase (PI3K) pathway and mitogen-activated protein (MAP) kinase cascade, and is involved in NF-kappa-B activation, mitogenic signalling, cell proliferation, cell polarity, inflammatory response and maintenance of long-term potentiation (LTP). Upon lipopolysaccharide (LPS) treatment in macrophages, or following mitogenic stimuli, functions downstream of PI3K to activate MAP2K1/MEK1-MAPK1/ERK2 signalling cascade independently of RAF1 activation. Required for insulin-dependent activation of AKT3, but may function as an adapter rather than a direct activator. Upon insulin treatment may act as a downstream effector of PI3K and contribute to the activation of translocation of the glucose transporter SLC2A4/GLUT4 and subsequent glucose transport in adipocytes. In EGF-induced cells, binds and activates MAP2K5/MEK5-MAPK7/ERK5 independently of its kinase activity and can activate JUN promoter through MEF2C. Through binding with SQSTM1/p62, functions in interleukin-1 signalling and activation of NF-kappa-B with the specific adapters RIPK1 and TRAF6. Location: Cytoplasm; Endosome; Cell junction; Membrane (UniProt). Locus 1p36.33 (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:"PRKCZ" OR ABSTRACT:"PRKCZ" OR TITLE:"protein kinase C zeta" OR ABSTRACT:"protein kinase C zeta" OR TITLE:"Protein kinase C zeta type" OR ABSTRACT:"Protein kinase C zeta type" OR TITLE:"PKC2" OR ABSTRACT:"PKC2") 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 PRKCZ, not a curated reading list.
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