PRKCG
PRKCG (Protein kinase C gamma 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-activated, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that plays diverse roles in neuronal cells and eye tissues, such as regulation of the neuronal receptors GRIA4/GLUR4 and GRIN1/NMDAR1, modulation of receptors and neuronal functions related to sensitivity to opiates, pain and alcohol, mediation of synaptic function and cell survival after ischemia, and inhibition of gap junction activity after oxidative stress. Binds and phosphorylates GRIA4/GLUR4 glutamate receptor and regulates its function by increasing plasma membrane-associated GRIA4 expression. In primary cerebellar neurons treated with the agonist 3,5-dihyidroxyphenylglycine, functions downstream of the metabotropic glutamate receptor GRM5/MGLUR5 and phosphorylates GRIN1/NMDAR1 receptor which plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning.
Open Targets scores its association with cancer at 0.59 (direct and indirect evidence; datatypes literature 0.89, animal model 0.47, genetic association 0.00, 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 · PRKCG (Protein kinase C gamma 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
PRKCG (Protein kinase C gamma 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-activated, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that plays diverse roles in neuronal cells and eye tissues, such as regulation of the neuronal receptors GRIA4/GLUR4 and GRIN1/NMDAR1, modulation of receptors and neuronal functions related to sensitivity to opiates, pain and alcohol, mediation of synaptic function and cell survival after ischemia, and inhibition of gap junction activity after oxidative stress.
- 3 · How drugs use it
No product in this corpus aims at PRKCG 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:9402 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P05129 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000126583 (association with cancer (MONDO_0004992) 0.59; 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-activated, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that plays diverse roles in neuronal cells and eye tissues, such as regulation of the neuronal receptors GRIA4/GLUR4 and GRIN1/NMDAR1, modulation of receptors and neuronal functions related to sensitivity to opiates, pain and alcohol, mediation of synaptic function and cell survival after ischemia, and inhibition of gap junction activity after oxidative stress. Binds and phosphorylates GRIA4/GLUR4 glutamate receptor and regulates its function by increasing plasma membrane-associated GRIA4 expression. In primary cerebellar neurons treated with the agonist 3,5-dihyidroxyphenylglycine, functions downstream of the metabotropic glutamate receptor GRM5/MGLUR5 and phosphorylates GRIN1/NMDAR1 receptor which plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. May be involved in the regulation of hippocampal long-term potentiation (LTP), but may be not necessary for the process of synaptic plasticity. May be involved in desensitisation of mu-type opioid receptor-mediated G protein activation in the spinal cord, and may be critical for the development and/or maintenance of morphine-induced reinforcing effects in the limbic forebrain. May modulate the functionality of mu-type-opioid receptors by participating in a signalling pathway which leads to the phosphorylation and degradation of opioid receptors. Location: Cytoplasm; Cytoplasm, perinuclear region; Cell membrane; Synapse, synaptosome (UniProt). Locus 19q13.42 (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:"PRKCG" OR ABSTRACT:"PRKCG" OR TITLE:"protein kinase C gamma" OR ABSTRACT:"protein kinase C gamma" OR TITLE:"Protein kinase C gamma type" OR ABSTRACT:"Protein kinase C gamma type" OR TITLE:"MGC57564" OR ABSTRACT:"MGC57564" OR TITLE:"PKCγ" OR ABSTRACT:"PKCγ" OR TITLE:"SCA14" OR ABSTRACT:"SCA14") 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 PRKCG, not a curated reading list.
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