PRKCI
PRKCI (Protein kinase C iota 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 plays a general protective role against apoptotic stimuli, is involved in NF-kappa-B activation, cell survival, differentiation and polarity, and contributes to the regulation of microtubule dynamics in the early secretory pathway. Is necessary for BCR-ABL oncogene-mediated resistance to apoptotic drug in leukaemia cells, protecting leukaemia cells against drug-induced apoptosis. In cultured neurons, prevents amyloid beta protein-induced apoptosis by interrupting cell death process at a very early step.
Open Targets scores its association with cancer at 0.67 (direct and indirect evidence; datatypes literature 0.97, genetic association 0.54, 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 · PRKCI (Protein kinase C iota 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
PRKCI (Protein kinase C iota 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 plays a general protective role against apoptotic stimuli, is involved in NF-kappa-B activation, cell survival, differentiation and polarity, and contributes to the regulation of microtubule dynamics in the early secretory pathway.
- 3 · How drugs use it
No product in this corpus aims at PRKCI 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:9404 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P41743 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000163558 (association with cancer (MONDO_0004992) 0.67; 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 plays a general protective role against apoptotic stimuli, is involved in NF-kappa-B activation, cell survival, differentiation and polarity, and contributes to the regulation of microtubule dynamics in the early secretory pathway. Is necessary for BCR-ABL oncogene-mediated resistance to apoptotic drug in leukaemia cells, protecting leukaemia cells against drug-induced apoptosis. In cultured neurons, prevents amyloid beta protein-induced apoptosis by interrupting cell death process at a very early step. In glioblastoma cells, may function downstream of phosphatidylinositol 3-kinase (PI(3)K) and PDPK1 in the promotion of cell survival by phosphorylating and inhibiting the pro-apoptotic factor BAD. Can form a protein complex in non-small cell lung cancer (NSCLC) cells with PARD6A and ECT2 and regulate ECT2 oncogenic activity by phosphorylation, which in turn promotes transformed growth and invasion. In response to nerve growth factor (NGF), acts downstream of SRC to phosphorylate and activate IRAK1, allowing the subsequent activation of NF-kappa-B and neuronal cell survival. Location: Cytoplasm; Membrane; Endosome; Nucleus (UniProt). Locus 3q26.2 (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:"PRKCI" OR ABSTRACT:"PRKCI" OR TITLE:"protein kinase C iota" OR ABSTRACT:"protein kinase C iota" OR TITLE:"Protein kinase C iota type" OR ABSTRACT:"Protein kinase C iota type" OR TITLE:"DXS1179E" OR ABSTRACT:"DXS1179E") 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 PRKCI, not a curated reading list.
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