Protein kinase C is a family of signalling enzymes; the AML drug midostaurin started life as a PKC inhibitor and still hits the family alongside FLT3.
The protein kinase C family (PRKCA and its relatives) transmits signals from calcium and diacylglycerol to growth, survival and secretion pathways. Midostaurin (PKC412) was developed as a PKC inhibitor and gained approval in FLT3-mutant acute myeloid leukaemia and systemic mastocytosis through its FLT3 and KIT activity; PKC remains among its listed targets. PKC-beta inhibitors such as enzastaurin were tested in lymphoma without success.
In plain words · Protein kinase C is a family of signalling enzymes; the AML drug midostaurin started life as a PKC inhibitor and still hits the family alongside FLT3.
Protein kinase C is a family of signalling enzymes; the AML drug midostaurin started life as a PKC inhibitor and still hits the family alongside FLT3.
Serine/threonine kinases in conventional, novel and atypical subfamilies; PKC-alpha also drives resistance and vascular permeability signalling.
No product in this corpus aims at Protein kinase C family (PKC) yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Tumour-associated overexpression: HPA finds the RNA tissue enhanced in normal brain, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA PRKCA: RNA tissue enhanced (brain 33 nTPM); high antibody staining in 3 normal tissues. Distribution: 1 cancer family in the corpus carries a prevalence row, label threshold or catalogue link for it (Leukaemia); Open Targets associates it with 1 specific cancer type at or above 0.5 (acute myeloid leukemia). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas PRKCA tissue; Human Protein Atlas PRKCA pathology; Open Targets ENSG00000154229 associations
First described 1990. Earliest sequence paper UniProt cites for the protein: Finkenzeller et al, Nucleic Acids Res, 1990, "Sequence of human protein kinase C alpha". Source.
Serine/threonine kinases in conventional, novel and atypical subfamilies; PKC-alpha also drives resistance and vascular permeability signalling.
RNA: tissue enhanced (brain 33 nTPM), detected in many normal tissues.
Medium: Appendix, Bronchus, Caudate, Cerebral cortex, Colon, Endometrium, Epididymis, Esophagus.
No cancer stained high; medium in carcinoid, endometrial cancer, glioma, lymphoma.
HPA PRKCA tissue · HPA PRKCA pathology · HPA protein class: FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Metastatic cancer | all% | Signalling protein present in most cells (protein kinase C family); drugs act on the pathway rather than on a mutation that selects patients, so no prevalence applies. |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Query for this target: (TITLE:"Protein kinase C family" OR ABSTRACT:"Protein kinase C family" OR TITLE:"PKC" OR ABSTRACT:"PKC" OR TITLE:"PRKCA" OR ABSTRACT:"PRKCA") 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 Protein kinase C family (PKC), not a curated reading list.
Shares FLT3, Acute myeloid leukaemia.
Shares Midostaurin, FLT3, Acute myeloid leukaemia.
Shares FLT3, Acute myeloid leukaemia.
Shares Midostaurin, FLT3, Acute myeloid leukaemia.
Shares FLT3, Acute myeloid leukaemia.
Shares Midostaurin, FLT3, Acute myeloid leukaemia.
Shares FLT3, Acute myeloid leukaemia.
Shares FLT3, Acute myeloid leukaemia.