Protein kinase C family (PKC)
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.
Overview
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.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
Serine/threonine kinases in conventional, novel and atypical subfamilies; PKC-alpha also drives resistance and vascular permeability signalling.
- 3 · How drugs use it
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.
External identifiers
Biology
Serine/threonine kinases in conventional, novel and atypical subfamilies; PKC-alpha also drives resistance and vascular permeability signalling.
- Ubiquitous
- Inhibited by midostaurin in AML and mastocytosis
Latest papers
topQuery 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.
Similar pages
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