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Target intelligence / Profile preview
Protein Kinase C-iota (PKCι)
- Target
- PKCι
- Molecular classification
- Enzyme, Serine/threonine-protein kinase, Atypical protein kinase C isoform
01
Overview
Protein kinase C-iota (PKCι) is a member of the protein kinase C (PKC) family of serine/threonine kinases. It is encoded by the PRKCI gene and classified as an atypical PKC isoform. PKCι is calcium-independent and phospholipid-dependent, but it is not activated by phorbol esters or diacylglycerol. PKCι plays diverse roles in cellular signaling and has been implicated as a bona fide human oncogene, particularly in colon cancer, lung cancer, and alveolar rhabdomyosarcoma. It is involved in apoptosis regulation, cell polarity, tight junctions, and directional migration of epithelial cells. PKCι is a therapeutic target under clinical investigation.
- Other names
- Protein kinase C iota typePKC iotaPRKCI
02
Mechanism of action
PKCι inhibitors are under clinical investigation for cancer therapy. The mechanism involves blocking the kinase activity of PKCι, thereby inhibiting its downstream signaling pathways that promote cell growth, survival, and invasion.
03
Biological functions
Apoptosis regulationCell polarityTight junction formationEpithelial barrier integrityWound healingCell migrationRAC1/ERK signalingMicrotubule dynamics
04
Disease associations
CancerColon cancerLung cancerAlveolar rhabdomyosarcoma
05
Safety considerations
Potential for off-target effects due to the broad expression of atypical PKCs.Development of resistance to PKCι inhibitors may occur.
06
Biomarkers
PKCι overexpression in tumor tissueTFF3 expression
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