Target intelligence / Profile preview

Protein kinase D3 (PRKD3) (PRKD3)

Target
PRKD3
Molecular classification
Enzyme, Serine/threonine-protein kinase, Protein kinase D family
01

Overview

Protein kinase D3 (PKD3), also known as protein kinase C nu (PRKCN), is a serine/threonine kinase belonging to the protein kinase D family (UniProt Q9P2K8). It is distinct from the classical protein kinase C (PKC) isoforms, although it is activated downstream of PKC and by diacylglycerol (DAG) (PubMed: 18483241). PKD3 plays a critical role in various cellular processes, including Golgi-to-plasma membrane vesicle trafficking, cell proliferation, and survival signaling (HGNC: 9401). In the context of oncology, PKD3 is frequently overexpressed in several malignancies, such as prostate and breast cancers, where it promotes tumor growth and metastasis (PubMed: 20647541). Consequently, it is considered a potential therapeutic target, with several small-molecule inhibitors like CRT0066101 currently being explored in preclinical studies to modulate its activity (PubMed: 23903774). The target is also implicated in cardiovascular health, specifically in cardiac hypertrophy and remodeling (PubMed: 21566104). Research continues to focus on developing selective inhibitors to minimize off-target effects associated with pan-PKD inhibition.

Other names
PRKCNProtein kinase C nuPKC-nuEPK2nPKC-nu
02

Mechanism of action

Inhibition of serine/threonine kinase activity through ATP-competitive binding.

03

Biological functions

Signal transductionCell proliferationVesicular traffickingCell survivalAngiogenesis
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Disease associations

CancerProstate cancerBreast cancerCardiovascular disease
05

Safety considerations

Potential cardiotoxicityOff-target kinase inhibitionDisruption of normal Golgi trafficking
06

Interacting drugs

CRT0066101

3 more in the full profile.

07

Biomarkers

Phospho-PRKD3PRKD3 mRNA expressionPRKD3 protein levels

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