Protein kinase C (PKC) isoforms (PKC)

The Protein Kinase C (PKC) family comprises a group of serine/threonine kinases that are essential mediators of intracellular signal transduction (UniProt, 2024). These enzymes are categorized into three subfamilies—conventional, novel, and atypical—based on their activation requirements for calcium and diacylglycerol (StatPearls, 2023). PKCs are involved in regulating a wide array of cellular functions, including proliferation, differentiation, and apoptosis (PubMed, 2022). Their dysregulation is a hallmark of several diseases, most notably cancer, where they can act as either oncoproteins or tumor suppressors depending on the context and isoform (NIH, 2023). Therapeutic targeting of PKCs has been explored for conditions like diabetic retinopathy and various malignancies, though clinical success has been limited by the difficulty of achieving isoform-specific inhibition and the resulting systemic toxicity (Nature Reviews Drug Discovery, 2021).

Other names

Protein kinase C familyPRKCSerine/threonine-protein kinase CPKCs

Inhibition of the kinase catalytic domain through ATP-competitive binding or modulation of the regulatory domain via diacylglycerol (DAG) binding sites (StatPearls, 2023; Nature Reviews Drug Discovery, 2021).