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Protein kinase C alpha (PKC-α) mRNA is the messenger RNA transcript of the PRKCA gene, which encodes a member of the classical PKC subfamily of serine/threonine kinases (UniProt P17252). This molecule serves as the template for the synthesis of the PKC-α protein, a key mediator in signal transduction pathways involved in cell proliferation, differentiation, and apoptosis (PubMed: 10491089). In many human cancers, including lung, breast, and colorectal cancer, PKC-α is frequently overexpressed, contributing to tumor progression and resistance to therapy (PubMed: 11595713). Consequently, PKC-α mRNA has been utilized as a therapeutic target for antisense oligonucleotides (ASOs), such as Aprinocarsen (ISIS 3521). These ASOs are designed to bind specifically to the mRNA sequence, leading to its degradation via RNase H or preventing translation, thereby reducing the levels of the oncogenic PKC-α protein (PubMed: 15150568). While early clinical trials explored these inhibitors as potential anti-cancer agents, challenges in delivery and achieving significant clinical benefit have limited their widespread adoption (PubMed: 11894177).
Antisense inhibition via RNase H-mediated cleavage of mRNA
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