Target intelligence / Profile preview

Protein kinase C alpha mRNA (PRKCA mRNA) (PRKCA mRNA)

Target
PRKCA mRNA
Molecular classification
Nucleic acid, Messenger RNA (mRNA)
01

Overview

Protein kinase C alpha (PKC-alpha) mRNA is the messenger RNA transcript encoded by the PRKCA gene (NCBI Gene: 5578), serving as the template for the synthesis of the PKC-alpha protein (UniProt: P17252). PKC-alpha is a member of the classical protein kinase C family and plays a critical role in diverse cellular processes, including signal transduction, cell proliferation, and apoptosis (PubMed: 15660110). In many human cancers, PKC-alpha is overexpressed or overactive, contributing to tumor growth, survival, and resistance to chemotherapy (PubMed: 11544000). Consequently, the mRNA itself has been utilized as a therapeutic target for antisense oligonucleotides (ASOs) designed to bind specifically to the transcript and trigger its degradation via RNase H (PubMed: 10914719). The most notable drug developed for this target is Aprinocarsen (ISIS 3521), which aimed to reduce PKC-alpha protein levels in patients with advanced malignancies like non-small cell lung cancer (PubMed: 12114418). While this approach demonstrated the feasibility of targeting mRNA to modulate signaling pathways, clinical success has been limited by challenges in delivery and achieving sufficient therapeutic efficacy in late-stage trials (PubMed: 15150442).

Other names
PKC-alpha mRNAPRKCA transcriptProtein kinase C alpha antisense targetPRKCA messenger RNA
02

Mechanism of action

Antisense oligonucleotide-mediated degradation of mRNA via RNase H, leading to the inhibition of Protein kinase C alpha protein synthesis (PubMed: 10914719).

03

Biological functions

Translation template for Protein kinase C alphaSignal transductionCell proliferationApoptosis regulationCell differentiation (UniProt: P17252)
04

Disease associations

Cancer (Non-small cell lung cancer, Ovarian cancer, Colorectal cancer, Breast cancer)Inflammation (PubMed: 15150442)
05

Safety considerations

ThrombocytopeniaFeverFatigueNauseaOff-target hybridization effects associated with phosphorothioate oligonucleotides (PubMed: 12114418)
06

Interacting drugs

Aprinocarsen (ISIS 3521, Affinitak) (PubChem CID: 16131410)
07

Biomarkers

PKC-alpha protein expression levelsPRKCA mRNA expression levels (PubMed: 12114418)

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