Target intelligence / Profile preview

Epidermal growth factor receptor mRNA (EGFR mRNA)

Target
EGFR mRNA
Molecular classification
Nucleic acid, Messenger RNA, Oncogene transcript
01

Overview

Epidermal growth factor receptor (EGFR) mRNA is the messenger RNA transcript encoded by the EGFR gene, which serves as the essential template for the synthesis of the EGFR protein, a member of the ErbB family of receptor tyrosine kinases (Source: NCBI Gene ID 1956). The translation of this mRNA results in a transmembrane protein that regulates critical cellular processes including proliferation, differentiation, and survival through the MAPK, PI3K/Akt, and STAT pathways (Source: UniProt P00533). In various malignancies, such as non-small cell lung cancer and glioblastoma, EGFR mRNA is frequently overexpressed or mutated, driving oncogenic signaling and tumor progression (Source: PubMed PMID: 25223563). Therapeutic targeting of the mRNA transcript using antisense oligonucleotides (ASOs) or small interfering RNAs (siRNAs) aims to silence gene expression at the pre-translational level, potentially bypassing resistance mechanisms that affect small molecule inhibitors or monoclonal antibodies (Source: Nature Reviews Drug Discovery, 2017). By degrading the mRNA, these therapies can reduce the total cellular pool of both wild-type and mutant EGFR proteins, offering a comprehensive approach to inhibiting this well-validated oncogenic driver (Source: ClinicalTrials.gov NCT00005851).

Other names
ERBB1 mRNAHER1 mRNAPIG61 mRNAEpidermal growth factor receptor transcriptProto-oncogene c-ErbB-1 mRNA
02

Mechanism of action

Antisense inhibition and RNA interference (RNAi) leading to RNase H-mediated cleavage or RISC-mediated degradation of the mRNA transcript, thereby preventing translation into the EGFR protein.

03

Biological functions

Protein synthesis templateRegulation of cell growthSignal transductionCell proliferationCell survival
04

Disease associations

Non-small cell lung cancerGlioblastoma multiformeColorectal cancerHead and neck squamous cell carcinomaPancreatic cancer
05

Safety considerations

Off-target silencing of related ErbB family membersSystemic delivery challenges to solid tumorsActivation of the innate immune system (TLR7/8 signaling)Potential epithelial toxicity (skin rash, diarrhea) due to suppression of wild-type EGFR
06

Interacting drugs

GTI-2501 (Antisense oligonucleotide)

2 more in the full profile.

07

Biomarkers

EGFR mRNA expression levelsEGFR gene amplificationEGFRvIII mutation statusT790M mutation status

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