Target intelligence / Profile preview

Fibroblast growth factor receptor 1 messenger RNA (FGFR1 mRNA) (FGFR1 mRNA)

Target
FGFR1 mRNA
Molecular classification
Nucleic acid, Messenger RNA
01

Overview

Fibroblast growth factor receptor 1 (FGFR1) messenger RNA (mRNA) is the transcript produced from the FGFR1 gene, serving as the essential template for the synthesis of the FGFR1 protein, a critical receptor tyrosine kinase (NCBI Gene: 2260). This mRNA plays a vital role in cellular signaling pathways that govern proliferation, survival, and embryonic development (UniProt: P11362). In various cancers, such as non-small cell lung cancer and breast cancer, FGFR1 mRNA is frequently overexpressed due to gene amplification, acting as a potent oncogenic driver (PubMed: 23539236). While most current clinical therapies utilize small-molecule inhibitors to target the FGFR1 protein, the mRNA itself is an attractive target for gene-silencing approaches. Therapeutic strategies such as antisense oligonucleotides (ASOs) and small interfering RNAs (siRNAs) are designed to bind specifically to the FGFR1 mRNA, leading to its degradation or the inhibition of translation (PubMed: 21602828). By preventing the production of the FGFR1 protein at the source, these RNA-targeted therapies aim to provide a more precise intervention and potentially overcome resistance mechanisms associated with traditional kinase inhibitors.

Other names
FGFR1 transcriptCD331 mRNABFGFR mRNAFLT2 mRNAHBGFR mRNAFibroblast growth factor receptor 1 transcript
02

Mechanism of action

Targeted degradation of the mRNA transcript via RNase H-mediated cleavage (for antisense oligonucleotides) or the RNA-induced silencing complex (for siRNAs), which prevents the translation of the FGFR1 protein.

03

Biological functions

Protein synthesis templateRegulation of cell proliferationRegulation of angiogenesisEmbryonic developmentRegulation of cell survival
04

Disease associations

Non-small cell lung cancerBreast cancerSquamous cell carcinomaKallmann syndromePfeiffer syndromeOsteoglophonic dysplasia
05

Safety considerations

Off-target hybridization with other FGFR isoformsInduction of innate immune responses to nucleic acidsDelivery challenges to solid tumor tissuesPotential hepatotoxicity associated with oligonucleotide therapy
06

Interacting drugs

Experimental FGFR1-targeting antisense oligonucleotides

1 more in the full profile.

07

Biomarkers

FGFR1 mRNA expression levels (via RT-qPCR or RNA-seq)FGFR1 gene amplification (via FISH)FGFR1/CEP8 ratio

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