Target intelligence / Profile preview

EZR antisense RNA 1 (non-protein coding) (EZR-AS1)

Target
EZR-AS1
Molecular classification
Long non-coding RNA (lncRNA), Natural antisense transcript, Other
01

Overview

EZR antisense RNA 1 (EZR-AS1) is a long non-coding RNA transcribed in the antisense direction at the EZR gene locus and is primarily localized in the nucleus[1][2][3][5]. EZR-AS1 serves as an epigenetic regulator of gene expression, especially by upregulating the transcription of the EZR gene—linked to cell migration and cancer progression—through direct interactions with RNA polymerase II and recruitment of the histone methyltransferase SMYD3, thereby promoting H3K4 trimethylation at the EZR promoter[1][2]. It additionally regulates key cancer-related pathways such as PI3K/AKT and TGF-β[3][5]. Elevated expression of EZR-AS1 is associated with increased proliferation, migration, invasion, and epithelial–mesenchymal transition in various cancer cells, highlighting its potential as a therapeutic target and biomarker for several cancer types, including esophageal squamous cell carcinoma, colorectal cancer, and cutaneous squamous cell carcinoma[1][3][5][4][6]. There are no approved drugs or therapeutics directly targeting EZR-AS1 at this time.

Other names
EZR-AS1EZR antisense RNA 1 (non-protein coding)Long non-coding RNA EZR-AS1lncRNA EZR-AS1
02

Mechanism of action

Acts as scaffold for chromatin modifiers (e.g., recruits SMYD3 methyltransferase to specific promoter regions); Forms complexes with RNA polymerase II to activate transcription of the EZR gene; Modulates PI3K/AKT and TGF-β signaling pathways in cancer cells[1][3][5]

03

Biological functions

Regulation of gene expressionModulation of chromatin structurePromotion of cell migrationRegulation of cell proliferationRegulation of epithelial–mesenchymal transition (EMT)Inhibition of apoptosis
04

Disease associations

CancerSpecifically, esophageal squamous cell carcinoma (ESCC)Colorectal cancerCutaneous squamous cell carcinoma (cSCC)Other (various solid tumors; evidence in multiple cancers)
05

Safety considerations

Targeting lncRNAs may raise concerns about off-target genetic regulation and unintended modulation of gene networks[1]
06

Interacting drugs

None known or validated
07

Biomarkers

Elevated EZR-AS1 expression is a potential biomarker for tumor aggressiveness (migration, invasion) in ESCC, colorectal cancer, and cSCC[1][3][5]

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