Target intelligence / Profile preview

PTPRE antisense RNA 1 (PTPRE-AS1)

Target
PTPRE-AS1
Molecular classification
Long noncoding RNA (lncRNA), Other
01

Overview

PTPRE antisense RNA 1 (PTPRE-AS1) is a long noncoding RNA (lncRNA) located antisense to the protein-coding gene PTPRE (receptor-type tyrosine-protein phosphatase epsilon). It is selectively upregulated in IL-4–stimulated macrophages and functions as a negative regulator of M2 macrophage activation by enhancing the expression of PTPRE through epigenetic mechanisms involving recruitment of the WDR5 histone methyltransferase complex and trimethylation of H3K4 at the PTPRE promoter. PTPRE-AS1 deficiency leads to increased M2 macrophage polarization and related inflammation, while also modulating susceptibility to allergic disease and colitis. Its expression and functional effects implicate it as an important regulator of inflammatory responses, but not as a conventional therapeutic target like a receptor, enzyme, or transporter[1][2][3].

02

Mechanism of action

Epigenetic modulation via binding to WDR5, facilitating H3K4me3 at the PTPRE promoter, which enhances PTPRE expression and impacts downstream MAPK/ERK signaling in macrophages[1][2][3]

03

Biological functions

Regulation of macrophage activation (specifically, inhibition of IL-4–induced M2 macrophage activation)Epigenetic regulation (chromatin remodeling via recruitment of WDR5)Regulation of cell proliferation and apoptosis in macrophagesImmunomodulation
04

Disease associations

InflammationAllergic diseases (e.g., asthma, pulmonary allergic inflammation)Colitis (intestinal inflammation)Potential involvement in cancer, based on lncRNA function in macrophage polarization[3]
05

Safety considerations

Potential risk in broadly targeting lncRNAs for therapy due to pleiotropic effects and widespread chromatin regulation[1][3]
06

Biomarkers

PTPRE-AS1 expression in peripheral blood mononuclear cells (PBMCs), noted as lower in patients with allergic asthma compared to healthy controls[1][2]

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