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C5orf66 antisense RNA 1 (PITX1-AS1)

Target
PITX1-AS1
Molecular classification
Long non-coding RNA (lncRNA), Antisense RNA, Genic lncRNA (sense-type; classified based on its location and transcription direction relative to coding gene PITX1)
01

Overview

C5orf66 antisense RNA 1 (PITX1-AS1) is a long non-coding RNA located near and transcribed in the same direction as PITX1, a critical transcription factor involved in pituitary development and tumor suppression[1][4]. PITX1-AS1 is highly expressed in pituitary and esophageal tissues, where it exerts tumor-suppressive effects by regulating cell viability and invasion. Downregulation or loss of PITX1-AS1, often via epigenetic methylation, has been associated with tumor progression in pituitary adenomas, esophageal squamous cell carcinoma, head and neck squamous cell carcinoma, and other cancers[1][4]. Its expression correlates with tumor aggressiveness and patient prognosis, establishing its role as a promising biomarker and potential therapeutic target in oncology. Mechanistically, PITX1-AS1 may act both through direct cis-regulation of PITX1 and more distantly via impact on the Ras signaling pathway, crucial for controlling cell proliferation[1][4][6].

Other names
C5orf66-AS1PITX1-AS1EpistlincRNA C5orf66-AS1
02

Mechanism of action

Epigenetic modulation (demethylating agents could restore PITX1-AS1 expression) Inhibitors of Ras/ERK pathway, e.g., sorafenib, are postulated to be more effective in cases where PITX1-AS1/PITX1 regulation is lost

03

Biological functions

Transcriptional regulation of nearby genes (cis-regulation), notably PITX1Post-transcriptional regulation of gene expression (inferred from antisense RNA properties)Tumor suppression: inhibits cell proliferation and invasion, especially in pituitary adenomas and esophageal squamous cell carcinomaEpigenetic regulation (DNA methylation status of C5orf66-AS1 and PITX1)
04

Disease associations

Cancer (pituitary adenomas, head and neck squamous cell carcinoma (HNSCC), esophageal, gastric, colon, bladder cancer)Tumor progression and invasionPrognostic biomarker in HNSCC and potentially other tumor types
05

Safety considerations

No specific safety concerns listed for PITX1-AS1 as a therapeutic target; challenges primarily involve specificity and off-target effects typical of lncRNA-targeting therapeutics
06

Interacting drugs

sorafenib
07

Biomarkers

DNA methylation status of C5orf66-AS1 (PITX1-AS1) and PITX1, especially in HNSCC

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