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IDH1 antisense RNA 1 (IDH1-AS1)

Target
IDH1-AS1
Molecular classification
Long non-coding RNA (lncRNA), Non-protein coding RNA, Antisense RNA
01

Overview

IDH1 antisense RNA 1 (IDH1-AS1) is a cytoplasmic long non-coding RNA transcribed in proximity and antisense to the IDH1 gene. Unlike other antisense RNAs that regulate gene expression, IDH1-AS1 does not alter IDH1 mRNA or protein levels, but physically interacts with wild-type IDH1 enzyme and enhances its enzymatic activity by promoting homodimerization[4][2]. This interaction selectively increases the conversion of isocitrate to α-ketoglutarate and NADPH, thereby reducing cellular reactive oxygen species (ROS)[4]. IDH1-AS1 also links the metabolic and transcriptional activities of c-Myc and HIF1α, and participates in oncogenic processes, including sustaining the Warburg effect and regulating autophagy in cancer cells[4][2][6]. It is implicated in the development and progression of cancers such as glioma and prostate cancer, serving as a potential biomarker and therapeutic target[5][4][2][6]. However, there are no specific clinical drugs that directly target IDH1-AS1 at present.

Other names
IDH1-AS1IDH1 antisense RNA 1 (non-protein coding)IDH1 antisense RNA 1lncRNA IDH1-AS1
02

Mechanism of action

Not applicable for drugs directly targeting IDH1-AS1; for IDH1 pathway inhibition, mechanisms include modulation of IDH1 enzyme activity, alteration of metabolite production (α-ketoglutarate, NADPH), and downstream effects on gene expression and cellular metabolism

03

Biological functions

Regulation of IDH1 enzyme activityModulation of cellular metabolism (especially NADPH, α-ketoglutarate levels, and ROS)Influence on glycolysis and Warburg effect via HIF1α pathwayRegulation of autophagy in prostate cancer cells
04

Disease associations

Cancer (including glioma, prostate cancer, breast cancer)Metabolic disease (indirectly, via IDH1 regulation and metabolic effects)
05

Safety considerations

Long non-coding RNAs like IDH1-AS1 present therapeutic challenges for specificity, delivery, and off-target effectsNo specific clinical safety concerns for targeting IDH1-AS1 are listed in current literature
06

Biomarkers

Expression of IDH1-AS1 in cancer tissues as a biomarker for metabolic reprogramming and tumor progressionCellular levels of α-ketoglutarate, NADPH, ROS as indirect readouts for IDH1-AS1 function

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