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Long intergenic non-protein coding RNA 114 (LINC00114) is a long non-coding RNA molecule expressed in both the cytoplasm and nucleus. Highly upregulated in colorectal cancer, it acts as an oncogenic factor by suppressing the tumor suppressor miRNA miR-133b, predominantly via recruitment of the methyltransferase EZH2 and DNMT1, which leads to methylation-induced silencing of miR-133b's promoter. This, in turn, derepresses NUP214, a protein promoting cancer cell proliferation. Experimental knockdown of LINC00114 inhibits colorectal cancer cell growth in vitro and in vivo, suggesting that LINC00114 is both a mechanistic driver of cancer progression and a promising diagnostic and therapeutic target in oncology.
Drugs such as RG108 act by inhibiting DNA methyltransferase, which can counteract the LINC00114-driven epigenetic silencing of miR-133b promoter, restoring tumor suppressor miRNA activity
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