From: HOTAIR: a potential metastatic, drug-resistant and prognostic regulator of breast cancer
Bioactive compounds/ anticancer drugs/HOTAIR inhibitor | Mechanism of action | Ref |
---|---|---|
Delphinidin (DEL) | • Inhibits 1-methyl-1-nitrosourea-induced BC in rats by upregulating miR-34a via the targeting of HOTAIR expression • Reduces the occupancy of EZH2 and histone H3 Lys27 trimethylation at the promoter site of miR-34a | [103] |
DEL-3-glucoside | • Inhibits nitrosamine and benzopyrene-induced carcinogenesis in normal breast epithelial cells by reducing the expression of HOTAIR. • Reduces the expression of HOTAIR and Akt by increasing the expression and binding of IRF1 to the of HOTAIR promoter | [104] |
Calycosin and genistein | • Reduces HOTAIR expression by reducing Akt phosphorylation in MCF-7 BC cells | [105] |
Peptide nucleic acid (PNA3) | • Reduces the invasion of BC cells by increasing the sensitivity to chemotherapy via reduction in NF-kB dependent expression of MMP9 and IL-6 | [107] |
Imatinib and lapatinib | • Synergistically reduces the expression of HOTAIR by regulating β-catenin recruitment at the promoter via interference with the LEF1/TCF4-binding site | [108] |
AC1Q3QWB (AQB) | • Enhances the expression of tumor suppressors by interfering with the recruitment of PRC2 via the disruption of the interaction between HOTAIR and EZH2 • Upregulates HOTAIR target genes especially APC2 via the suppression of Wnt/catenin signaling and the promotion of transcription via RNA pol II | [109] |
AC1NOD4Q (ADQ | • Inhibits BC metastasis by blocking HOTAIR activity via interference with the EZH2 interaction • Impairs the H3K27-dependent trimethylation of the target gene and subsequent inhibition of the Wnt/catenin pathway in an orthotopic BC model • Prevents the interaction of HOTAIR with EZH2 by binding to a specific HOTAIR domain | [110] |
Metformin (MET) | • Inhibits HOTAIR expression by affecting the methylation pattern of CpG islands in the promoter region and reverses EMT by lowering vimentin and β-catenin levels • Reduces the invasiveness and migratory potential of TNBC cells | [111] |
Aurora kinase inhibitor (CCT137690) | • Inhibits the expansion of TNBC cells by reducing HOTAIR levels via its influence on AURK and associated network proteins | [112] [113] |
Steroidal saponin (Dioscin) | • Inhibits stem-like properties and EMT in BC. | [114] |
• Reduces HOTAIR expression in gastric cancer | [115] | |
Polyphylla I | • Disrupts the interaction of HOTAIR with its upstream regulators and downstream mediators. | [116] |
• Inhibits the cell cycle and induces apoptosis in BC | [117] | |
Berberine | • Inhibits BC and gefitinib and inhibits HOTAIR expression by inducing miR-34a-5p expression in lung cancer cells | [118] [119] |