mtdna

IMT1B (LDC203974) is an orally administered, specific noncompetitive allosteric inhibitor of mitochondrial RNA polymerase (POLRMT), effectively suppressing mitochondrial DNA (mtDNA) expression and conferring anti-tumor properties.

Stavudine (BMY-27857), a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.

IMT1 (Propanamide, N,N-dimethyl-2-[[4-(2-methylphenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-) has anticancer activity.

PZL-A, an activator of mtDNA synthesis, restored the function and activity of the most common POLγ mutant variant and activated mtDNA synthesis in the cells of pediatric patients with fatal diseases, thereby enhancing the oxidative phosphorylation mechanism and the biogenesis of cellular respiration, and can be used to treat progressive diseases associated with mtDNA depletion.

NA-Ir is a ferroptosis (Ferroptosis) inducer that targets mitochondrial DNA (mtDNA) and activates the cGAS-STING pathway to stimulate ferritin autophagy (). It also induces the production of reactive oxygen species (ROS) through photodynamic therapy (PDT), depletes glutathione (GSH), and downregulates glutathione peroxidase 4 (GPX4), thereby triggering lipid peroxidation and ferroptosis. NA-Ir exhibits enhanced anticancer activity under light exposure and selectively inhibits cancer cells with high H2S content.

Anticanceragent 205 (compound 9) is an effective anticancer agent that binds to the G4-mtDNA target, inhibiting the replication, transcription, and translation of mtDNA (mitochondrial genome). It induces mitochondrial dysfunction, increases ROS production, and triggers DNA damage and cellular senescence. Anticanceragent 205 also promotes apoptosis and causes cell cycle arrest at the G0/G1 phase, showing potential for research in colorectal cancer.

Stavudine sodium (d4T), an orally active nucleoside reverse transcriptase inhibitor (NRTI), demonstrates activity against both HIV-1 and HIV-2. It also inhibits mitochondrial DNA (mtDNA) replication, reduces NLRP3 inflammasome activation, modulates Amyloid-β autophagy, and induces apoptosis [1] [2] [3] [4].

Zn(BQTC) is a potent inhibitor of both mitochondrial DNA (mtDNA) and nuclear DNA (nDNA), causing significant damage that disrupts mitochondrial and nuclear functions sequentially. It facilitates apoptotic signaling pathways triggered by DNA damage and exhibits selective antiproliferative effects on A549R cells, rendering it useful for anticancer research [1].

BKN-1, a bifunctional ligand, facilitates the tracking of mtG4s (G-quadruplexes, four-stranded DNA structures containing Hoogsteen bonds) formation via far-red emission and can induce mitochondrial dysfunction. This compound exhibits anti-tumor properties, potentially causing mtDNA loss, damaging mitochondrial integrity, reducing ATP levels, and triggering ROS imbalance, which can lead to apoptosis and autophagy [1].