WebSep 25, 2024 · The release of DOX, intercalation of the drug with DNA and inhibition of topoisomerase II activity occurs Citation 173, Citation 174. Preclinical studies performed … WebAug 1, 2013 · The drugs bind at the enzyme-DNA interface and block DNA religation, ... Capranico G. DNA topoisomerase I inhibition by camptothecin induces escape of RNA polymerase II from promoter-proximal pause site, antisense transcription and histone acetylation at the human HIF-1alpha gene locus. Nucleic Acids Res. 2010; 38:159–171.
Targeting Topoisomerase I in the Era of Precision Medicine
WebPotent topoisomerase inhibitor analogs with substituents of different hydrophobic bonding constants showed a roughly inverse correlation between lipophilicity and MDR1 sensitivity. This is consistent with the notion that lipophilic compounds with faster passive diffusion rates can overwhelm the relatively slower unidirectional ATP-dependent drug efflux MDR1 … WebSeveral other drugs which ‘poison’ topoisomerase II have demonstrated antitumor activity in animal or clinical studies, but have not yet been approved for general clinically use. This paper will review the therapeutic use of currently approved topoisomerase II targeting anticancer drugs. It will be directed primarily at non-clinicians. cheap kitchen cabinets handles
Frontiers Discovery of New Catalytic Topoisomerase II Inhibitors for A…
WebJul 26, 2024 · DNA topoisomerase II is a nuclear enzyme that regulates DNA’s topological states and which is the main target for a number of important anticancer drugs (Corbett & Osherof, 1993; Maxwell, 1997). Therefore, topoisomerase inhibitors have become one of the effective and commonly used anticancer agents (Shigematsu et al., 2024 ; Wu et al., … Web9010 Background: Treatment options are limited for EGFRm NSCLC resistant to EGFR TKIs. HER3 is expressed in a majority of NSCLC tumors. U3-1402 is a HER3-targeted antibody drug conjugate with a fully human HER3-targeted antibody, novel cleavable peptide-based linker, and topoisomerase I inhibitor payload. WebDxd is a potent inhibitor of DNA topoisomerase I with an IC50 of 0.31 μM. It is used as a conjugated drug of HER2-targeting ADC. Targets&IC50: Topoisomerase I:0.31 μM: In vitro: In vivo: Dxd is cytotoxic to human cancer cell lines of KPL-4, NCI-N87, SK-BR-3, and MDA-MB-468 with IC50s of 1.43 nM-4.07 nM. cyberfirst schools and colleges