Oxoisoaporphine as Potent Telomerase Inhibitor
AbstractTwo compounds previously isolated from traditional Chinese medicine, Menispermum dauricum (DC), 6-hydroxyl-oxoisoaporphine (H-La), and 4,6-di(2-pyridinyl)benzo[h]isoindolo[4,5,6-de]quinolin-8(5H)-one (H-Lb), were known to have in vitro antitumor activity and to selectively bind human telomeric, c-myc, and bcl-2 G-quadruplexes (G4s). In this study, the binding properties of these two compounds to telomerase were investigated through molecular docking and telomeric repeat amplication protocol and silver staining assay (TRAP-silver staining assay). The binding energies bound to human telomerase RNA were calculated by molecular docking to be −6.43 and −9.76 kcal/mol for H-La and H-Lb, respectively. Compared with H-La, the ligand H-Lb more strongly inhibited telomerase activity in the SK-OV-3 cells model. View Full-Text
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Wei, Z.-Z.; Qin, Q.-P.; Chen, J.-N.; Chen, Z.-F. Oxoisoaporphine as Potent Telomerase Inhibitor. Molecules 2016, 21, 1534.
Wei Z-Z, Qin Q-P, Chen J-N, Chen Z-F. Oxoisoaporphine as Potent Telomerase Inhibitor. Molecules. 2016; 21(11):1534.Chicago/Turabian Style
Wei, Zu-Zhuang; Qin, Qi-Pin; Chen, Jia-Nian; Chen, Zhen-Feng. 2016. "Oxoisoaporphine as Potent Telomerase Inhibitor." Molecules 21, no. 11: 1534.
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