Entecavir competitively inhibits deoxyguanosine and deoxyadenosine phosphorylation in isolated mitochondria and the perfused rat heart

Ward, Avery S.; Hsiung, Chia-Heng; Kesterson, Daniel G.; Kamath, Vasudeva; McKee, Edward E.

doi:10.1016/j.jbc.2022.101876

Cited by 1 publication

(1 citation statement)

References 50 publications

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“…HIV integrase inhibitors are an important class of anti-AIDS drug, which can inhibit the replication process of the retrovirus and block the integration of virus DNA and host chromosome DNA [3,4]. Combination therapy with other anti-retroviral drugs, such as Entecavir, effectively treats HIV infection, reduces drug resistance, significantly improves the quality of life and survival time of patients with AIDS, and reduces mortality [5,6]. However, AIDS patients are prone to liver damage when receiving drug treatment, especially when multiple drugs are used in combination.…”

Section: Introductionmentioning

confidence: 99%

Discovery of Dolutegravir Derivative against Liver Cancer via Inducing Autophagy and DNA Damage

Hou,

Yan,

et al. 2024

Molecules

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We introduced a terminal alkyne into the core structure of dolutegravir, resulting in the synthesis of 34 novel dolutegravir-1,2,3-triazole compounds through click chemistry. These compounds exhibited remarkable inhibitory activities against two hepatocellular carcinoma cell lines, Huh7 and HepG2. Notably, compounds 5e and 5p demonstrated exceptional efficacy, particularly against Huh7 cells, with IC50 values of 2.64 and 5.42 μM. Additionally, both compounds induced apoptosis in Huh7 cells, suppressed tumor cell clone formation, and elevated reactive oxygen species (ROS) levels, further promoting tumor cell apoptosis. Furthermore, compounds 5e and 5p activated the LC3 signaling pathway, inducing autophagy, and triggered the γ-H2AX signaling pathway, resulting in DNA damage in tumor cells. Compound 5e exhibited low toxicity, highlighting its potential as a promising anti-tumor drug.

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