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Discovery of a novel Aurora B inhibitor GSK650394 with potent anticancer and anti-aspergillus fumigatus dual efficacies in vitro

التفاصيل البيبلوغرافية
العنوان: Discovery of a novel Aurora B inhibitor GSK650394 with potent anticancer and anti-aspergillus fumigatus dual efficacies in vitro
المؤلفون: Yuhua He, Wei Fu, Liyang Du, Huiqiao Yao, Zhengkang Hua, Jinyu Li, Zhonghui Lin
المصدر: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 109-117 (2022)
بيانات النشر: Taylor & Francis Group, 2022.
سنة النشر: 2022
المجموعة: LCC:Therapeutics. Pharmacology
مصطلحات موضوعية: aurora b, inhibitor, anti-cancer, anti-aspergillus fumigatus, Therapeutics. Pharmacology, RM1-950
الوصف: Invasive fungal infections including Candidiasis and Aspergillosis are associated with considerable morbidity and mortality in immunocompromised individuals, such as cancer patients. Aurora B is a key mitotic kinase required for the cell division of eukaryotes from fungus to man. Here, we identified a novel Aurora B inhibitor GSK650394 that can inhibit the recombinant Aurora B from human and Aspergillus fumigatus, with IC50 values of 5.68 and 1.29 µM, respectively. In HeLa and HepG2 cells, GSK650394 diminishes the endogenous Aurora B activity and causes cell cycle arrest in G2/M phase. Further cell-based assays demonstrate that GSK650394 efficiently suppresses the proliferation of both cancer cells and Aspergillus fumigatus. Finally, the molecular docking calculation and site-directed mutagenesis analyses reveal the molecular mechanism of Aurora B inhibition by GSK650394. Our work is expected to provide new insight into the combinational therapy of cancer and Aspergillus fumigatus infection.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 1475-6366
1475-6374
14756366
Relation: https://doaj.org/toc/1475-6366; https://doaj.org/toc/1475-6374
DOI: 10.1080/14756366.2021.1975693
URL الوصول: https://doaj.org/article/b06e4be3e5fb45878a2e305dba9f046f
رقم الأكسشن: edsdoj.b06e4be3e5fb45878a2e305dba9f046f
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:14756366
14756374
DOI:10.1080/14756366.2021.1975693