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2,169 results on '"Zhu, Chun"'

14. Design of hadronic calorimeter for DarkSHINE experiment

Author

Wang, Zhen, Yuan, Rui, Liu, Han-Qing, Chen, Jing, Chen, Xiang, Khaw, Kim Siang, Li, Liang, Li, Shu, Liu, Kun, Liu, Qi-Bin, Song, Si-Yuan, Sun, Tong, Wang, Xiao-Long, Wang, Yu-Feng, Yang, Hai-Jun, Zhang, Jun-Hua, Zhang, Yu-Lei, Zhao, Zhi-Yu, Zhu, Chun-Xiang, Zhu, Xu-Liang, and Zhu, Yi-Fan

Published
2024
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19. Risk factors for renal outcomes in children with antineutrophil cytoplasmic antibody-associated vasculitis: a nationwide retrospective study in China

Author

Tan, Li-Wen, Wan, Jun-Li, Zhu, Chun-Hua, Xu, Hong, Xia, Zheng-Kun, Chen, Li-Zhi, Wu, Xiao-Chuan, Wang, Fang, Liu, Xiao-Rong, Zhao, Cheng-Guang, Li, Xiao-Zhong, Mao, Jian-Hua, Wang, Xiao-Wen, Huang, Wen-Yan, Li, Yu-Hong, Zhang, Jian-Jiang, Feng, Shi-Pin, Yang, Jun, Liu, Jiao-Jiao, Gao, Chun-Lin, Rong, Li-Ping, Shuai, Lan-Jun, Xu, Ke, Zhang, He-Jia, Li, Qiu, Zhang, Ai-Hua, and Wang, Mo

Published
2024
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34. In-cell bioluminescence resonance energy transfer (BRET)-based assay uncovers ceritinib and CA-074 as SARS-CoV-2 papain-like protease inhibitors

Author

Mei Li, Zhu-Chun Bei, Yongtian Yuan, Baogang Wang, Dongna Zhang, Likun Xu, Liangliang Zhao, Qin Xu, and Yabin Song

Subjects
papain-like protease (PLpro), SARS-CoV-2, bioluminescence resonance energy transfer (BRET), protease inhibitors, high-throughput screening (HTS), Therapeutics. Pharmacology, RM1-950
Abstract

Papain-like protease (PLpro) is an attractive anti-coronavirus target. The development of PLpro inhibitors, however, is hampered by the limitations of the existing PLpro assay and the scarcity of validated active compounds. We developed a novel in-cell PLpro assay based on BRET and used it to evaluate and discover SARS-CoV-2 PLpro inhibitors. The developed assay demonstrated remarkable sensitivity for detecting the reduction of intracellular PLpro activity while presenting high reliability and performance for inhibitor evaluation and high-throughput screening. Using this assay, three protease inhibitors were identified as novel PLpro inhibitors that are structurally disparate from those previously known. Subsequent enzymatic assays and ligand-protein interaction analysis based on molecular docking revealed that ceritinib directly inhibited PLpro, showing high geometric complementarity with the substrate-binding pocket in PLpro, whereas CA-074 methyl ester underwent intracellular hydrolysis, exposing a free carboxyhydroxyl group essential for hydrogen bonding with G266 in the BL2 groove, resulting in PLpro inhibition.

Published
2024
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36. In vitro interaction of naphthoquine with ivermectin, atovaquone, curcumin, and ketotifen in the asexual blood stage of Plasmodium falciparum 3D7

Author

Ruotong Liu, Guoming Li, Mei Li, Baogang Wang, Dongna Zhang, Likun Xu, Liangliang Zhao, Ruhe Liao, Qin Xu, Zhu-Chun Bei, and Yabin Song

Subjects
antimalarial drugs, Plasmodium falciparum, malaria, pharmacodynamics, drug interactions, Microbiology, QR1-502
Abstract

ABSTRACT Naphthoquine is a promising candidate for antimalarial combination therapy. Its combination with artemisinin has demonstrated excellent efficacy in clinical trials conducted across various malaria-endemic areas. A co-formulated combination of naphthoquine and azithromycin has also shown high clinical efficacy for malaria prophylaxis in Southeast Asia. Developing new combination therapies using naphthoquine will provide additional arsenal responses to the growing threat of artemisinin resistance. Furthermore, due to its long half-life, the possible interaction of naphthoquine with other drugs also needs attention. However, studies on its pharmacodynamic interactions with other drugs are still limited. In this study, the in vitro interactions of naphthoquine with ivermectin, atovaquone, curcumin, and ketotifen were evaluated in the asexual stage of Plasmodium falciparum 3D7. By using the combination index analysis and the SYBR Green I-based fluorescence assay, different interaction patterns of selected drugs with naphthoquine were revealed. Curcumin showed a slight but significant synergistic interaction with naphthoquine at lower effect levels, and no antagonism was observed across the full range of effect levels for all tested ratios. Atovaquone showed a potency decline when combined with naphthoquine. For ivermectin, a significant antagonism with naphthoquine was observed at a broad range of effect levels below 75% inhibition, although no significant interaction was observed at higher effect levels. Ketotifen interacted with naphthoquine similar to ivermectin, but significant antagonism was observed for only one tested ratio. These findings should be helpful to the development of new naphthoquine-based combination therapy and the clinically reasonable application of naphthoquine-containing therapies.IMPORTANCEPharmacodynamic interaction between antimalarials is not only crucial for the development of new antimalarial combination therapies but also important for the appropriate clinical use of antimalarials. The significant synergism between curcumin and naphthoquine observed in this study suggests the potential value for further development of new antimalarial combination therapy. The finding of a decline in atovaquone potency in the presence of naphthoquine alerts to a possible risk of treatment or prophylaxis failure for atovaquone–proguanil following naphthoquine-containing therapies. The observation of antagonism between naphthoquine and ivermectin raised a need for concern about the applicability of naphthoquine-containing therapy in malaria-endemic areas with ivermectin mass drug administration deployed. Considering the role of atovaquone–proguanil as a major alternative when first-line artemisinin-based combination therapy is ineffective and the wide implementation of ivermectin mass drug administration in malaria-endemic countries, the above findings will be important for the appropriate clinical application of antimalarials involving naphthoquine-containing therapies.

Published
2024
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