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Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor.

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机构： [a]School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China [b]Innovation Center for Marine Drug Screening and Evaluation, Qingdao National Laboratory for Marine Science and Technology, Qingdao 266071, China [c]Marine Biomedical Research Institute of Qingdao, Qingdao 266071, China [d]Precision Medicine Research Center, Department of Respiratory and Critical Care Medicine, West China Hospital, Sichuan University, Chengdu 610041, China [e]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital of Sichuan University and Collaborative Innovation Center of Biotherapy and Cancer, Chengdu 610041, China

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关键词： MBRI-001 Polymorphs Co-crystal structure Tubulin inhibition Anti-cancer agent

摘要：

MBRI-001, a deuterium-substituted plinabulin derivative, has been reported to have better pharmacokinetic and similar antitumor effects in comparison with plinabulin. In this approach, we further carried out its polymorphs, co-crystal structure of MBRI-001-tubulin and tubulin inhibition study. Among the different polymorphs, Form F (MBRI-001/H2O) was prepared and evaluated, which had better physical stability and suitable process for scale-up production. Co-crystal structure of MBRI-001-tubulin (PDB:5XI5) was prepared and analyzed. The result of tubulin polymerization assay demonstrated that MBRI-001 could inhibit tubulin polymerization which was similar as plinabulin. Subsequently, the anti-proliferative activities of plinabulin and MBRI-001 were evaluated against two different human lung cancer cell lines. In vivo study, MBRI-001 revealed similar antitumor inhibition in comparison with plinabulin in A549 xenograft tumor model. Therefore, we suggested that MBRI-001 could be developed as a promising anti-cancer agent in near future. Copyright © 2019 Elsevier Ltd. All rights reserved.

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出版当年[2019]版：

大类 | 3 区医学

小类 | 2 区有机化学 3 区生化与分子生物学 3 区药物化学

最新[2023]版：

大类 | 3 区医学

小类 | 2 区有机化学 3 区生化与分子生物学 3 区药物化学

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第一作者机构： [a]School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China

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通讯机构： [a]School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China [b]Innovation Center for Marine Drug Screening and Evaluation, Qingdao National Laboratory for Marine Science and Technology, Qingdao 266071, China [c]Marine Biomedical Research Institute of Qingdao, Qingdao 266071, China [e]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital of Sichuan University and Collaborative Innovation Center of Biotherapy and Cancer, Chengdu 610041, China [*1]School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China

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