Flupyranochromene, a novel inhibitor of influenza virus cap-dependent endonuclease, from Penicillium sp. f28743

Yamasaki Manabu; Igarashi Masayuki; Sawa Ryuichi; Nosaka Chisato; Umekita Maya; Hatano Masaki; Kimura Tomoyuki; Iijima Kiyoko; Takizawa Naoki; Kato Taira; Mizumoto Kiyohisa; Nomoto Akio

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Flupyranochromene, a novel inhibitor of influenza virus cap-dependent endonuclease, from Penicillium sp. f28743

机译：Flupyranochromene是一种来自Penicillium sp的流感病毒覆盖型内切核酸酶的新型抑制剂。 F28743.

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Influenza virus RNA polymerase has cap-dependent endonuclease activity that produces capped RNA fragments for priming viral mRNA synthesis. This enzymatic activity is essential for viral propagation, but it is not present in any host cellular enzyme, making it an attractive target for the development of anti-influenza drugs. Here, we isolated a novel inhibitor of cap-dependent endonuclease, named flupyranochromene, from the fermentation broth of the fungus Penicillium sp. f28743. Structural analysis revealed that this compound bears a putative pharmacophore that chelates divalent metal ion(s) present in the endonuclease active site in the PA subunit of the polymerase. Consistently, in vitro endonuclease assays showed that flupyranochromene exerts its inhibitory effects by blocking endonucleolytic cleavage by the PA subunit of viral RNA polymerase complex.

机译：流感病毒RNA聚合酶具有覆盖依赖性内切核酸酶活性，其产生用于引发病毒mRNA合成的盖RNA片段。该酶活性对于病毒繁殖至关重要，但它不存在于任何宿主细胞酶中，使其成为抗流感药物的发育的有吸引力的靶标。在这里，我们将一种新的胱盖依赖性内切核酸酶的抑制剂，命名为Flupyranochromene，来自真菌的Penicillium sp的发酵液。 F28743。结构分析表明，该化合物承载了一种推定的药镜，其在聚合酶的PA亚基中螯合在内切核酸酶活性位点中的二价金属离子。始终如一地，体外内切核酸酶测定表明，Flupyranochromene通过通过病毒RNA聚合酶复合物的PA亚基阻断内外核酸裂解来施加其抑制作用。

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《The Journal of Antibiotics: An International Journal》 |2019年第3期|共9页
作者
Yamasaki Manabu; Igarashi Masayuki; Sawa Ryuichi; Nosaka Chisato; Umekita Maya; Hatano Masaki; Kimura Tomoyuki; Iijima Kiyoko; Takizawa Naoki; Kato Taira; Mizumoto Kiyohisa; Nomoto Akio;
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Inst Microbial Chem BIKAKEN Shinagawa Ku Tokyo Japan;

Inst Microbial Chem BIKAKEN Shinagawa Ku Tokyo Japan;

Inst Microbial Chem BIKAKEN Shinagawa Ku Tokyo Japan;

Inst Microbial Chem BIKAKEN Shinagawa Ku Tokyo Japan;

Inst Microbial Chem BIKAKEN Shinagawa Ku Tokyo Japan;

Inst Microbial Chem BIKAKEN Shinagawa Ku Tokyo Japan;

Inst Microbial Chem BIKAKEN Shinagawa Ku Tokyo Japan;

Inst Microbial Chem BIKAKEN Shinagawa Ku Tokyo Japan;

Inst Microbial Chem BIKAKEN Shinagawa Ku Tokyo Japan;

MicroBiopharm Japan Co Ltd Chuo Ku Tokyo Japan;

Kitasato Univ Sch Pharm Lab Biochem Minato Ku Tokyo Japan;

Inst Microbial Chem BIKAKEN Shinagawa Ku Tokyo Japan;

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正文语种 eng
中图分类药学;
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1. Flupyranochromene, a novel inhibitor of influenza virus cap-dependent endonuclease, from Penicillium sp. f28743 [J] . Yamasaki Manabu, Igarashi Masayuki, Sawa Ryuichi, The Journal of Antibiotics: An International Journal . 2019,第3期

机译：Flupyranochromene是一种来自Penicillium sp的流感病毒覆盖型内切核酸酶的新型抑制剂。 F28743.
2. Global update on the susceptibilities of human influenza viruses to neuraminidase inhibitors and the cap-dependent endonuclease inhibitor baloxavir, 2017-2018 [J] . Antiviral Research . 2020,第期

机译：全球关于人流感病毒对神经酰胺酶抑制剂的敏感性的最新性和涵盖型内切核酸酶抑制剂Baloxavir，2017-2018
3. Combination treatment with the cap-dependent endonuclease inhibitor baloxavir marboxil and a neuraminidase inhibitor in a mouse model of influenza A virus infection [J] . Fukao Keita, Noshi Takeshi, Yamamoto Atsuko, The Journal of Antimicrobial Chemotherapy . 2019,第3期

机译：用CAP依赖性内切核酸酶的组合治疗抑制剂Baloxavir Marboxil和流感病毒感染小鼠模型中的神经氨酸酶抑制剂
4. Novel Protease Inhibitor Inhibiting Proliferation of Influenza Virus: Purification and cDNA Cloning of a Novel Protease Inhibitor Secreted by MDCK Cells [C] . Kiyoto Nishiyama, Keishin Sugawara, Kenji Soejima, Annual and International Meeting of the Japanese Association for Animal Cell Technology . 2010

机译：抑制流感病毒的新型蛋白酶抑制剂：用MDCK细胞分泌的新型蛋白酶抑制剂的纯化和cDNA克隆
5. Influenza A Virus Replication: Biochemical Characterization of Conserved RNA Promoter Structure and PA Subunit Endonuclease Activity [D] . Noble, Erin. 2013

机译：甲型流感病毒复制：保守的RNA启动子结构和PA亚基核酸内切酶活性的生化特征
6. Delayed Dosing of S-033188 a Novel Inhibitor of Influenza Virus Cap-dependent Endonuclease Exhibited Significant Reduction of Viral Titer and Mortality in Mice Infected with Influenza A Virus [O] . Keita Fukao, Yoshinori Ando, Takeshi Noshi, 2017

机译：S-033188一种新型的流感病毒帽依赖性核酸内切酶抑制剂延迟给药在感染甲型流感病毒的小鼠中显示出显着的病毒滴度和死亡率降低
7. Delayed Dosing of S-033188, a Novel Inhibitor of Influenza Virus Cap-dependent Endonuclease, Exhibited Significant Reduction of Viral Titer and Mortality in Mice Infected with Influenza A Virus [O] . Keita Fukao, Yoshinori Ando, Takeshi Noshi, 2017

机译：S-033188的延迟剂量，流感病毒依赖性内切核酸酶的新型抑制剂，在感染甲型病毒中感染的小鼠病毒滴度和死亡率显着降低

Flupyranochromene, a novel inhibitor of influenza virus cap-dependent endonuclease, from Penicillium sp. f28743

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