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本文引用的文献

1
Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors.SARS-CoV-2 主蛋白酶的晶体结构为设计改良的 α-酮酰胺抑制剂提供了基础。
Science. 2020 Apr 24;368(6489):409-412. doi: 10.1126/science.abb3405. Epub 2020 Mar 20.
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Aminoquinolines against coronavirus disease 2019 (COVID-19): chloroquine or hydroxychloroquine.抗2019冠状病毒病(COVID-19)的氨基喹啉:氯喹或羟氯喹。
Int J Antimicrob Agents. 2020 Apr;55(4):105945. doi: 10.1016/j.ijantimicag.2020.105945. Epub 2020 Mar 17.
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SARS-CoV-2 is an appropriate name for the new coronavirus.严重急性呼吸综合征冠状病毒2型是这种新型冠状病毒的恰当名称。
Lancet. 2020 Mar 21;395(10228):949-950. doi: 10.1016/S0140-6736(20)30557-2. Epub 2020 Mar 6.
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In Vitro Antiviral Activity and Projection of Optimized Dosing Design of Hydroxychloroquine for the Treatment of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).羟氯喹治疗严重急性呼吸综合征冠状病毒 2 (SARS-CoV-2)的体外抗病毒活性和优化剂量设计预测。
Clin Infect Dis. 2020 Jul 28;71(15):732-739. doi: 10.1093/cid/ciaa237.
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SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor.严重急性呼吸综合征冠状病毒 2 型(SARS-CoV-2)进入细胞依赖于 ACE2 和 TMPRSS2,可被一种临床验证的蛋白酶抑制剂所阻断。
Cell. 2020 Apr 16;181(2):271-280.e8. doi: 10.1016/j.cell.2020.02.052. Epub 2020 Mar 5.
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Therapeutic options for the 2019 novel coronavirus (2019-nCoV).2019新型冠状病毒(2019-nCoV)的治疗选择。
Nat Rev Drug Discov. 2020 Mar;19(3):149-150. doi: 10.1038/d41573-020-00016-0.
7
Small Molecule Inhibitors of Middle East Respiratory Syndrome Coronavirus Fusion by Targeting Cavities on Heptad Repeat Trimers.通过靶向七聚体重复三聚体上的腔来抑制中东呼吸综合征冠状病毒融合的小分子抑制剂
Biomol Ther (Seoul). 2020 Jul 1;28(4):311-319. doi: 10.4062/biomolther.2019.202.
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Anti-HCV, nucleotide inhibitors, repurposing against COVID-19.抗 HCV,核苷酸抑制剂,重新用于 COVID-19。
Life Sci. 2020 May 1;248:117477. doi: 10.1016/j.lfs.2020.117477. Epub 2020 Feb 28.
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Therapeutic strategies in an outbreak scenario to treat the novel coronavirus originating in Wuhan, China.针对源自中国武汉的新型冠状病毒在疫情爆发情况下的治疗策略。
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Structure-Based Stabilization of Non-native Protein-Protein Interactions of Coronavirus Nucleocapsid Proteins in Antiviral Drug Design.基于结构的冠状病毒核衣壳蛋白非天然蛋白-蛋白相互作用的稳定化在抗病毒药物设计中的应用。
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药物研发与药物化学在 SARS-CoV-2 与新冠病毒治疗方面的努力

Drug Development and Medicinal Chemistry Efforts toward SARS-Coronavirus and Covid-19 Therapeutics.

机构信息

Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.

Department of Medicinal Chemistry and Molecular Pharmacolgy, Purdue University, West Lafayette, IN 47907, USA.

出版信息

ChemMedChem. 2020 Jun 4;15(11):907-932. doi: 10.1002/cmdc.202000223. Epub 2020 May 7.

DOI:10.1002/cmdc.202000223
PMID:32324951
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7264561/
Abstract

The COVID-19 pandemic caused by SARS-CoV-2 infection is spreading at an alarming rate and has created an unprecedented health emergency around the globe. There is no effective vaccine or approved drug treatment against COVID-19 and other pathogenic coronaviruses. The development of antiviral agents is an urgent priority. Biochemical events critical to the coronavirus replication cycle provided a number of attractive targets for drug development. These include, spike protein for binding to host cell-surface receptors, proteolytic enzymes that are essential for processing polyproteins into mature viruses, and RNA-dependent RNA polymerase for RNA replication. There has been a lot of ground work for drug discovery and development against these targets. Also, high-throughput screening efforts have led to the identification of diverse lead structures, including natural product-derived molecules. This review highlights past and present drug discovery and medicinal-chemistry approaches against SARS-CoV, MERS-CoV and COVID-19 targets. The review hopes to stimulate further research and will be a useful guide to the development of effective therapies against COVID-19 and other pathogenic coronaviruses.

摘要

由 SARS-CoV-2 感染引起的 COVID-19 大流行正在以惊人的速度传播,在全球范围内造成了前所未有的卫生紧急情况。目前尚无针对 COVID-19 和其他致病性冠状病毒的有效疫苗或批准的药物治疗方法。开发抗病毒药物是当务之急。冠状病毒复制周期中的关键生化事件为药物开发提供了许多有吸引力的靶点。这些靶点包括与宿主细胞表面受体结合的刺突蛋白、对多蛋白加工成成熟病毒至关重要的蛋白酶以及用于 RNA 复制的 RNA 依赖性 RNA 聚合酶。针对这些靶点的药物发现和开发已经取得了很多进展。此外,高通量筛选工作已经确定了多种先导结构,包括天然产物衍生的分子。本综述重点介绍了过去和现在针对 SARS-CoV、MERS-CoV 和 COVID-19 靶点的药物发现和药物化学方法。综述希望能激发进一步的研究,并为开发针对 COVID-19 和其他致病性冠状病毒的有效疗法提供有用的指导。