ONO-5334结构式
CAS号：868273-90-9
COVID-19：来自Ono Pharmaceutical的有前途的骨质疏松症药物：MDL-28170，ONO 5334，Apilimod
新型冠状病毒肺炎（COVID-19）：新冠肺炎（COVID-19）：COVID-19：
【华盛顿】
美国团队24日在英国科学杂志《自然》上宣布。
细胞实验结果：
我们在细胞实验中调查了大约12,000种正在开发或存在的药物是否可用于COVID-19治疗。
结果，来自美国的一个小组于7月24日在英国科学杂志《自然》上发表了“三种类型有希望的论文”。
ONO5334：
其中之一是“ ONO5334”，其由小野制药有限公司（大阪）开发用于治疗骨质疏松症，但尚未投入实际使用。
小野制药说：“我们将仔细检查内容并考虑响应。”
培养的肺细胞中的病毒感染实验：
该实验是“用病毒感染由人iPS细胞制成的培养的肺细胞的实验”。
施用ONO5334后，感染细胞减少72％。
其他两种类型也下降了65至85％。
联合沟通
https://this.kiji.is/659573789646046305
Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing
Published: 24 July 2020
This is an unedited manuscript that has been accepted for publication.
Nature Research
are providing this early version of the manuscript as a service to our authors and readers.
The manuscript will undergo copyediting, typesetting and a proof review before it is published in its final form.
Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers apply.
Laura Riva, Shuofeng Yuan, […]Sumit K. Chanda
Abstract
The emergence of the novel SARS coronavirus 2 (SARS-CoV-2) in 2019
has triggered an ongoing global pandemic of severe pneumonia-like disease designated as coronavirus disease 2019 (COVID-19)1.
The development of a vaccine
is likely to require at least 12-18 months, and the typical timeline for approval of a novel antiviral therapeutic can exceed 10 years.
Thus, repurposing of known drugs
could significantly accelerate the deployment of novel therapies for COVID-19.
Towards this end, we profiled a library of known drugs encompassing approximately 12,000 clinical-stage or FDA-approved small molecules.
We report the identification of 100 molecules that inhibit viral replication, including 21 known drugs that exhibit dose response relationships.
Of these, thirteen
were found to harbor effective concentrations likely commensurate with achievable therapeutic doses in patients,
including
- the PIKfyve kinase inhibitor apilimod2–4,
- the cysteine protease inhibitors
- MDL-28170,
- Z LVG CHN2,
- VBY-825,
- ONO 5334.
Notably,
- MDL-28170,
- ONO 5334,
- apilimod
were found to antagonize viral replication in human iPSC-derived pneumocyte-like cells,
the PIKfyve inhibitor also
demonstrated antiviral efficacy in a primary human lung explant model.
Since most of the molecules identified in this study have already advanced into the clinic, the known pharmacological
and human safety profiles of these compounds will enable accelerated preclinical and clinical evaluation of these drugs for the treatment of COVID-19.
https://www.nature.com/articles/s41586-020-2577-1
ONO-5334 | Cathepsin K 阻害剤 |
ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with Ki values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO-5334 has the potential for the study of osteoporosis.
MedChemExpress