• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

一种在体外可中和严重急性呼吸综合征冠状病毒2(SARS-CoV-2)及其最具传染性的变体德尔塔(Delta)和奥密克戎(Omicron)感染的小分子。

A Small Molecule That In Vitro Neutralizes Infection of SARS-CoV-2 and Its Most Infectious Variants, Delta, and Omicron.

作者信息

Reyes-Alcaraz Arfaxad, Qasim Hanan, Merlinsky Elizabeth, Fox Glenn, Islam Tasneem, Medina Bryan, Schwartz Robert J, Craft John W, McConnell Bradley K

机构信息

Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, USA.

Rogers State University, 1701 W. Will Rogers Blvd., Claremore, OK 74017, USA.

出版信息

Biomedicines. 2023 Mar 15;11(3):916. doi: 10.3390/biomedicines11030916.

DOI:10.3390/biomedicines11030916
PMID:36979895
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10046252/
Abstract

The COVID-19 pandemic has underscored the urgent need to develop highly potent and safe medications that are complementary to the role of vaccines. Specifically, it has exhibited the need for orally bioavailable broad-spectrum antivirals that are able to be quickly deployed against newly emerging viral pathogens. The Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV2) and its variants Delta and Omicron are still a major threat to patients of all ages. In this brief report, we describe that the small molecule CD04872SC was able to neutralize SARS-CoV2 infection with a half-maximal effective concentration (EC50) = 248 μM. Serendipitously, we also were able to observe that CD04872SC inhibited the infection of the SARS-CoV-2 variants; Delta (EC50 = 152 μM) and Omicron (EC50 = 308 μM). These properties may define CD04872SC as a potential broad-spectrum candidate lead for the development of treatments for COVID-19.

摘要

新冠疫情凸显了开发高效且安全的药物的迫切需求,这些药物可作为疫苗的补充。具体而言,这表明需要口服生物利用度高的广谱抗病毒药物,以便能够迅速用于对抗新出现的病毒病原体。严重急性呼吸综合征冠状病毒2(SARS-CoV2)及其变种德尔塔和奥密克戎仍然对各年龄段的患者构成重大威胁。在本简要报告中,我们描述了小分子CD04872SC能够以半数有效浓度(EC50)= 248 μM中和SARS-CoV2感染。意外的是,我们还观察到CD04872SC抑制了SARS-CoV-2变种德尔塔(EC50 = 152 μM)和奥密克戎(EC50 = 308 μM)的感染。这些特性可能使CD04872SC成为开发新冠治疗药物的潜在广谱候选先导物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5652/10046252/7da0d8108955/biomedicines-11-00916-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5652/10046252/41a264625d86/biomedicines-11-00916-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5652/10046252/7da0d8108955/biomedicines-11-00916-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5652/10046252/41a264625d86/biomedicines-11-00916-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5652/10046252/7da0d8108955/biomedicines-11-00916-g002.jpg

相似文献

1
A Small Molecule That In Vitro Neutralizes Infection of SARS-CoV-2 and Its Most Infectious Variants, Delta, and Omicron.一种在体外可中和严重急性呼吸综合征冠状病毒2(SARS-CoV-2)及其最具传染性的变体德尔塔(Delta)和奥密克戎(Omicron)感染的小分子。
Biomedicines. 2023 Mar 15;11(3):916. doi: 10.3390/biomedicines11030916.
2
A mosaic-type trimeric RBD-based COVID-19 vaccine candidate induces potent neutralization against Omicron and other SARS-CoV-2 variants.一种基于三聚体 RBD 的马赛克型 COVID-19 疫苗候选物可诱导针对奥密克戎和其他 SARS-CoV-2 变体的强大中和作用。
Elife. 2022 Aug 25;11:e78633. doi: 10.7554/eLife.78633.
3
A Bispecific Antibody Targeting RBD and S2 Potently Neutralizes SARS-CoV-2 Omicron and Other Variants of Concern.一种靶向 RBD 和 S2 的双特异性抗体能有效中和 SARS-CoV-2 奥密克戎及其他关注变异株。
J Virol. 2022 Aug 24;96(16):e0077522. doi: 10.1128/jvi.00775-22. Epub 2022 Aug 2.
4
Structural Study of SARS-CoV-2 Antibodies Identifies a Broad-Spectrum Antibody That Neutralizes the Omicron Variant by Disassembling the Spike Trimer.SARS-CoV-2 抗体的结构研究鉴定出一种广谱抗体,通过分解 Spike 三聚体来中和奥密克戎变体。
J Virol. 2022 Aug 24;96(16):e0048022. doi: 10.1128/jvi.00480-22. Epub 2022 Aug 4.
5
Discovery of lead natural products for developing pan-SARS-CoV-2 therapeutics.发现用于开发泛 SARS-CoV-2 治疗药物的铅类天然产物。
Antiviral Res. 2023 Jan;209:105484. doi: 10.1016/j.antiviral.2022.105484. Epub 2022 Dec 8.
6
Novel Affibody Molecules Specifically Bind to SARS-CoV-2 Spike Protein and Efficiently Neutralize Delta and Omicron Variants.新型亲和体分子特异性结合 SARS-CoV-2 刺突蛋白并有效中和德尔塔和奥密克戎变异株。
Microbiol Spectr. 2023 Feb 14;11(1):e0356222. doi: 10.1128/spectrum.03562-22. Epub 2022 Dec 13.
7
Baculoviral COVID-19 Delta DNA vaccine cross-protects against SARS-CoV2 variants in K18-ACE2 transgenic mice.杆状病毒 COVID-19 Delta DNA 疫苗可在 K18-ACE2 转基因小鼠中交叉保护针对 SARS-CoV2 变体。
Vaccine. 2023 Feb 3;41(6):1223-1231. doi: 10.1016/j.vaccine.2022.12.067. Epub 2023 Jan 6.
8
A Glycosylated RBD Protein Induces Enhanced Neutralizing Antibodies against Omicron and Other Variants with Improved Protection against SARS-CoV-2 Infection.一种糖基化 RBD 蛋白诱导针对奥密克戎和其他变体的增强型中和抗体,提高对 SARS-CoV-2 感染的保护作用。
J Virol. 2022 Sep 14;96(17):e0011822. doi: 10.1128/jvi.00118-22. Epub 2022 Aug 16.
9
Extremely potent monoclonal antibodies neutralize Omicron and other SARS-CoV-2 variants.超强效单克隆抗体可中和奥密克戎及其他新冠病毒变体。
medRxiv. 2022 Jan 13:2022.01.12.22269023. doi: 10.1101/2022.01.12.22269023.
10
Wild-type SARS-CoV-2 neutralizing immunity decreases across variants and over time but correlates well with diagnostic testing.野生型 SARS-CoV-2 中和抗体的免疫活性会随着时间推移和变异株的不同而降低,但与诊断检测有很好的相关性。
Front Immunol. 2023 Feb 8;14:1055429. doi: 10.3389/fimmu.2023.1055429. eCollection 2023.

本文引用的文献

1
An infectious SARS-CoV-2 B.1.1.529 Omicron virus escapes neutralization by therapeutic monoclonal antibodies.一种传染性 SARS-CoV-2 B.1.1.529 奥密克戎病毒能够逃避治疗性单克隆抗体的中和作用。
Nat Med. 2022 Mar;28(3):490-495. doi: 10.1038/s41591-021-01678-y. Epub 2022 Jan 19.
2
Effectiveness of BNT162b2 Vaccine against Omicron Variant in South Africa.BNT162b2疫苗在南非针对奥密克戎变异株的有效性
N Engl J Med. 2022 Feb 3;386(5):494-496. doi: 10.1056/NEJMc2119270. Epub 2021 Dec 29.
3
Covid-19: Pfizer's paxlovid is 89% effective in patients at risk of serious illness, company reports.
新冠病毒:辉瑞公司报告称,其新冠口服药帕罗韦德对有重症风险的患者有效率达89%。
BMJ. 2021 Nov 8;375:n2713. doi: 10.1136/bmj.n2713.
4
Neuropilin-1 assists SARS-CoV-2 infection by stimulating the separation of Spike protein S1 and S2.神经纤毛蛋白-1通过刺激刺突蛋白S1和S2的分离来协助新型冠状病毒2感染。
Biophys J. 2021 Jul 20;120(14):2828-2837. doi: 10.1016/j.bpj.2021.05.026. Epub 2021 Jun 2.
5
Identification of Inhibitors of Integrin Cytoplasmic Domain Interactions With Syk.鉴定整合素胞质结构域与 Syk 相互作用的抑制剂。
Front Immunol. 2021 Jan 8;11:575085. doi: 10.3389/fimmu.2020.575085. eCollection 2020.
6
CD147-spike protein is a novel route for SARS-CoV-2 infection to host cells.CD147-刺突蛋白是 SARS-CoV-2 感染宿主细胞的新途径。
Signal Transduct Target Ther. 2020 Dec 4;5(1):283. doi: 10.1038/s41392-020-00426-x.
7
Neuropilin-1 facilitates SARS-CoV-2 cell entry and infectivity.神经纤毛蛋白-1 促进 SARS-CoV-2 细胞进入和感染性。
Science. 2020 Nov 13;370(6518):856-860. doi: 10.1126/science.abd2985. Epub 2020 Oct 20.
8
Learning from the past: development of safe and effective COVID-19 vaccines.从过去中学习:安全有效的 COVID-19 疫苗的研发。
Nat Rev Microbiol. 2021 Mar;19(3):211-219. doi: 10.1038/s41579-020-00462-y. Epub 2020 Oct 16.
9
Protocol and Reagents for Pseudotyping Lentiviral Particles with SARS-CoV-2 Spike Protein for Neutralization Assays.用于中和测定的用 SARS-CoV-2 刺突蛋白假型化慢病毒颗粒的方案和试剂。
Viruses. 2020 May 6;12(5):513. doi: 10.3390/v12050513.
10
Cell entry mechanisms of SARS-CoV-2.SARS-CoV-2 的细胞进入机制。
Proc Natl Acad Sci U S A. 2020 May 26;117(21):11727-11734. doi: 10.1073/pnas.2003138117. Epub 2020 May 6.