Evidence map›Paper›PMID 34364941›Full record

ArticleInternational journal of biological macromolecules2021

Repurposing clinically approved drugs for COVID-19 treatment targeting SARS-CoV-2 papain-like protease.

Yunxia Xu, Ke Chen, Juanli Pan, Yingshou Lei, Danting Zhang, Lipei Fang, Jinle Tang, Xin Chen, Yanhong Ma, Yi Zheng and 4 more

Open access · greenAbstract read
In one paragraph

Article in International journal of biological macromolecules, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.

0numbers the graph read from it
0cells of the map it votes in
22citing papers in PubMed
5.7field-weighted citation impact, top 4% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

22 citing papers in PubMed, 43 citations in OpenAlex.

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  19. Inhibitors of SARS-CoV-2 PLpro.Frontiers in chemistry · 2022
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

14 authors at 5 institutions in 2 countries.

Yunxia XuGuangzhou Eighth People's Hospital, Guangzhou Medical University, Guangzhou, Guangdong 510060, China; Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, Guangdong 510515, China.
Ke ChenShenzhen Graduate School, Peking University, Shenzhen, Guangdong 518055, China; Institute for Systems and Physical Biology, Shenzhen Bay Laboratory, Shenzhen, Guangdong 518038, China.
Juanli PanGuangzhou Eighth People's Hospital, Guangzhou Medical University, Guangzhou, Guangdong 510060, China.
Yingshou LeiInstitute for Systems and Physical Biology, Shenzhen Bay Laboratory, Shenzhen, Guangdong 518038, China.
Danting ZhangInstitute for Systems and Physical Biology, Shenzhen Bay Laboratory, Shenzhen, Guangdong 518038, China.
Lipei FangInstitute for Systems and Physical Biology, Shenzhen Bay Laboratory, Shenzhen, Guangdong 518038, China.
Jinle TangInstitute for Systems and Physical Biology, Shenzhen Bay Laboratory, Shenzhen, Guangdong 518038, China.
Xin ChenGuangzhou Eighth People's Hospital, Guangzhou Medical University, Guangzhou, Guangdong 510060, China.
Yanhong MaGuangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, Guangdong 510515, China.
Yi ZhengDepartment of Developmental Biology, School of Basic Medical Science, Southern Medical University, Guangzhou, Guangdong 510515, China.
Bao ZhangBiosafety Level-3 Laboratory, School of Public Health, Southern Medical University, Guangzhou 510515, China.
Yaoqi ZhouShenzhen Graduate School, Peking University, Shenzhen, Guangdong 518055, China; Institute for Systems and Physical Biology, Shenzhen Bay Laboratory, Shenzhen, Guangdong 518038, China; Institute for Glycomics, Griffith University, Southport, Queensland 4222, Australia. Electronic address: zhouyq@szbl.ac.cn.
Jian ZhanInstitute for Systems and Physical Biology, Shenzhen Bay Laboratory, Shenzhen, Guangdong 518038, China; Institute for Glycomics, Griffith University, Southport, Queensland 4222, Australia. Electronic address: zhanjian@szbl.ac.cn.
Wei XuGuangzhou Eighth People's Hospital, Guangzhou Medical University, Guangzhou, Guangdong 510060, China; Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, Guangdong 510515, China. Electronic address: xuwei3322@smu.edu.cn.
Shenzhen Bay Laboratory · CNSouthern Medical University · CNGuangzhou Medical University · CNGuangzhou Eighth People's Hospital · CNPeking University Shenzhen Hospital · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

COVID-19 is a disease caused by SARS-CoV-2, which has led to more than 4 million deaths worldwide. As a result, there is a worldwide effort to develop specific drugs for targeting COVID-19. Papain-like protease (PLpro) is an attractive drug target because it has multiple essential functions involved in processing viral proteins, including viral genome replication and removal of post-translational ubiquitination modifications. Here, we established two assays for screening PLpro inhibitors according to protease and anti-ISGylation activities, respectively. Application of the two screening techniques to the library of clinically approved drugs led to the discovery of tanshinone IIA sulfonate sodium and chloroxine with their IC50 values of lower than 10 μM. These two compounds were found to directly interact with PLpro and their molecular mechanisms of binding were illustrated by docking and molecular dynamics simulations. The results highlight the usefulness of the two developed screening techniques for locating PLpro inhibitors.

Indexed as

COVID-19 Drug TreatmentDrug RepositioningAntiviral AgentsBinding SitesChloroquinolinolsCoronavirus Papain-Like ProteasesCoronavirus Protease InhibitorsHigh-Throughput Screening AssaysHumansMolecular Docking SimulationMolecular Dynamics SimulationPhenanthrenesSARS-CoV-2Antiviral AgentsChloroquinolinolschloroxineCoronavirus Papain-Like ProteasesCoronavirus Protease Inhibitorspapain-like protease, SARS-CoV-2Phenanthrenestanshinone II A sodium sulfonateChloroxinePapain-like proteaseTanshinone IIA sulfonate sodium

Identifiers

PMID34364941
PMCPMC8342870
OpenAlexW3191665138

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.