Evidence map›Paper›PMID 29799746›Full record

ArticleJournal of medicinal chemistry2018

Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.

Xin Zhao, Runfeng Li, Yang Zhou, Mengjie Xiao, Chunlong Ma, Zhongjin Yang, Shaogao Zeng, Qiuling Du, Chunguang Yang, Haiming Jiang and 10 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
2.1field-weighted citation impact, top 13% 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

14 citing papers in PubMed, 34 citations in OpenAlex.

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  13. Small Molecule Inhibitors of Influenza Virus Entry.Pharmaceuticals (Basel, Switzerland) · 2021
    Review
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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

20 authors at 4 institutions in 4 countries.

Xin ZhaoState Key Laboratory of Respiratory Disease, Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Sciences & The Fifth Affiliated Hospital , Guangzhou Medical University , Guangzhou 511436 , P. R. China.ORCID 0000-0002-6659-3748
Runfeng LiState Key Laboratory of Respiratory Disease, National Clinical Research Center for Respiratory Disease, Guangzhou Institute of Respiratory Health, The First Affiliated Hospital , Guangzhou Medical University , Guangzhou 510120 , P. R. China.
Yang ZhouDivision of Theoretical Chemistry and Biology, School of Biotechnology , Royal Institute of Technology (KTH), AlbaNova University Center , Stockholm SE-100 44 , Sweden.
Mengjie XiaoState Key Laboratory of Respiratory Disease, Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Sciences & The Fifth Affiliated Hospital , Guangzhou Medical University , Guangzhou 511436 , P. R. China.
Chunlong MaDepartment of Pharmacology and Toxicology, College of Pharmacy , The University of Arizona , Tucson , Arizona 85721 , United States.
Zhongjin YangState Key Laboratory of Respiratory Disease, Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Sciences & The Fifth Affiliated Hospital , Guangzhou Medical University , Guangzhou 511436 , P. R. China.
Shaogao ZengGuangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences , Guangzhou 510530 , P. R. China.
Qiuling DuState Key Laboratory of Respiratory Disease, National Clinical Research Center for Respiratory Disease, Guangzhou Institute of Respiratory Health, The First Affiliated Hospital , Guangzhou Medical University , Guangzhou 510120 , P. R. China.
Chunguang YangState Key Laboratory of Respiratory Disease, National Clinical Research Center for Respiratory Disease, Guangzhou Institute of Respiratory Health, The First Affiliated Hospital , Guangzhou Medical University , Guangzhou 510120 , P. R. China.
Haiming JiangState Key Laboratory of Respiratory Disease, National Clinical Research Center for Respiratory Disease, Guangzhou Institute of Respiratory Health, The First Affiliated Hospital , Guangzhou Medical University , Guangzhou 510120 , P. R. China.
Yanmei HuDepartment of Pharmacology and Toxicology, College of Pharmacy , The University of Arizona , Tucson , Arizona 85721 , United States.
Kefeng WangState Key Laboratory of Respiratory Disease, Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Sciences & The Fifth Affiliated Hospital , Guangzhou Medical University , Guangzhou 511436 , P. R. China.
Chris Ka Pun MokState Key Laboratory of Respiratory Disease, National Clinical Research Center for Respiratory Disease, Guangzhou Institute of Respiratory Health, The First Affiliated Hospital , Guangzhou Medical University , Guangzhou 510120 , P. R. China.
Ping SunState Key Laboratory of Respiratory Disease, Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Sciences & The Fifth Affiliated Hospital , Guangzhou Medical University , Guangzhou 511436 , P. R. China.
Jianghong DongGuangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences , Guangzhou 510530 , P. R. China.
Wei CuiGuangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences , Guangzhou 510530 , P. R. China.
Jun WangDepartment of Pharmacology and Toxicology, College of Pharmacy , The University of Arizona , Tucson , Arizona 85721 , United States.ORCID 0000-0002-4845-4621
Yaoquan TuDivision of Theoretical Chemistry and Biology, School of Biotechnology , Royal Institute of Technology (KTH), AlbaNova University Center , Stockholm SE-100 44 , Sweden.
Zifeng YangState Key Laboratory of Respiratory Disease, National Clinical Research Center for Respiratory Disease, Guangzhou Institute of Respiratory Health, The First Affiliated Hospital , Guangzhou Medical University , Guangzhou 510120 , P. R. China.
Wenhui HuState Key Laboratory of Respiratory Disease, Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Sciences & The Fifth Affiliated Hospital , Guangzhou Medical University , Guangzhou 511436 , P. R. China.
First Affiliated Hospital of Guangzhou Medical University · CNChinese Academy of Sciences · CNUniversity of Arizona · USAlbaNova · SE

Funding

Drug Discovery Targeting the Influenza A Virus M2-S31N Proton ChannelR33AI119187 · NIAID · UNIVERSITY OF ARIZONA · PI PEREZ, DANIEL R, WANG, JUN · 2017 to 2019
$1.2M
Drug Discovery Targeting the Influenza A Virus M2-S31N Proton ChannelR21AI119187 · NIAID · UNIVERSITY OF ARIZONA · PI PEREZ, DANIEL R, WANG, JUN · 2015 to 2016
$419k
NIAID NIH HHS R21 AI119187NIAID NIH HHS R33 AI119187
6 · The paper itself

Abstract

Influenza pandemic is a constant major threat to public health caused by influenza A viruses (IAVs). IAVs are subcategorized by the surface proteins hemagglutinin (HA) and neuraminidase (NA), in which they are both essential targets for drug discovery. While it is of great concern that NA inhibitor oseltamivir resistant strains are frequently identified from human or avian influenza virus, structural and functional characterization of influenza HA has raised hopes for new antiviral therapies. In this study, we explored a structure-activity relationship (SAR) of pinanamine-based antivirals and discovered a potent inhibitor M090 against amantadine-resistant viruses, including the 2009 H1N1 pandemic strains, and oseltamivir-resistant viruses. Mechanism of action studies, particularly hemolysis inhibition, indicated that M090 targets influenza HA and it occupied a highly conserved pocket of the HA

Indexed as

Drug DiscoveryAmantadineAntiviral AgentsDose-Response Relationship, DrugDrug Resistance, ViralEnzyme InhibitorsHemagglutininsImidazolesInfluenza A virusMicrobial Sensitivity TestsMolecular ConformationNeuraminidaseOseltamivirStructure-Activity RelationshipAmantadineAntiviral AgentsEnzyme InhibitorsHemagglutininsImidazolesNeuraminidaseOseltamivirpinanamine

Identifiers

PMID29799746
PMCPMC6496959
OpenAlexW2804001771

What OpenQuestion holds

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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.