Evidence map›Paper›PMID 29039736›Full record

ArticleeLife2017

A novel central nervous system-penetrating protease inhibitor overcomes human immunodeficiency virus 1 resistance with unprecedented aM to pM potency.

Manabu Aoki, Hironori Hayashi, Kalapala Venkateswara Rao, Debananda Das, Nobuyo Higashi-Kuwata, Haydar Bulut, Hiromi Aoki-Ogata, Yuki Takamatsu, Ravikiran S Yedidi, David A Davis and 12 more

Open access · goldAbstract read
In one paragraph

Article in eLife, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.

0numbers the graph read from it
0cells of the map it votes in
39citing papers in PubMed
3.7field-weighted citation impact, top 6% 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

39 citing papers in PubMed, 52 citations in OpenAlex.

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  12. Identification of SARS-CoV-2 MNature communications · 2023
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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

22 authors at 6 institutions in 2 countries.

Manabu AokiExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, United States.
Hironori HayashiNational Center for Global Health and Medicine Research Institute, Tokyo, Japan.
Kalapala Venkateswara RaoDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, United States.
Debananda DasExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, United States.ORCID 0000-0001-9943-5888
Nobuyo Higashi-KuwataNational Center for Global Health and Medicine Research Institute, Tokyo, Japan.
Haydar BulutExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, United States.
Hiromi Aoki-OgataExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, United States.
Yuki TakamatsuExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, United States.ORCID 0000-0001-7967-1576
Ravikiran S YedidiExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, United States.
David A DavisRetroviral Disease Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, United States.
Shin-Ichiro HattoriNational Center for Global Health and Medicine Research Institute, Tokyo, Japan.
Noriko NishidaBioanalysis Group, Drug Metabolism and Analysis Department, Nonclinical Research Center, Drug Development Service Segment, LSI Medience Corporation, Tokyo, Japan.
Kazuya HasegawaProtein Crystal Analysis Division, Japan Synchrotron Radiation Research Institute, Hyogo, Japan.
Nobutoki TakamuneInnovative Collaboration Organization, Kumamoto University, Kumamoto, Japan.
Prasanth R NyalapatlaDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, United States.
Heather L OsswaldDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, United States.
Hirofumi JonoDepartment of Pharmacy, Kumamoto University Hospital, Kumamoto, Japan.
Hideyuki SaitoDepartment of Pharmacy, Kumamoto University Hospital, Kumamoto, Japan.
Robert YarchoanRetroviral Disease Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, United States.
Shogo MisumiDepartment of Environmental and Molecular Health Sciences, Faculty of Medical and Pharmaceutical Sciences, Kumamoto University, Kumamoto, Japan.
Arun K GhoshDepartment of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, United States.
Hiroaki MitsuyaExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, United States.ORCID 0000-0001-9274-3853
National Institutes of Health · USPurdue University West Lafayette · USNational Center for Global Health and Medicine · JPKumamoto University · JPKumamoto University Hospital · JPJapan Synchrotron Radiation Research Institute · JP

Funding

Development of Antiviral Therapy of HIV-1 InfectionZIASC006738 · NCI · DIVISION OF CLINICAL SCIENCES - NCI · PI MITSUYA, HIROAKI · 2009 to 2025
$10.0M
Design & Synthesis of Nonpeptide Protease InhibitorsR37GM053386 · NIGMS · PURDUE UNIVERSITY · PI GHOSH, ARUN K · 2011 to 2018
$3.9M
DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORSR01GM053386 · NIGMS · UNIVERSITY OF ILLINOIS AT CHICAGO · PI GHOSH, ARUN K · 1995 to 2010
$3.7M
NIGMS NIH HHS R01 GM053386NIGMS NIH HHS R37 GM053386
6 · The paper itself

Abstract

Antiretroviral therapy for HIV-1 infection/AIDS has significantly extended the life expectancy of HIV-1-infected individuals and reduced HIV-1 transmission at very high rates. However, certain individuals who initially achieve viral suppression to undetectable levels may eventually suffer treatment failure mainly due to adverse effects and the emergence of drug-resistant HIV-1 variants. Here, we report GRL-142, a novel HIV-1 protease inhibitor containing an unprecedented 6-5-5-ring-fused crown-like tetrahydropyranofuran, which has extremely potent activity against all HIV-1 strains examined with IC

Indexed as

AnimalsCells, CulturedCentral Nervous SystemDrug Resistance, ViralHIV-1HIV ProteaseHIV Protease InhibitorsHumansInhibitory Concentration 50Microbial Sensitivity TestsProtein BindingRatsHIV ProteaseHIV Protease InhibitorsCNS penetrationdrug-resistant HIV-1GRL-142infectious diseasemicrobiologyprotease inhibitorvirus

Identifiers

PMID29039736
PMCPMC5644950
OpenAlexW2766696270

What Socratic holds

Textmetadata
LicenceCC0
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 Socratic graph.