Evidence map›Paper›PMID 26491257›Full record

ArticleDrug design, development and therapy2015

A novel small-molecule inhibitor of HIV-1 entry.

Alonso Heredia, Olga S Latinovic, Florent Barbault, Erik P H de Leeuw

Open access · goldAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Drug design, development and therapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
0.6field-weighted citation impact, top 31% 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

6 citing papers in PubMed, 10 citations in OpenAlex.

  1. Benzothiazoles as potential antiviral agents.The Journal of pharmacy and pharmacology · 2020
    Review
  2. Antiviral Activities of Human Host Defense Peptides.Current medicinal chemistry · 2020
    Review
  3. Article
  4. Article
  5. Review
  6. Review
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

4 authors at 2 institutions in 2 countries.

Alonso HerediaDepartment of Medicine, University of Maryland Baltimore School of Medicine, Baltimore, MD, USA ; Institute of Human Virology, University of Maryland Baltimore School of Medicine, Baltimore, MD, USA.
Olga S LatinovicDepartment of Microbiology and Immunology, University of Maryland Baltimore School of Medicine, Baltimore, MD, USA ; Institute of Human Virology, University of Maryland Baltimore School of Medicine, Baltimore, MD, USA.
Florent BarbaultUniv Paris Diderot, Sorbonne Paris Cité, ITODYS, UMRCNRS7086, Paris, France.
Erik P H de LeeuwInstitute of Human Virology, University of Maryland Baltimore School of Medicine, Baltimore, MD, USA ; Department of Biochemistry and Molecular Biology, University of Maryland Baltimore School of Medicine, Baltimore, MD, USA.
University of Maryland, Baltimore · USUniversité Paris Cité · FR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundAntiretroviral therapy has transformed HIV-1 infection into a managed condition with near-normal life expectancy. However, a significant number of patients remain with limited therapeutic options due to HIV-1 resistance, side effects, or drug costs. Further, it is likely that current drugs will not retain efficacy, due to risks of side effects and transmitted resistance.

resultsWe describe compound 5660386 (3-ethyl-2-[3-(1,3,3-trimethyl-1,3-dihydro-2H-indol-2-ylidene)-1-propen-1-yl]-1,3-benzothiazol-3-ium) as a novel inhibitor of HIV-1 entry. Compound 5660386 inhibits HIV-1 entry in cell lines and primary cells, binds to HIV-1 envelope protein, and inhibits the interaction of GP120 to CD4. Further, compound 5660386 showed a unique and broad-range activity against primary HIV-1 isolates from different subtypes and geographical areas.

conclusionDevelopment of small-molecule entry inhibitors of HIV-1 such as 5660386 may lead to novel classes of anti-HIV-1 therapeutics. These inhibitors may be particularly effective against viruses resistant to current antiretroviral drugs and could have potential applications in both treatment and prevention.

Indexed as

Drug DesignBenzothiazolesBinding SitesCD4 AntigensCell LineCell SurvivalDose-Response Relationship, DrugHIV-1HIV Envelope Protein gp120HIV Fusion InhibitorsHIV InfectionsHumansKineticsMolecular Docking SimulationMolecular StructureProtein BindingBenzothiazolesCD4 Antigensgp120 protein, Human immunodeficiency virus 1HIV Envelope Protein gp120HIV Fusion Inhibitorsantiviral therapyCD4defensindrugentryHIV-1

Identifiers

PMID26491257
PMCPMC4598220
OpenAlexW2156954694

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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.