Evidence map›Paper›PMID 39062532›Full record

ArticleBiomolecules2024

Discovery of Benzisothiazolone Derivatives as Bifunctional Inhibitors of HIV-1 Reverse Transcriptase DNA Polymerase and Ribonuclease H Activities.

Alondra Vázquez Rivera, Heather Donald, Mounia Alaoui-El-Azher, John J Skoko, John S Lazo, Michael A Parniak, Paul A Johnston, Nicolas Sluis-Cremer

Abstract read
In one paragraph

Article in Biomolecules, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
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

1 citing paper in PubMed.

  1. 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

8 authors.

Alondra Vázquez RiveraDepartment of Medicine, Division of Infectious Diseases, University of Pittsburgh School of Medicine, Pittsburgh, PA 15261, USA.
Heather DonaldDepartment of Medicine, Division of Infectious Diseases, University of Pittsburgh School of Medicine, Pittsburgh, PA 15261, USA.
Mounia Alaoui-El-AzherDepartment of Medicine, Division of Infectious Diseases, University of Pittsburgh School of Medicine, Pittsburgh, PA 15261, USA.
John J SkokoDepartment of Chemical Biology and Pharmacology, University of Pittsburgh School of Medicine, Pittsburgh, PA 15261, USA.
John S LazoDepartment of Pharmacology, University of Virginia, Charlottesville, VA 22908, USA.ORCID 0000-0002-0645-4025
Michael A ParniakDepartment of Microbiology and Molecular Genetics, University of Pittsburgh School of Medicine, Pittsburgh, PA 15219, USA.
Paul A JohnstonDepartment of Pharmaceutical Sciences, University of Pittsburgh School of Pharmacy, Pittsburgh, PA 15261, USA.
Nicolas Sluis-CremerDepartment of Medicine, Division of Infectious Diseases, University of Pittsburgh School of Medicine, Pittsburgh, PA 15261, USA.

Funding

Women's Oncology Program - WONP30CA044579 · NCI · UNIVERSITY OF VIRGINIA CHARLOTTESVILLE · PI Jay William FOX · 1987 to 2026
$72.1M
Pittsburgh Molecular Libraries Screening Center(RMI)U54MH074411 · NIMH · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · PI LAZO, JOHN S. · 2005 to 2008
$10.1M
NCI NIH HHS P30 CA044579NIH HHS 1U54MH074411-08A1NIH HHS U54MH074411; XO1MH077605; R01AI175067
6 · The paper itself

Abstract

The ribonuclease H (RNase H) active site of HIV-1 reverse transcriptase (RT) is the only viral enzyme not targeted by approved antiretroviral drugs. Using a fluorescence-based in vitro assay, we screened 65,239 compounds at a final concentration of 10 µM to identify inhibitors of RT RNase H activity. We identified 41 compounds that exhibited 50% inhibitory concentration (i.e., IC

Indexed as

HIV-1HIV Reverse TranscriptaseReverse Transcriptase InhibitorsThiazolesAnti-HIV AgentsDrug DiscoveryHumansRibonuclease HStructure-Activity Relationship1,2-benzisothiazoline-3-oneAnti-HIV AgentsHIV Reverse Transcriptasereverse transcriptase, Human immunodeficiency virus 1Reverse Transcriptase InhibitorsRibonuclease HThiazolesbenzisothiazoloneHIV-1inhibitorpolymerasereverse transcriptaseribonuclease H

Identifiers

PMID39062532
PMCPMC11274943

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Registered trials

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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.