Evidence map›Paper›PMID 21600931›Full record

ArticleAntiviral research2011

Identification of low-molecular weight inhibitors of HIV-1 reverse transcriptase using a cell-based high-throughput screening system.

Oyebisi Jegede, Ana Khodyakova, Mikhail Chernov, Jan Weber, Luis Menéndez-Arias, Andrei Gudkov, Miguel E Quiñones-Mateu

Open access · greenAbstract read
In one paragraph

Article in Antiviral research, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.7field-weighted citation impact, top 35% 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

5 citing papers in PubMed, 9 citations in OpenAlex.

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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

7 authors at 3 institutions in 2 countries.

Oyebisi JegedeDepartment of Molecular Genetics, Section of Virology, Lerner Research Institute, Cleveland Clinic, Cleveland, OH, USA.
Ana Khodyakova
Mikhail Chernov
Jan Weber
Luis Menéndez-Arias
Andrei Gudkov
Miguel E Quiñones-Mateu
Cleveland Clinic Lerner College of Medicine · USConsejo Superior de Investigaciones Científicas · ESKent State University · US

Funding

WG3: HIV, Co-infections and Co-morbiditiesP30AI036219 · NIAID · CASE WESTERN RESERVE UNIVERSITY · PI Sharon L. Hillier, JONATHAN KARN · 1994 to 2026
$50.0M
HIV EVOLUTION AND ROLE OF CHEMOKINES IN THE LUNGK01HL067610 · NHLBI · CLEVELAND CLINIC LERNER COL/MED-CWRU · PI QUINONES-MATEU, MIGUEL E · 2000 to 2004
$660k
Effects of drug resistance mutations on HIV replicative fitnessR21AI071747 · NIAID · CASE WESTERN RESERVE UNIVERSITY · PI QUINONES-MATEU, MIGUEL E · 2007 to 2008
$421k
NHLBI NIH HHS HL-67610NHLBI NIH HHS K01 HL067610NIAID NIH HHS AI-36219NIAID NIH HHS P30 AI036219NIAID NIH HHS R21 AI071747
6 · The paper itself

Abstract

A cell-based drug screening system that utilizes a green fluorescent protein (GFP)-tagged recombinant lentiviral vector has been used to screen a chemical library of 34,000 small molecules for antiretroviral compounds. Thirty-three initial hits were analyzed and four compounds were selected based on their anti-human immunodeficiency virus type 1 (HIV-1) activity (EC(50) values ranging from 0.17 to 1.9 μM) and low cellular toxicity (CC(50) values >50 μM). The four compounds blocked reverse transcription and were able to inhibit the replication of a panel of different HIV-1 strains, including non-B subtype and viruses resistant to different drug classes. Serial in vitro passages of HIV-1(B-HXB2) in the presence of increasing drug concentrations selected for viruses with reduced susceptibility. Mutations previously associated with resistance to non-nucleoside reverse transcriptase (RT) inhibitors (L100I and Y181C for CBL-17 and CBL-21, respectively) or linked to nucleoside analogue resistance (A62V for CBL-4.0 and CBL-4.1) were identified. Viruses with reduced susceptibility to CBL-17 and CBL-21 but not the ones resistant to CBL-4.0 or CBL-4.1 showed a decrease in replicative fitness. Interestingly, two of the small molecules (CBL-4.0 and CBL-4.1) are indolopyridinones that were previously described as nucleotide-competing RT inhibitors.

Indexed as

Microbial Sensitivity TestsAnti-HIV AgentsCell LineDrug Resistance, ViralGreen Fluorescent ProteinsHigh-Throughput Screening AssaysHIV-1HIV Reverse TranscriptaseHumansMolecular WeightMutationReverse Transcriptase InhibitorsVirus ReplicationAnti-HIV AgentsGreen Fluorescent ProteinsHIV Reverse Transcriptasereverse transcriptase, Human immunodeficiency virus 1Reverse Transcriptase Inhibitors

Identifiers

PMID21600931
PMCPMC3144253
OpenAlexW2092322650

What OpenQuestion holds

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LicenceTDM
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.