Evidence map›Paper›PMID 27568924›Full record

ArticleAntiviral research2016

Preclinical evaluation of a mercaptobenzamide and its prodrug for NCp7-targeted inhibition of human immunodeficiency virus.

T L Hartman, L Yang, A N Helfrick, M Hassink, N I Shank, K George Rosenker, M T Scerba, M Saha, E Hughes, A Q Wang and 4 more

Abstract readEvaluation Study
PubMed Full text at PMC Publisher
In one paragraph

Article in Antiviral research, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
1.1field-weighted citation impact, top 22% 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

10 citing papers in PubMed, 16 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

14 authors at 3 institutions in 1 country.

T L HartmanImQuest Biosciences, Frederick, MD, USA.
L YangImQuest Biosciences, Frederick, MD, USA.
A N HelfrickImQuest Biosciences, Frederick, MD, USA.
M HassinkLaboratory of Bioorganic Chemistry, NIDDK, NIH, Bethesda, MD, USA.
N I ShankLaboratory of Bioorganic Chemistry, NIDDK, NIH, Bethesda, MD, USA.
K George RosenkerLaboratory of Bioorganic Chemistry, NIDDK, NIH, Bethesda, MD, USA.
M T ScerbaLaboratory of Bioorganic Chemistry, NIDDK, NIH, Bethesda, MD, USA.
M SahaLaboratory of Bioorganic Chemistry, NIDDK, NIH, Bethesda, MD, USA.
E HughesNCATS, NIH, Bethesda, MD, USA.
A Q WangNCATS, NIH, Bethesda, MD, USA.
X XuNCATS, NIH, Bethesda, MD, USA.
P GuptaLaboratory of Bioorganic Chemistry, NIDDK, NIH, Bethesda, MD, USA.
R W BuckheitImQuest Biosciences, Frederick, MD, USA. Electronic address: rbuckheit@imquestbio.com.
D H AppellaLaboratory of Bioorganic Chemistry, NIDDK, NIH, Bethesda, MD, USA. Electronic address: appellad@niddk.nih.gov.
National Institutes of Health · USImQuest BioSciences (United States) · USNational Center for Advancing Translational Sciences · US

Funding

Small Molecular Inactivators of HIVZIADK075135 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI APPELLA, DANIEL H · 2016 to 2025
$7.2M
6 · The paper itself

Abstract

Although the effective use of highly active antiretroviral therapy results in the suppression of virus production in infected individuals, it does not eliminate the infection and low level virus production in cells harboring virus in sanctuary sites. Thus, the continued search for new antiretroviral agents with unique and different mechanisms of HIV inhibition remains critical, and compounds that can reduce the level of virus production from cells already infected with HIV, as opposed to preventing de novo infection, would be of great benefit. A mercaptobenzamide (MDH-1-38) and its prodrug (NS1040) are being developed as potential therapeutic compounds targeting the zinc finger of HIV nucleocapsid. In the presence of esterase enzymes, NS1040 is designed to be converted to MDH-1-38 which has antiviral activity. While we presume that NS1040 is rapidly converted to MDH-1-38 in all experiments, the two compounds were tested side-by-side to determine whether the presence of a prodrug affects the antiviral activity or mechanism of action. The two compounds were evaluated against a panel of HIV-1 clinical isolates in human PBMCs and monocyte-macrophages and yielded EC

Indexed as

Anti-HIV AgentsBenzimidazolesDrug DiscoveryDrug Evaluation, PreclinicalDrug Resistance, Viralgag Gene Products, Human Immunodeficiency VirusHIV-1HIV InfectionsHumansMacrophagesMonocytesProdrugsVirus ReplicationAnti-HIV AgentsBenzimidazolesgag Gene Products, Human Immunodeficiency VirusNCP7 protein, Human immunodeficiency virus 1Prodrugs

Identifiers

PMID27568924
PMCPMC7113734
OpenAlexW2514344893

What OpenQuestion holds

Textmetadata
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.