Evidence map›Paper›PMID 36298823›Full record

ArticleViruses2022

Comparative Pharmacokinetics of a Dual Inhibitor of HIV-1, NBD-14189, in Rats and Dogs with a Proof-of-Concept Evaluation of Antiviral Potency in SCID-hu Mouse Model.

Cheryl A Stoddart, Francesca Curreli, Stephen Horrigan, Andrea Altieri, Alexander V Kurkin, Asim K Debnath

Open access · goldAbstract read
In one paragraph

Article in Viruses, 2022. 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
0.1field-weighted citation impact, top 59% 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

1 citing paper in PubMed, 1 citations in OpenAlex.

  1. Antiviral Activity and Crystal Structures of HIV-1 gp120 Antagonists.International journal of molecular sciences · 2022
    Article
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

6 authors at 3 institutions in 1 country.

Cheryl A StoddartDivision of Experimental Medicine, Department of Medicine, Zuckerberg San Francisco General Hospital, University of California, San Francisco, CA 94110, USA.ORCID 0000-0002-7024-6044
Francesca CurreliLaboratory of Molecular Modeling & Drug Design, New York Blood Center, Lindsley F. Kimball Research Institute, 310 E 67th Street, New York, NY 10065, USA.
Stephen HorriganNoble Life Sciences Inc., Woodbine, MD 21784, USA.
Andrea AltieriEDASA Scientific srls, Via Stingi 37, 66050 San Salvo, Italy.ORCID 0000-0002-9815-9866
Alexander V KurkinEDASA Scientific srls, Via Stingi 37, 66050 San Salvo, Italy.
Asim K DebnathLaboratory of Molecular Modeling & Drug Design, New York Blood Center, Lindsley F. Kimball Research Institute, 310 E 67th Street, New York, NY 10065, USA.ORCID 0000-0003-2761-0506
New York Blood Center · USNoble Life Sciences (United States) · USSan Francisco General Hospital · US

Funding

Design of inhibitors targeted to the CD4 binding site on HIV-1 gp120R01AI104416 · NIAID · NEW YORK BLOOD CENTER · PI DEBNATH, ASIM K · 2013 to 2022
$7.9M
NIAID NIH HHS HHSN272201400002CNIAID NIH HHS R01 AI104416NIH HHS R01 AI104416
6 · The paper itself

Abstract

We earlier reported substantial progress in designing gp120 antagonists. Notably, we discovered that NBD-14189 is not only the most active gp120 antagonist but also shows antiviral activity against HIV-1 Reverse Transcriptase (RT). We also confirmed its binding to HIV-1 RT by X-ray crystallography. The dual inhibition is highly significant because, intriguingly, this compound bridges the dNTP and NNRTI-binding sites and inhibits the polymerase activity of isolated RT in the enzymatic assay. This novel finding is expected to lead to new avenues in designing a novel class of HIV-1 dual inhibitors. Therefore, we needed to advance this inhibitor to preclinical assessment. To this end, we report the pharmacokinetics (PK) study of NBD-14189 in rats and dogs. Subsequently, we assessed the toxicity and therapeutic efficacy in vivo in the SCID-hu Thy/Liv mouse model. The PK data indicated a favorable half-life (t

Indexed as

Anti-HIV AgentsHIV-1HIV InfectionsHIV SeropositivityAnimalsDisease Models, AnimalDogsHumansMiceMice, SCIDRatsAnti-HIV Agentsbioavailabilitydual inhibitorsHIV-1 gp120 antagonisthuman immunodeficiency virus type 1 (HIV-1)pharmacokinetics (PK)SCID-hu mouse model

Identifiers

PMID36298823
PMCPMC9611370
OpenAlexW4306404306

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.