Evidence map›Paper›PMID 27620483›Full record

ArticleAntimicrobial agents and chemotherapy2016

A Modified P1 Moiety Enhances In Vitro Antiviral Activity against Various Multidrug-Resistant HIV-1 Variants and In Vitro Central Nervous System Penetration Properties of a Novel Nonpeptidic Protease Inhibitor, GRL-10413.

Masayuki Amano, Pedro Miguel Salcedo-Gómez, Rui Zhao, Ravikiran S Yedidi, Debananda Das, Haydar Bulut, Nicole S Delino, Venkata Reddy Sheri, Arun K Ghosh, Hiroaki Mitsuya

Abstract read
In one paragraph

Article in Antimicrobial agents and chemotherapy, 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
–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

10 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Novel Protease Inhibitors Containing C-5-ModifiedAntimicrobial agents and chemotherapy · 2019
    Article
  6. Article
  7. Article
  8. Article
  9. Article
  10. 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

10 authors.

Masayuki AmanoDepartments of Infectious Diseases and Hematology, Kumamoto University School of Medicine, Kumamoto, Japan.ORCID 0000-0003-0516-9502
Pedro Miguel Salcedo-GómezDepartments of Infectious Diseases and Hematology, Kumamoto University School of Medicine, Kumamoto, Japan.
Rui ZhaoDepartments of Infectious Diseases and Hematology, Kumamoto University School of Medicine, Kumamoto, Japan.
Ravikiran S YedidiExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA.ORCID 0000-0003-2755-1307
Debananda DasExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA.
Haydar BulutExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA.
Nicole S DelinoExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA.
Venkata Reddy SheriDepartments of Chemistry and Medicinal Chemistry, Purdue University, West Lafayette, Indiana, USA.
Arun K GhoshDepartments of Chemistry and Medicinal Chemistry, Purdue University, West Lafayette, Indiana, USA.
Hiroaki MitsuyaDepartments of Infectious Diseases and Hematology, Kumamoto University School of Medicine, Kumamoto, Japan hm21q@nih.gov.

Funding

Design & Synthesis of Nonpeptide Protease InhibitorsR37GM053386 · NIGMS · PURDUE UNIVERSITY · PI GHOSH, ARUN K · 2011 to 2018
$3.9M
DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORSR01GM053386 · NIGMS · UNIVERSITY OF ILLINOIS AT CHICAGO · PI GHOSH, ARUN K · 1995 to 2010
$3.7M
Study of HIV Protease Dimerization (PD) and Identification of PD InhibitorsZIABC011105 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI MITSUYA, HIROAKI · 2009 to 2017
$1.6M
NIGMS NIH HHS R01 GM053386NIGMS NIH HHS R37 GM053386
6 · The paper itself

Abstract

We report here that GRL-10413, a novel nonpeptidic HIV-1 protease inhibitor (PI) containing a modified P1 moiety and a hydroxyethylamine sulfonamide isostere, is highly active against laboratory HIV-1 strains and primary clinical isolates (50% effective concentration [EC

Indexed as

AnimalsBlood-Brain BarrierCarbamatesCell LineCentral Nervous SystemCrystallography, X-RayDarunavirDrug Evaluation, PreclinicalDrug Resistance, Multiple, ViralEthylaminesFuransHIV-1HIV ProteaseHIV Protease InhibitorsHumansLopinaviramprenavirCarbamatesDarunavirEthylaminesFuransGRL-10413HIV ProteaseHIV Protease InhibitorsLopinavirp16 protease, Human immunodeficiency virus 1PeptidesSulfonamides

Identifiers

PMID27620483
PMCPMC5118983

What OpenQuestion holds

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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.