Evidence map›Paper›PMID 23994876›Full record

ArticleAntiviral chemistry & chemotherapy2014

Characterization of permeability, stability and anti-HIV-1 activity of decitabine and gemcitabine divalerate prodrugs.

Christine L Clouser, Laurent Bonnac, Louis M Mansky, Steven E Patterson

Abstract read
In one paragraph

Article in Antiviral chemistry & chemotherapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
0.7field-weighted citation impact, top 29% 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

9 citing papers in PubMed, 14 citations in OpenAlex.

  1. Article
  2. Review
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  6. Di-International journal of nanomedicine · 2019
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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

4 authors at 1 institution in 1 country.

Christine L ClouserInstitute for Molecular Virology, University of Minnesota, Minneapolis, MN, USA. cclouser@umn.edu.
Laurent Bonnac
Louis M Mansky
Steven E Patterson
University of Minnesota · US

Funding

Mechanisms of HIV-1 VariationR01GM056615 · NIGMS · UNIVERSITY OF MINNESOTA TWIN CITIES · PI MANSKY, LOUIS M. · 2003 to 2011
$2.6M
HIV Reverse Transcriptase-Mediated MutagenesisR01GM105876 · NIGMS · UNIVERSITY OF MINNESOTA · PI KIM, BAEK, MANSKY, LOUIS M. · 2013 to 2016
$2.4M
NIGMS NIH HHS R01 GM056615NIGMS NIH HHS R01 GM105876NIGMS NIH HHS R01 GM56615
6 · The paper itself

Abstract

backgroundOver 25 drugs have been approved for the treatment of HIV-1 replication. All but one of these drugs is delivered as an oral medication. Previous studies have demonstrated that two drugs, decitabine and gemcitabine, have potent anti-HIV-1 activities and can work together in synergy to reduce HIV-1 infectivity via lethal mutagenesis. For their current indications, decitabine and gemcitabine are delivered intravenously.

methodsAs an initial step towards the clinical translation of these drugs for the treatment of HIV-1 infection, we synthesized decitabine and gemcitabine prodrugs in order to increase drug permeability, which has generally been shown to correlate with increased bioavailability in vivo. In the present study we investigated the permeability, stability and anti-HIV-1 activity of decitabine and gemcitabine prodrugs and selected the divalerate esters of each as candidates for further investigation.

resultsOur results provide the first demonstration of divalerate prodrugs of decitabine and gemcitabine that are readily permeable, stable and possess anti-HIV-1 activity.

conclusionsThese observations predict improved oral availability of decitabine and gemcitabine, and warrant further study of their ability to reduce HIV-1 infectivity in vivo.

Indexed as

Anti-HIV AgentsAzacitidineBiological AvailabilityCaco-2 CellsCell ProliferationDecitabineDeoxycytidineDrug StabilityGemcitabineHalf-LifeHEK293 CellsHIV-1HumansHydrogen-Ion ConcentrationPermeabilityProdrugsAnti-HIV AgentsAzacitidineDecitabineDeoxycytidineGemcitabineProdrugs

Identifiers

PMID23994876
PMCPMC4489529
OpenAlexW2104373350

What OpenQuestion holds

Textmetadata
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.