Evidence map›Paper›PMID 18452606›Full record

ArticleVirology journal2008

Closing two doors of viral entry: intramolecular combination of a coreceptor- and fusion inhibitor of HIV-1.

Erhard Kopetzki, Andreas Jekle, Changhua Ji, Eileen Rao, Jun Zhang, Stephan Fischer, Nick Cammack, Surya Sankuratri, Gabrielle Heilek

Open access · goldAbstract read
In one paragraph

Article in Virology journal, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
1.1field-weighted citation impact, top 25% 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

16 citing papers in PubMed, 25 citations in OpenAlex.

  1. Article
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  9. Article
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  12. Potent strategy to inhibit HIV-1 by binding both gp120 and gp41.Antimicrobial agents and chemotherapy · 2011
    Article
  13. Article
  14. Article
  15. Progress towards recombinant anti-infective antibodies.Recent patents on anti-infective drug discovery · 2009
    Review
  16. Review
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

9 authors at 2 institutions in 1 country.

Erhard Kopetzki1Pharmaceuticals Division, Roche Penzberg, Penzberg, Germany. erhard.kopetzki@roche.com
Andreas Jekle
Changhua Ji
Eileen Rao
Jun Zhang
Stephan Fischer
Nick Cammack
Surya Sankuratri
Gabrielle Heilek
FX Palo Alto Laboratory · USRoche (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

We describe a novel strategy in which two inhibitors of HIV viral entry were incorporated into a single molecule. This bifunctional fusion inhibitor consists of an antibody blocking the binding of HIV to its co-receptor CCR5, and a covalently linked peptide which blocks envelope mediated virus-cell fusion. This novel bifunctional molecule is highly active on CCR5- and X4-tropic viruses in a single cycle assay and a reporter cell line with IC50 values of 0.03-0.05 nM. We demonstrated that both inhibitors contribute to the antiviral activity. In the natural host peripheral blood mononuclear cells (PBMC) the inhibition of CXCR4-tropic viruses is dependant on the co-expression of CCR5 and CXCR4 receptors. This bifunctional inhibitor may offer potential for improved pharmacokinetic parameters for a fusion inhibitor in humans and the combination of two active antiviral agents in one molecule may provide better durability in controlling the emergence of resistant viruses.

Indexed as

AnimalsCCR5 Receptor AntagonistsCell LineHIV-1HIV Fusion InhibitorsHumansInhibitory Concentration 50Membrane FusionMiceReceptors, CCR5Receptors, CXCR4Recombinant Fusion ProteinsVirus AttachmentVirus InternalizationCCR5 Receptor AntagonistsHIV Fusion InhibitorsReceptors, CCR5Receptors, CXCR4Recombinant Fusion Proteins

Identifiers

PMID18452606
PMCPMC2397382
OpenAlexW2097953079

What OpenQuestion holds

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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.