Evidence map›Paper›PMID 22424973›Full record

ArticleBioorganic & medicinal chemistry letters2012

Discovery of HIV fusion inhibitors targeting gp41 using a comprehensive α-helix mimetic library.

Landon R Whitby, Kristopher E Boyle, Lifeng Cai, Xiaoqian Yu, Miriam Gochin, Dale L Boger

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing 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

14 citing papers in PubMed.

  1. Article
  2. Article
  3. Enhanced potency of bivalent small molecule gp41 inhibitors.Bioorganic & medicinal chemistry · 2017
    Article
  4. Article
  5. Article
  6. A review on recent developments of indole-containing antiviral agents.European journal of medicinal chemistry · 2015
    Review
  7. Article
  8. Article
  9. Article
  10. Article
  11. Review
  12. Review
  13. Article
  14. 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.

Landon R WhitbyDepartment of Chemistry, Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, United States.
Kristopher E Boyle
Lifeng Cai
Xiaoqian Yu
Miriam Gochin
Dale L Boger

Funding

ANTITUMORE ANTIBIOTICS: STREPTONIGRIN AND LAVENDAMYCINR01CA042056 · NCI · SCRIPPS RESEARCH INSTITUTE, THE · PI BOGER, DALE L · 1985 to 2024
$10.6M
Structure-based discovery and development of HIV-1 gp41 fusion inhibitorsR01GM087998 · NIGMS · TOURO UNIVERSITY OF CALIFORNIA · PI GOCHIN, MIRIAM · 2010 to 2013
$1.1M
High-Throughput Screening for Human Immunodeficiency Virus Fusion InhibitorsR21NS059403 · NINDS · TOURO UNIVERSITY OF CALIFORNIA · PI GOCHIN, MIRIAM · 2007 to 2008
$245k
NCI NIH HHS CA42056NCI NIH HHS R01 CA042056NIGMS NIH HHS GM87998NIGMS NIH HHS R01 GM087998NINDS NIH HHS NS59403NINDS NIH HHS R21 NS059403
6 · The paper itself

Abstract

The evaluation of a comprehensive α-helix mimetic library for binding the gp41 NHR hydrophobic pocket recognizing an intramolecular CHR α-helix provided a detailed depiction of structural features required for binding and led to the discovery of small molecule inhibitors (K(i) 0.6-1.3 μM) that not only match or exceed the potency of those disclosed over the past decade, but that also exhibit effective activity in a cell-cell fusion assay (IC(50) 5-8 μM).

Indexed as

Drug DiscoveryMolecular MimicryAnti-HIV AgentsHIV Envelope Protein gp41HIV Fusion InhibitorsHumansHydrophobic and Hydrophilic InteractionsInhibitory Concentration 50Models, MolecularMolecular StructureProtein Structure, SecondarySmall Molecule LibrariesAnti-HIV AgentsHIV Envelope Protein gp41HIV Fusion InhibitorsSmall Molecule Libraries

Identifiers

PMID22424973
PMCPMC3321071

What OpenQuestion holds

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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.