Evidence map›Paper›PMID 26985324›Full record

ArticleACS medicinal chemistry letters2016

Small-Molecule CD4-Mimics: Structure-Based Optimization of HIV-1 Entry Inhibition.

Bruno Melillo, Shuaiyi Liang, Jongwoo Park, Arne Schön, Joel R Courter, Judith M LaLonde, Daniel J Wendler, Amy M Princiotto, Michael S Seaman, Ernesto Freire and 4 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 68 papers.

0numbers the graph read from it
0cells of the map it votes in
68citing papers in PubMed
7.2field-weighted citation impact, top 3% 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

68 citing papers in PubMed, 103 citations in OpenAlex.

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  13. Antiviral Protein-Protein Interaction Inhibitors.Journal of medicinal chemistry · 2024
    Review
  14. Article
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8 more citing papers are in PubMed but not listed here.

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

14 authors at 4 institutions in 1 country.

Bruno MelilloDepartment of Chemistry, University of Pennsylvania , Philadelphia, Pennsylvania 19104, United States.
Shuaiyi LiangDepartment of Biochemistry and Molecular Biophysics and Department of Physiology and Cellular Biophysics, Columbia University , New York, New York 10032, United States.
Jongwoo ParkDepartment of Chemistry, University of Pennsylvania , Philadelphia, Pennsylvania 19104, United States.
Arne SchönDepartment of Biology, The Johns Hopkins University , Baltimore, Maryland 21218, United States.
Joel R CourterDepartment of Chemistry, University of Pennsylvania , Philadelphia, Pennsylvania 19104, United States.
Judith M LaLondeDepartment of Chemistry, Bryn Mawr College , Bryn Mawr, Pennsylvania 19010, United States.
Daniel J WendlerDepartment of Chemistry, University of Pennsylvania , Philadelphia, Pennsylvania 19104, United States.
Amy M PrinciottoDepartment of Cancer Immunology and Virology, Dana-Farber Cancer Institute, Center for Virology and Vaccine Research, Beth Israel Deaconess Medical Center, and Department of Microbiology and Immunobiology, Harvard Medical School , Boston, Massachusetts 02115, United States.
Michael S SeamanDepartment of Cancer Immunology and Virology, Dana-Farber Cancer Institute, Center for Virology and Vaccine Research, Beth Israel Deaconess Medical Center, and Department of Microbiology and Immunobiology, Harvard Medical School , Boston, Massachusetts 02115, United States.
Ernesto FreireDepartment of Biology, The Johns Hopkins University , Baltimore, Maryland 21218, United States.
Joseph SodroskiDepartment of Cancer Immunology and Virology, Dana-Farber Cancer Institute, Center for Virology and Vaccine Research, Beth Israel Deaconess Medical Center, and Department of Microbiology and Immunobiology, Harvard Medical School, Boston, Massachusetts 02115, United States; Department of Cancer Immunology and Virology, Dana-Farber Cancer Institute, Center for Virology and Vaccine Research, Beth Israel Deaconess Medical Center, and Department of Microbiology and Immunobiology, Harvard Medical School, Boston, Massachusetts 02115, United States; Department of Immunology and Infectious Diseases, Harvard School of Public Health, Boston, Massachusetts 02115, United States.
Navid MadaniDepartment of Cancer Immunology and Virology, Dana-Farber Cancer Institute, Center for Virology and Vaccine Research, Beth Israel Deaconess Medical Center, and Department of Microbiology and Immunobiology, Harvard Medical School , Boston, Massachusetts 02115, United States.
Wayne A HendricksonDepartment of Biochemistry and Molecular Biophysics and Department of Physiology and Cellular Biophysics, Columbia University, New York, New York 10032, United States; Department of Biochemistry and Molecular Biophysics and Department of Physiology and Cellular Biophysics, Columbia University, New York, New York 10032, United States.
Amos B SmithDepartment of Chemistry, University of Pennsylvania , Philadelphia, Pennsylvania 19104, United States.
University of Pennsylvania · USJohns Hopkins University · USBryn Mawr College · USHarvard University · US

Funding

Understanding Envelope Function in HIV-1 Infection: The Design, Synthesis and Validation of Small Molecule HIV-1 Env InhibitorsP01GM056550 · NIGMS · UNIVERSITY OF PENNSYLVANIA · PI ABRAMS, CAMERON F · 1997 to 2018
$31.2M
NIGMS NIH HHS P01 GM056550
6 · The paper itself

Abstract

The optimization, based on computational, thermodynamic, and crystallographic data, of a series of small-molecule ligands of the Phe43 cavity of the envelope glycoprotein gp120 of human immunodeficiency virus (HIV) has been achieved. Importantly, biological evaluation revealed that the small-molecule CD4 mimics (4-7) inhibit HIV-1 entry into target cells with both significantly higher potency and neutralization breadth than previous congeners, while maintaining high selectivity for the target virus. Their binding mode was characterized via thermodynamic and crystallographic studies.

Indexed as

CD4entry inhibitorgp120HIVprotein−protein interactionsstructure-based drug designthermodynamicsviral inhibitionX-ray crystallography

Identifiers

PMID26985324
PMCPMC4789667
OpenAlexW2318401834

What OpenQuestion holds

Textmetadata
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.