Evidence map›Paper›PMID 32184972›Full record

ArticleACS medicinal chemistry letters2020

Optimization of Small Molecules That Sensitize HIV-1 Infected Cells to Antibody-Dependent Cellular Cytotoxicity.

Melissa C Grenier, Shilei Ding, Dani Vézina, Jean-Philippe Chapleau, William D Tolbert, Rebekah Sherburn, Arne Schön, Sambasivarao Somisetti, Cameron F Abrams, Marzena Pazgier and 2 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
0.6field-weighted citation impact, top 34% 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

6 citing papers in PubMed, 11 citations in OpenAlex.

  1. Article
  2. A Chemoselective Polarity-Mismatched Photocatalytic C(spAngewandte Chemie (International ed. in English) · 2023
    Article
  3. Article
  4. Article
  5. The Genesis and Future Prospects of Small Molecule HIV-1 Attachment Inhibitors.Advances in experimental medicine and biology · 2022
    Review
  6. 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

12 authors at 5 institutions in 2 countries.

Melissa C GrenierDepartment of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104, United States.
Shilei DingCentre de Recherche du CHUM, Montreal, Quebec, Canada.
Dani VézinaCentre de Recherche du CHUM, Montreal, Quebec, Canada.
Jean-Philippe ChapleauCentre de Recherche du CHUM, Montreal, Quebec, Canada.
William D TolbertInfections Diseases Division, Uniformed Services University of the Health Sciences, Bethesda, Maryland 20814, United States.
Rebekah SherburnInfections Diseases Division, Uniformed Services University of the Health Sciences, Bethesda, Maryland 20814, United States.
Arne SchönDepartment of Biology, The Johns Hopkins University, Baltimore, Maryland 21218, United States.
Sambasivarao SomisettiDepartment of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104, United States.
Cameron F AbramsDepartment of Chemical and Biological Engineering, Drexel University, Philadelphia, Pennsylvania 19104, United States.
Marzena PazgierInfections Diseases Division, Uniformed Services University of the Health Sciences, Bethesda, Maryland 20814, United States.
Andrés FinziCentre de Recherche du CHUM, Montreal, Quebec, Canada.
Amos B SmithDepartment of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104, United States.
Centre Hospitalier de l’Université de Montréal · CAUniformed Services University of the Health Sciences · USDrexel University · USUniversity of Pennsylvania · USJohns Hopkins University · US

Funding

Understanding Envelope Function in HIV-1 Infection: The Design, Synthesis and Validation of Small Molecule HIV-1 Env InhibitorsP01AI150471 · NIAID · DREXEL UNIVERSITY · PI HENDRICKSON, WAYNE A. · 2019 to 2022
$7.8M
Unlocking Envelope: A New Strategy for a Functional Cure Through Antibody-Dependent Cell-Mediated CytotoxicityR01AI129769 · NIAID · UNIVERSITY OF MARYLAND BALTIMORE · PI PAZGIER, MARZENA ELZBIETA · 2017 to 2021
$2.3M
Structural Targeting of Potentially Protective gp120 Epitopes in the C1/C2 RegionR01AI116274 · NIAID · UNIVERSITY OF MARYLAND BALTIMORE · PI PAZGIER, MARZENA ELZBIETA · 2016 to 2019
$1.5M
NIAID NIH HHS P01 AI150471NIAID NIH HHS R01 AI116274NIAID NIH HHS R01 AI129769
6 · The paper itself

Abstract

With approximately 37 million people living with HIV worldwide and an estimated 2 million new infections reported each year, the need to derive novel strategies aimed at eradicating HIV-1 infection remains a critical worldwide challenge. One potential strategy would involve eliminating infected cells via antibody-dependent cellular cytotoxicity (ADCC). HIV-1 has evolved sophisticated mechanisms to conceal epitopes located in its envelope glycoprotein (Env) that are recognized by ADCC-mediating antibodies present in sera from HIV-1 infected individuals. Our aim is to circumvent this evasion via the development of small molecules that expose relevant anti-Env epitopes and sensitize HIV-1 infected cells to ADCC. Rapid elaboration of an initial screening hit using parallel synthesis and structure-based optimization has led to the development of potent small molecules that elicit this humoral response. Efforts to increase the ADCC activity of this class of small molecules with the aim of increasing their therapeutic potential was based on our recent cocrystal structures with gp120 core.

Identifiers

PMID32184972
PMCPMC7074219
OpenAlexW2988428941

What Socratic 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 Socratic graph.