Evidence map›Paper›PMID 40356906›Full record

ArticleFrontiers in immunology2025

SuFEx-enabled high-throughput medicinal chemistry for developing potent tamoxifen analogs as Ebola virus entry inhibitors.

Lucas Dada, Emiko Nagai, Sashank Agrawal, Ariel S Wirchnianski, Ian A Wilson, Kartik Chandran, Seiya Kitamura

Abstract read
In one paragraph

Article in Frontiers in immunology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing 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

5 citing papers in PubMed.

  1. Review
  2. Article
  3. Review
  4. Article
  5. Virus infection and vesicle trafficking.Frontiers in immunology · 2025
    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

7 authors.

Lucas Dada *Department of Biochemistry, Albert Einstein College of Medicine, Bronx, NY, United States.
Emiko Nagai *Department of Biochemistry, Albert Einstein College of Medicine, Bronx, NY, United States.
Sashank Agrawal *Department of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, CA, United States.
Ariel S WirchnianskiDepartment of Microbiology & Immunology, Albert Einstein College of Medicine, Bronx, NY, United States.
Ian A WilsonDepartment of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, CA, United States.
Kartik ChandranDepartment of Microbiology & Immunology, Albert Einstein College of Medicine, Bronx, NY, United States.
Seiya KitamuraDepartment of Biochemistry, Albert Einstein College of Medicine, Bronx, NY, United States.

Funding

WORD PROCESSORP30CA013330 · NCI · YESHIVA UNIVERSITY · PI Ulrich Steidl · 1985 to 2026
$111.2M
X-ray Absorption Spectroscopy (XAS) pp.711-759P41GM103393 · NIGMS · STANFORD UNIVERSITY · PI HODGSON, KEITH O · 2012 to 2019
$30.6M
Expanding the chemical probe development paradigm toward underexplored targetsR35GM155249 · NIGMS · ALBERT EINSTEIN COLLEGE OF MEDICINE · PI Seiya Kitamura · 2024 to 2026
$1.3M
Console and probe upgrade for 600 MHz NMRS10OD016305 · OD · ALBERT EINSTEIN COLLEGE OF MEDICINE · PI COWBURN, DAVID · 2014 to 2014
$595k
A universal high-throughput platform to improve biological functions of small moleculesR00GM138758 · NIGMS · ALBERT EINSTEIN COLLEGE OF MEDICINE · PI KITAMURA, SEIYA · 2022 to 2023
$497k
NCI NIH HHS P30 CA013330NIGMS NIH HHS P41 GM103393NIGMS NIH HHS R00 GM138758NIGMS NIH HHS R35 GM155249NIH HHS S10 OD016305
6 · The paper itself

Abstract

Ebola virus (EBOV) causes severe hemorrhagic fever with a high mortality rate in humans. In acute infection, an abnormal immune response results in excessive inflammatory cytokines and uncontrolled systemic inflammation that can result in organ damage and multi-organ failure. While vaccines and monoclonal antibody therapies are available, there is an urgent need for effective small-molecule antivirals against EBOV. Here, we report on the optimization of tamoxifen, an EBOV-glycoprotein (GP) binder that inhibits viral entry, using our Sulfur-Fluoride Exchange (SuFEx) click chemistry-based high-throughput medicinal chemistry (HTMC) strategy. Using a "Direct-to-Biology" approach, we generated a focused library of 2,496 tamoxifen analogs overnight and screened them in a cell-based pseudo-EBOV infection assay. The HTMC workflow enabled the development of a potent EBOV entry inhibitor with submicromolar EC

Indexed as

Antiviral AgentsEbolavirusHemorrhagic Fever, EbolaTamoxifenVirus InternalizationAnimalsChemistry, PharmaceuticalChlorocebus aethiopsClick ChemistryHigh-Throughput Screening AssaysHumansVero CellsAntiviral AgentsTamoxifendirect-to-biologydrug discoveryEbolasmall molecule antiviral drugsSuFEx

Identifiers

PMID40356906
PMCPMC12066687

What OpenQuestion holds

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LicenceCC BY
Read underepoch 390

Registered trials

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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.