Evidence map›Paper›PMID 39415197›Full record

ArticleBiology direct2024

Characterization of the symmetrical benzimidazole twin drug TL1228: the role as viral entry inhibitor for fighting COVID-19.

Michela Murdocca, Osvaldo Andrade Santos-Filho, Claudia De Masi, Edivaldo Dos Santos Rodrigues, Claudia Valeria Campos de Souza, Riccardo De Santis, Donatella Amatore, Andrea Latini, Rossella Schipani, Lino di Rienzo Businco and 9 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Biology direct, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

19 authors.

Michela Murdocca *Department of Biomedicine and Prevention, University of Rome Tor Vergata, Rome, Italy.
Osvaldo Andrade Santos-Filho *Center of Health Sciences Laboratory of Molecular Modelling & Computational Strutural Biology Cidade Universitária, Federal University of Rio de Janeiro IPPN, Av. Carlos Chagas Filho373, Bloco H, Rio de Janeiro, 21941-599, RJ, Brazil.
Claudia De MasiDepartment of Biomedicine and Prevention, University of Rome Tor Vergata, Rome, Italy.
Edivaldo Dos Santos RodriguesCenter of Health Sciences Laboratory of Molecular Modelling & Computational Strutural Biology Cidade Universitária, Federal University of Rio de Janeiro IPPN, Av. Carlos Chagas Filho373, Bloco H, Rio de Janeiro, 21941-599, RJ, Brazil.
Claudia Valeria Campos de SouzaCenter of Health Sciences Laboratory of Molecular Modelling & Computational Strutural Biology Cidade Universitária, Federal University of Rio de Janeiro IPPN, Av. Carlos Chagas Filho373, Bloco H, Rio de Janeiro, 21941-599, RJ, Brazil.
Riccardo De SantisDepartment of Public Health and Infectious Diseases, University of Rome Sapienza, Rome, Italy.
Donatella AmatoreDefence Institute for Biomedical Sciences, Rome, 00184, Italy.
Andrea LatiniDepartment of Biomedicine and Prevention, University of Rome Tor Vergata, Rome, Italy.
Rossella SchipaniDepartment of Biomedicine and Prevention, University of Rome Tor Vergata, Rome, Italy.
Lino di Rienzo BusincoOtorhinolaryngology Department, Institute of Sport Medicine and Science CONI, Rome, Italy.
Bruno BrandimarteElectronic Measurements Physics Department, Sapienza University, Rome, Italy.
Giorgia GrilliDefence Institute for Biomedical Sciences, Rome, 00184, Italy.
Tien L HuangFormerly Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA, 70125, USA.
Annie S MayenceFormerly Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA, 70125, USA.
Florigio ListaDefence Institute for Biomedical Sciences, Rome, 00184, Italy.
Andrea DurantiDepartment of Biomolecular Sciences, University of Urbino Carlo Bo, Urbino, 61029, Italy.
Federica SangiuoloDepartment of Biomedicine and Prevention, University of Rome Tor Vergata, Rome, Italy. sangiuolo@med.uniroma2.it.
Jean Jacques Vanden EyndeFormerly Department of Organic Chemistry (FS), University of Mons-UMONS, 1 place du Parc, Mons, 7000, Belgium.
Giuseppe NovelliDepartment of Biomedicine and Prevention, University of Rome Tor Vergata, Rome, Italy.

Funding

ERC HORIZON-HLTL-2021 project "UNDINE" (101057100)Italian Ministry of Research MUR program PNRR M4-C2-I1.1 PRIN2022 "HECORES" (2022ZSLRPT)Nutrintech Med Italia (Rome, I) Prot. n°2885/2022
6 · The paper itself

Abstract

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is reliably one of the largest pandemics the world has suffered in recent years. In the search for non-biological antivirals, special emphasis was placed on drug repurposing to accelerate the clinical implementation of effective drugs.The life cycle of the virus has been extensively investigated and many human targets have been identified, such as the molecular chaperone GRP78, representing a host auxiliary factor for SARS-CoV-2 entry. Here we report the inhibitor capacity of TL1228, a small molecule discovered through an in silico screening approach, which could interfere with the interaction of SARS-CoV-2 and its target cells, blocking the recognition of the GRP78 cellular receptor by the viral Spike protein. TL1228 showed in vitro the ability to reduce significantly both pseudoviral and authentic viral activity even through the reduction of GRP78/ACE2 transcript levels. Importantly, TL1228 acts in modulating expression levels of innate immunity and as inflammation markers.

Indexed as

Antiviral AgentsBenzimidazolesCOVID-19 Drug TreatmentEndoplasmic Reticulum Chaperone BiPSARS-CoV-2Virus InternalizationAnimalsChlorocebus aethiopsCOVID-19Heat-Shock ProteinsHEK293 CellsHumansImmunity, InnateSpike Glycoprotein, CoronavirusAntiviral AgentsBenzimidazolesEndoplasmic Reticulum Chaperone BiPHeat-Shock ProteinsHSPA5 protein, humanSpike Glycoprotein, Coronavirusspike protein, SARS-CoV-23CLproBenzimidazole drugGRP78Molecular dockingMolecular dynamicsSARS-CoV-2

Identifiers

PMID39415197
PMCPMC11481581

What Socratic holds

Textmetadata
LicenceCC BY-NC-ND
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.