Evidence map›Paper›PMID 40163818›Full record

ArticleJournal of medicinal chemistry2025

From N-0385 to N-0920: Unveiling a Host-Directed Protease Inhibitor with Picomolar Antiviral Efficacy against Prevalent SARS-CoV-2 Variants.

Gabriel Lemieux, Jimena Pérez-Vargas, Antoine Désilets, Malihe Hassanzadeh, Connor A H Thompson, Alice Gravel-Trudeau, Alexandre Joushomme, Siobhan Ennis, Ivan Villanueva, Étienne Marouseau and 8 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing 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

4 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
  4. 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

18 authors.

Gabriel LemieuxDepartment of Pharmacology-Physiology, Institut de Pharmacologie de Sherbrooke, Faculty of Medicine and Health Sciences, University of Sherbrooke, Sherbrooke J1H5N4, Quebec, Canada.ORCID 0000-0002-2313-5528
Jimena Pérez-VargasDepartment of Microbiology and Immunology, Life Sciences Institute, University of British Columbia, Vancouver V6T 1Z3, British Columbia, Canada.
Antoine DésiletsDepartment of Pharmacology-Physiology, Institut de Pharmacologie de Sherbrooke, Faculty of Medicine and Health Sciences, University of Sherbrooke, Sherbrooke J1H5N4, Quebec, Canada.ORCID 0000-0001-5081-5564
Malihe HassanzadehDepartment of Pharmacology-Physiology, Institut de Pharmacologie de Sherbrooke, Faculty of Medicine and Health Sciences, University of Sherbrooke, Sherbrooke J1H5N4, Quebec, Canada.
Connor A H ThompsonDepartment of Microbiology and Immunology, Life Sciences Institute, University of British Columbia, Vancouver V6T 1Z3, British Columbia, Canada.
Alice Gravel-TrudeauDepartment of Pharmacology-Physiology, Institut de Pharmacologie de Sherbrooke, Faculty of Medicine and Health Sciences, University of Sherbrooke, Sherbrooke J1H5N4, Quebec, Canada.
Alexandre JoushommeDepartment of Pharmacology-Physiology, Institut de Pharmacologie de Sherbrooke, Faculty of Medicine and Health Sciences, University of Sherbrooke, Sherbrooke J1H5N4, Quebec, Canada.
Siobhan EnnisFaculty of Health Sciences, Simon Fraser University, Burnaby J1H5N4, British Columbia, Canada.
Ivan VillanuevaDepartment of Microbiology and Immunology, Life Sciences Institute, University of British Columbia, Vancouver V6T 1Z3, British Columbia, Canada.
Étienne MarouseauDepartment of Pharmacology-Physiology, Institut de Pharmacologie de Sherbrooke, Faculty of Medicine and Health Sciences, University of Sherbrooke, Sherbrooke J1H5N4, Quebec, Canada.
Bryan J FraserDepartment of Medical Biophysics, University of Toronto, Toronto M5S 1A1, Ontario, Canada.ORCID 0000-0001-6398-106X
William ChampagneDepartment of Pharmacology-Physiology, Institut de Pharmacologie de Sherbrooke, Faculty of Medicine and Health Sciences, University of Sherbrooke, Sherbrooke J1H5N4, Quebec, Canada.
Matthieu LepageDepartment of Pharmacology-Physiology, Institut de Pharmacologie de Sherbrooke, Faculty of Medicine and Health Sciences, University of Sherbrooke, Sherbrooke J1H5N4, Quebec, Canada.
Masahiro NiikuraFaculty of Health Sciences, Simon Fraser University, Burnaby J1H5N4, British Columbia, Canada.
Cheryl H ArrowsmithDepartment of Medical Biophysics, University of Toronto, Toronto M5S 1A1, Ontario, Canada.ORCID 0000-0002-4971-3250
François JeanDepartment of Microbiology and Immunology, Life Sciences Institute, University of British Columbia, Vancouver V6T 1Z3, British Columbia, Canada.ORCID 0000-0002-6148-7460
Richard LeducDepartment of Pharmacology-Physiology, Institut de Pharmacologie de Sherbrooke, Faculty of Medicine and Health Sciences, University of Sherbrooke, Sherbrooke J1H5N4, Quebec, Canada.
Pierre-Luc BoudreaultDepartment of Pharmacology-Physiology, Institut de Pharmacologie de Sherbrooke, Faculty of Medicine and Health Sciences, University of Sherbrooke, Sherbrooke J1H5N4, Quebec, Canada.ORCID 0000-0002-2032-7970

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The worldwide spread of new SARS-CoV-2 variants emphasizes the need to diversify existing therapeutic strategies. TMPRSS2, a host protease crucial for SARS-CoV-2 entry, has garnered significant research attention as a potential target for therapeutic intervention. Here, we optimized N-0385, a previously reported TMPRSS2 ketobenzothiazole-based peptidomimetic inhibitor, by screening 135 derivatives for target affinity and antiviral potency. Among the top candidates, N-0695 exhibited low nanomolar

Indexed as

Antiviral AgentsCOVID-19 Drug TreatmentProtease InhibitorsSARS-CoV-2BenzothiazolesCOVID-19HumansMolecular Docking SimulationSerine EndopeptidasesStructure-Activity RelationshipSulfonamidesVirus Internalization(2S)-N-((2S)-1-(((2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)-2-(methanesulfonamido)pentanediamide)Antiviral AgentsBenzothiazolesProtease InhibitorsSerine EndopeptidasesSulfonamidesTMPRSS2 protein, human

Identifiers

PMID40163818
PMCPMC11998928

What OpenQuestion 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 OpenQuestion graph.