Evidence map›Paper›PMID 39933052›Full record

ReviewJournal of medicinal chemistry2025

Structural Chemistry of Helicase Inhibition.

Lakshi Selvaratnam, Timothy M Willson, Matthieu Schapira

Abstract readReview
In one paragraph

Review 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 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing 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

16 citing papers in PubMed.

  1. Review
  2. Article
  3. Article
  4. Article
  5. Article
  6. Article
  7. Article
  8. Review
  9. Review
  10. Article
  11. Article
  12. CACHE Challenge #2: Targeting the RNA Site of the SARS-CoV-2 Helicase Nsp13.Journal of chemical information and modeling · 2025
    Article
  13. Article
  14. Article
  15. Article
  16. 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

3 authors.

Lakshi SelvaratnamStructural Genomics Consortium, University of Toronto, Toronto, ON M5G 1L7, Canada.
Timothy M WillsonStructural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.ORCID 0000-0003-4181-8223
Matthieu SchapiraStructural Genomics Consortium, University of Toronto, Toronto, ON M5G 1L7, Canada.ORCID 0000-0002-1047-3309

Funding

Research Project 1: Coronavirus antiviral lead development and combination testingU19AI171292 · NIAID · UNIV OF NORTH CAROLINA CHAPEL HILL · PI BARIC, RALPH S, WILLSON, TIMOTHY M · 2022 to 2022
$65.5M
NIAID NIH HHS U19 AI171292
6 · The paper itself

Abstract

Helicases are essential motor enzymes that couple nucleoside-triphosphate hydrolysis with DNA or RNA strand unwinding. Helicases are integral to replication, transcription, splicing, and translation of the genome, play crucial roles in the proliferation of cancer cells and propagation of viral pathogens, and are implicated in neurodegenerative diseases. Despite their therapeutic potential, drug discovery efforts targeting helicases face significant challenges due to their dynamic enzymatic cycles, the transient nature of their conformational states, and the conservation of their active sites. Analysis of cocrystal structures of inhibitor-helicase complexes revealed four distinct mechanisms of inhibition: allosteric, ATP-competitive, RNA-competitive, and interfacial inhibitors. While these static X-ray structures reveal potential binding pockets that may support the development of selective drugs, the application of advanced techniques such as cryo-EM, single-molecule analysis, and computational modeling will be essential for understanding helicase dynamics and designing effective inhibitors.

Indexed as

Enzyme InhibitorsDNA HelicasesHumansModels, MolecularRNA HelicasesStructure-Activity RelationshipDNA HelicasesEnzyme InhibitorsRNA Helicases

Identifiers

PMID39933052
PMCPMC11873931

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.