Evidence map›Paper›PMID 27235842›Full record

ArticleEuropean journal of medicinal chemistry2016

Structure-based design and synthesis of triazole-based macrocyclic inhibitors of norovirus protease: Structural, biochemical, spectroscopic, and antiviral studies.

Pathum M Weerawarna, Yunjeong Kim, Anushka C Galasiti Kankanamalage, Vishnu C Damalanka, Gerald H Lushington, Kevin R Alliston, Nurjahan Mehzabeen, Kevin P Battaile, Scott Lovell, Kyeong-Ok Chang and 1 more

Open access · greenAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.

0numbers the graph read from it
0cells of the map it votes in
23citing papers in PubMed
3.6field-weighted citation impact, top 8% 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

23 citing papers in PubMed, 36 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Article
  6. PRSC chemical biology · 2023
    Review
  7. Review
  8. Structural similarities between SARS-CoV2 3CLFrontiers in chemistry · 2022
    Article
  9. Article
  10. Structural and functional significance of the amino acid differences ValInternational journal of biological macromolecules · 2021
    Article
  11. Review
  12. Review
  13. Article
  14. Article
  15. Article
  16. Norovirus antivirals: Where are we now?Medicinal research reviews · 2019
    Review
  17. Review
  18. Article
  19. Article
  20. Article
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

11 authors at 4 institutions in 1 country.

Pathum M WeerawarnaDepartment of Chemistry, Wichita State University, Wichita, KS 67260, USA.
Yunjeong KimDepartment of Diagnostic Medicine & Pathobiology, College of Veterinary Medicine, Kansas State University, Manhattan, KS 66506, USA.
Anushka C Galasiti KankanamalageDepartment of Chemistry, Wichita State University, Wichita, KS 67260, USA.
Vishnu C DamalankaDepartment of Chemistry, Wichita State University, Wichita, KS 67260, USA.
Gerald H LushingtonLiS Consulting, Lawrence, KS 66046, USA.
Kevin R AllistonDepartment of Chemistry, Wichita State University, Wichita, KS 67260, USA.
Nurjahan MehzabeenProtein Structure Laboratory, The University of Kansas, Lawrence, KS 66047, USA.
Kevin P BattaileIMCA-CAT, Hauptman-Woodward Medical Research Institute, APS Argonne National Laboratory, Argonne, IL 60439, USA.
Scott LovellProtein Structure Laboratory, The University of Kansas, Lawrence, KS 66047, USA.
Kyeong-Ok ChangDepartment of Diagnostic Medicine & Pathobiology, College of Veterinary Medicine, Kansas State University, Manhattan, KS 66506, USA. Electronic address: kchang@vet.ksu.edu.
William C GroutasDepartment of Chemistry, Wichita State University, Wichita, KS 67260, USA. Electronic address: bill.groutas@wichita.edu.
Wichita State University · USKansas State University · USUniversity of Kansas · USHauptman-Woodward Medical Research Institute · US

Funding

Protein Structure Laboratory P30GM110761 · NIGMS · UNIVERSITY OF KANSAS LAWRENCE · PI HANZLIK, ROBERT P · 2014 to 2018
$5.6M
Norovirus 3CL Protease-Based Anti-norovirus TherapeuticsR01AI109039 · NIAID · KANSAS STATE UNIVERSITY · PI BOWLIN, TERRY L., CHANG, KYEONG-OK · 2014 to 2018
$3.7M
NIAID NIH HHS R01 AI109039NIGMS NIH HHS P30 GM110761
6 · The paper itself

Abstract

Outbreaks of acute gastroenteritis caused by noroviruses constitute a public health concern worldwide. To date, there are no approved drugs or vaccines for the management and prophylaxis of norovirus infections. A potentially effective strategy for the development of norovirus therapeutics entails the discovery of inhibitors of norovirus 3CL protease, an enzyme essential for noroviral replication. We describe herein the structure-based design of the first class of permeable, triazole-based macrocyclic inhibitors of norovirus 3C-like protease, as well as pertinent X-ray crystallographic, biochemical, spectroscopic, and antiviral studies.

Indexed as

Drug DesignChemistry Techniques, SyntheticMacrocyclic CompoundsMagnetic Resonance SpectroscopyModels, MolecularNorovirusPeptide HydrolasesPermeabilityProtease InhibitorsProtein ConformationTriazolesMacrocyclic CompoundsPeptide HydrolasesProtease InhibitorsTriazoles3CL proteaseMacrocyclic inhibitorsNorovirusβ-strand conformation

Identifiers

PMID27235842
PMCPMC4916972
OpenAlexW2344804652

What OpenQuestion 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 OpenQuestion graph.