Evidence map›Paper›PMID 25761614›Full record

ArticleJournal of medicinal chemistry2015

Structure-guided design and optimization of dipeptidyl inhibitors of norovirus 3CL protease. Structure-activity relationships and biochemical, X-ray crystallographic, cell-based, and in vivo studies.

Anushka C Galasiti Kankanamalage, Yunjeong Kim, Pathum M Weerawarna, Roxanne Adeline Z Uy, Vishnu C Damalanka, Sivakoteswara Rao Mandadapu, Kevin R Alliston, Nurjahan Mehzabeen, Kevin P Battaile, Scott Lovell and 2 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers.

0numbers the graph read from it
0cells of the map it votes in
37citing papers in PubMed
4.7field-weighted citation impact, top 5% 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

37 citing papers in PubMed, 53 citations in OpenAlex.

  1. Article
  2. Article
  3. Review
  4. Article
  5. PRSC chemical biology · 2023
    Review
  6. Article
  7. A Bibliometric Analysis of the Literature on Norovirus Disease from 1991-2021.International journal of environmental research and public health · 2022
    Article
  8. Structural similarities between SARS-CoV2 3CLFrontiers in chemistry · 2022
    Article
  9. Article
  10. Review
  11. Postinfection treatment with a protease inhibitor increases survival of mice with a fatal SARS-CoV-2 infection.Proceedings of the National Academy of Sciences of the United States of America · 2021
    Article
  12. Article
  13. Article
  14. Article
  15. Journal of structural biology: X · 2020
    Article
  16. Article
  17. Norovirus antivirals: Where are we now?Medicinal research reviews · 2019
    Review
  18. Review
  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

12 authors at 4 institutions in 1 country.

Anushka C Galasiti Kankanamalage†Department of Chemistry, Wichita State University, 1845 North Fairmount Avenue, Wichita, Kansas 67260, United States.
Yunjeong Kim
Pathum M Weerawarna†Department of Chemistry, Wichita State University, 1845 North Fairmount Avenue, Wichita, Kansas 67260, United States.
Roxanne Adeline Z Uy†Department of Chemistry, Wichita State University, 1845 North Fairmount Avenue, Wichita, Kansas 67260, United States.
Vishnu C Damalanka†Department of Chemistry, Wichita State University, 1845 North Fairmount Avenue, Wichita, Kansas 67260, United States.
Sivakoteswara Rao Mandadapu†Department of Chemistry, Wichita State University, 1845 North Fairmount Avenue, Wichita, Kansas 67260, United States.
Kevin R Alliston†Department of Chemistry, Wichita State University, 1845 North Fairmount Avenue, Wichita, Kansas 67260, United States.
Nurjahan Mehzabeen§Protein Structure Laboratory,The University of Kansas, Lawrence, Kansas 66047, United States.
Kevin P Battaile∥IMCA-CAT, Hauptman-Woodward Medical Research Institute, APS Argonne National Laboratory, Argonne, Illinois 60439, United States.
Scott Lovell§Protein Structure Laboratory,The University of Kansas, Lawrence, Kansas 66047, United States.
Kyeong-Ok Chang
William C Groutas†Department of Chemistry, Wichita State University, 1845 North Fairmount Avenue, Wichita, Kansas 67260, United States.
Wichita State University · USKansas State University · USUniversity of Kansas · USHauptman-Woodward Medical Research Institute · US

Funding

TRAFFICKING OF THE PLASMA MEMBRANE CA2+-ATPASE TO RAFTSP20RR017708 · NCRR · UNIVERSITY OF KANSAS LAWRENCE · PI FISCHER, CHRISTOPHER JAMES · 2002 to 2011
$20.1M
Norovirus 3CL Protease-Based Anti-norovirus TherapeuticsR01AI109039 · NIAID · KANSAS STATE UNIVERSITY · PI BOWLIN, TERRY L., CHANG, KYEONG-OK · 2014 to 2018
$3.7M
Protein Structure and FunctionP20GM103420 · NIGMS · UNIVERSITY OF KANSAS LAWRENCE · PI HANZLIK, ROBERT P · 2012 to 2012
$2.0M
NCRR NIH HHS 5P20RR017708-10NCRR NIH HHS P20 RR017708NIAID NIH HHS AI109039NIAID NIH HHS R01 AI109039NIGMS NIH HHS 8P20GM103420-10NIGMS NIH HHS P20 GM103420
6 · The paper itself

Abstract

Norovirus infection constitutes the primary cause of acute viral gastroenteritis. There are currently no vaccines or norovirus-specific antiviral therapeutics available for the management of norovirus infection. Norovirus 3C-like protease is essential for viral replication, consequently, inhibition of this enzyme is a fruitful avenue of investigation that may lead to the emergence of antinorovirus therapeutics. We describe herein the optimization of dipeptidyl inhibitors of norovirus 3C-like protease using iterative SAR, X-ray crystallographic, and enzyme and cell-based studies. We also demonstrate herein in vivo efficacy of an inhibitor using the murine model of norovirus infection.

Indexed as

AnimalsAntiviral AgentsCell LineChemistry Techniques, SyntheticCoronavirus 3C ProteasesCrystallography, X-RayCysteine EndopeptidasesDipeptidyl-Peptidase IV InhibitorsDose-Response Relationship, DrugDrug DesignFemaleMacrophagesMice, Inbred BALB CModels, MolecularNorovirusPeptide HydrolasesAntiviral AgentsCoronavirus 3C ProteasesCysteine EndopeptidasesDipeptidyl-Peptidase IV InhibitorsPeptide HydrolasesProtease InhibitorsViral Proteins

Identifiers

PMID25761614
PMCPMC4484267
OpenAlexW1964154549

What OpenQuestion holds

Textmetadata
LicenceTDM
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.