Evidence map›Paper›PMID 28038326›Full record

ArticleEuropean journal of medicinal chemistry2017

Design, synthesis, and evaluation of a novel series of macrocyclic inhibitors of norovirus 3CL protease.

Vishnu C Damalanka, Yunjeong Kim, Anushka C Galasiti Kankanamalage, Gerald H Lushington, Nurjahan Mehzabeen, Kevin P Battaile, Scott Lovell, Kyeong-Ok Chang, William C Groutas

Abstract read
In one paragraph

Article in European journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing 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

8 citing papers in PubMed.

  1. PRSC chemical biology · 2023
    Review
  2. Review
  3. Journal of structural biology: X · 2020
    Article
  4. Article
  5. Norovirus antivirals: Where are we now?Medicinal research reviews · 2019
    Review
  6. Article
  7. Review
  8. 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

9 authors.

Vishnu C DamalankaDepartment 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.
Gerald H LushingtonLiS Consulting, Lawrence, KS 66046, 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.

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

Norovirus infections have a major impact on public health worldwide, yet there is a current dearth of norovirus-specific therapeutics and prophylactics. This report describes the discovery of a novel class of macrocyclic inhibitors of norovirus 3C-like protease, a cysteine protease that is essential for virus replication. SAR, structural, and biochemical studies were carried out to ascertain the effect of structure on pharmacological activity and permeability. Insights gained from these studies have laid a solid foundation for capitalizing on the therapeutic potential of the series of inhibitors described herein.

Indexed as

Drug Design3C Viral ProteasesAnimalsChemistry Techniques, SyntheticCysteine EndopeptidasesDose-Response Relationship, DrugMacrocyclic CompoundsMiceMolecular Docking SimulationNorovirusPermeabilityProtease InhibitorsProtein ConformationRAW 264.7 CellsStructure-Activity RelationshipViral Proteins3C Viral ProteasesCysteine EndopeptidasesMacrocyclic CompoundsProtease InhibitorsViral Proteins3CLproteaseMacrocyclic inhibitorsNorovirus

Identifiers

PMID28038326
PMCPMC5296247

What OpenQuestion holds

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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.