Evidence map›Paper›PMID 29227928›Full record

ArticleEuropean journal of medicinal chemistry2018

Structure-guided design, synthesis and evaluation of oxazolidinone-based inhibitors of norovirus 3CL protease.

Vishnu C Damalanka, Yunjeong Kim, Anushka C Galasiti Kankanamalage, Athri D Rathnayake, Nurjahan Mehzabeen, Kevin P Battaile, Scott Lovell, Harry Nhat Nguyen, Gerald H Lushington, Kyeong-Ok Chang and 1 more

Open access · greenAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2018. 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
0.6field-weighted citation impact, top 31% 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

4 citing papers in PubMed, 11 citations in OpenAlex.

  1. Observational
  2. Article
  3. Article
  4. Norovirus antivirals: Where are we now?Medicinal research reviews · 2019
    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

11 authors at 4 institutions in 1 country.

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.
Athri D RathnayakeDepartment 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.
Harry Nhat NguyenDepartment of Chemistry, Wichita State University, Wichita, KS 67260, USA.
Gerald H LushingtonLiS Consulting, Lawrence, KS 66046, 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 · USArgonne National Laboratory · 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

Acute nonbacterial gastroenteritis caused by noroviruses constitutes a global public health concern and a significant economic burden. There are currently no small molecule therapeutics or vaccines for the treatment of norovirus infections. A structure-guided approach was utilized in the design of a series of inhibitors of norovirus 3CL protease that embody an oxazolidinone ring as a novel design element for attaining optimal binding interactions. Low micromolar cell-permeable inhibitors that display anti-norovirus activity have been identified. The mechanism of action, mode of binding, and structural rearrangements associated with the interaction of the inhibitors and the enzyme were elucidated using X-ray crystallography.

Indexed as

3C Viral ProteasesCrystallography, X-RayCysteine EndopeptidasesDose-Response Relationship, DrugModels, MolecularMolecular StructureNorovirusOxazolidinonesProtease InhibitorsStructure-Activity RelationshipViral Proteins3C Viral ProteasesCysteine EndopeptidasesOxazolidinonesProtease InhibitorsViral Proteins

Identifiers

PMID29227928
PMCPMC5737831
OpenAlexW2772401016

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.