Evidence map›Paper›PMID 26823007›Full record

ArticleJournal of medicinal chemistry2016

Oxadiazole-Based Cell Permeable Macrocyclic Transition State Inhibitors of Norovirus 3CL Protease.

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

Abstract read
In one paragraph

Article in 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 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing 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

14 citing papers in PubMed.

  1. Article
  2. Structural similarities between SARS-CoV2 3CLFrontiers in chemistry · 2022
    Article
  3. Article
  4. Article
  5. Review
  6. Article
  7. Norovirus antivirals: Where are we now?Medicinal research reviews · 2019
    Review
  8. Review
  9. Review
  10. Article
  11. Article
  12. Structure-based exploration and exploitation of the SEuropean journal of medicinal chemistry · 2017
    Article
  13. Article
  14. 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.

Vishnu C DamalankaDepartment of Chemistry, Wichita State University , Wichita, Kansas 67260, United States.
Yunjeong KimDepartment of Diagnostic Medicine and Pathobiology, College of Veterinary Medicine, Kansas State University , Manhattan, Kansas 66506, United States.
Kevin R AllistonDepartment of Chemistry, Wichita State University , Wichita, Kansas 67260, United States.
Pathum M WeerawarnaDepartment of Chemistry, Wichita State University , Wichita, Kansas 67260, United States.
Anushka C Galasiti KankanamalageDepartment of Chemistry, Wichita State University , Wichita, Kansas 67260, United States.
Gerald H LushingtonLiS Consulting , Lawrence, Kansas 66046, United States.
Nurjahan MehzabeenProtein Structure Laboratory, The University of Kansas , Lawrence, Kansas 66047, United States.
Kevin P BattaileIMCA-CAT, Hauptman-Woodward Medical Research Institute, APS Argonne National Laboratory, Argonne, Illinois 60439, United States.
Scott LovellProtein Structure Laboratory, The University of Kansas , Lawrence, Kansas 66047, United States.
Kyeong-Ok ChangDepartment of Diagnostic Medicine and Pathobiology, College of Veterinary Medicine, Kansas State University , Manhattan, Kansas 66506, United States.
William C GroutasDepartment of Chemistry, Wichita State University , Wichita, Kansas 67260, United States.

Funding

TRAFFICKING OF THE PLASMA MEMBRANE CA2+-ATPASE TO RAFTSP20RR017708 · NCRR · UNIVERSITY OF KANSAS LAWRENCE · PI HOLYOAK, TODD · 2002 to 2011
$20.1M
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
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 R01 AI109039NIGMS NIH HHS 8P20GM103420-10NIGMS NIH HHS P20 GM103420NIGMS NIH HHS P30 GM110761
6 · The paper itself

Abstract

Human noroviruses are the primary causative agents of acute gastroenteritis and a pressing public health burden worldwide. There are currently no vaccines or small molecule therapeutics available for the treatment or prophylaxis of norovirus infections. Norovirus 3CL protease plays a vital role in viral replication by generating structural and nonstructural proteins via the cleavage of the viral polyprotein. Thus, molecules that inhibit the viral protease may have potential therapeutic value. We describe herein the structure-based design, synthesis, and in vitro and cell-based evaluation of the first class of oxadiazole-based, permeable macrocyclic inhibitors of norovirus 3CL protease.

Indexed as

Cell Membrane PermeabilityAnimalsAntiviral AgentsCell LineCrystallography, X-RayDose-Response Relationship, DrugHumansMacrocyclic CompoundsMiceModels, MolecularMolecular StructureNorovirusOxadiazolesPeptide HydrolasesProtease InhibitorsStructure-Activity RelationshipAntiviral AgentsMacrocyclic CompoundsOxadiazolesPeptide HydrolasesProtease Inhibitors

Identifiers

PMID26823007
PMCPMC5156532

What OpenQuestion holds

Textmetadata
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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.