Evidence map›Paper›PMID 24918716›Full record

ArticleJournal of medicinal chemistry2014

Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting.

Major Gooyit, Nancy Tricoche, Sara Lustigman, Kim D Janda

Open access · bronzeAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
2.0field-weighted citation impact, top 13% 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

11 citing papers in PubMed, 33 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Structure-based virtual screening of highly potent inhibitors of the nematode chitinaseJournal of enzyme inhibition and medicinal chemistry · 2021
    Article
  6. Article
  7. Chitinases: Therapeutic Scaffolds for Allergy and Inflammation.Recent patents on inflammation & allergy drug discovery · 2020
    Review
  8. Article
  9. Article
  10. Article
  11. 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

4 authors at 2 institutions in 1 country.

Major GooyitDepartments of Chemistry and Immunology and Microbial Science, The Skaggs Institute for Chemical Biology, and The Worm Institute of Research and Medicine, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Nancy Tricoche
Sara Lustigman
Kim D Janda
New York Blood Center · USScripps Research Institute · US

Funding

Exploration of Chitinase Inhibitors for Human HealthR21AI092076 · NIAID · SCRIPPS RESEARCH INSTITUTE, THE · PI JANDA, KIM · 2013 to 2014
$521k
NIAID NIH HHS AI092076NIAID NIH HHS R21 AI092076
6 · The paper itself

Abstract

The L3-stage-specific chitinase OvCHT1 has been implicated in the development of Onchocerca volvulus, the causative agent of onchocerciasis. Closantel, a known anthelmintic drug, was previously discovered as a potent and specific OvCHT1 inhibitor. As closantel is also a known protonophore, we performed a simple scaffold modulation to map out the structural features that are relevant for its individual or dual biochemical roles. Furthermore, we present that either OvCHT1 inhibition or protonophoric activity was capable of affecting O. volvulus L3 molting and that the presence of both activities in a single molecule yielded more potent inhibition of the nematode's developmental process.

Indexed as

AnimalsAntinematodal AgentsCaenorhabditis elegansChitinasesEnzyme InhibitorsIonophoresMoltingOnchocerca volvulusOnchocerciasisSalicylanilidesStructure-Activity RelationshipUncoupling AgentsAntinematodal AgentsChitinasesclosantelEnzyme InhibitorsIonophoresSalicylanilidesUncoupling Agents

Identifiers

PMID24918716
PMCPMC4216208
OpenAlexW2325624449

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.