Evidence map›Paper›PMID 24292269›Full record

ArticleScientific reports2013

Common pharmacophore of structurally distinct small-molecule inhibitors of intracellular retrograde trafficking of ribosome inactivating proteins.

Shichao Yu, Jewn Giew Park, Jennifer Nielsen Kahn, Nilgun E Tumer, Yuan-Ping Pang

Open access · goldAbstract read
In one paragraph

Article in Scientific reports, 2013. 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
–field-weighted citation impact, top 93% 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, 8 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. 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

5 authors at 3 institutions in 1 country.

Shichao YuComputer-Aided Molecular Design Laboratory, Mayo Clinic, Rochester, MN 55905, USA.
Jewn Giew Park
Jennifer Nielsen Kahn
Nilgun E Tumer
Yuan-Ping Pang
Mayo Clinic · USRutgers, The State University of New Jersey · USMayo Clinic in Florida · US

Funding

Optimization of Small-Molecule Inhibitors of Shiga and Ricin ToxinsU01AI082120 · NIAID · MAYO CLINIC ROCHESTER · PI PANG, YUAN-PING · 2009 to 2012
$3.0M
NIAID NIH HHS 5U01 AI082120-04NIAID NIH HHS U01 AI082120
6 · The paper itself

Abstract

We reported previously (±)-2-(5-methylthiophen-2-yl)-3-phenyl-2,3-dihydroquinazolin-4(1H)-one [(±)-Retro-2(cycl)] as the chemical structure of Retro-2 that showed mouse protection against ricin, a notorious ribosome inactivating protein (RIP). Herein we report our chemical resolution of (±)-Retro-2(cycl), analog synthesis, and cell-based evaluation showing that the two optically pure enantiomers and their achiral analog have nearly the same degree of cell protection against ricin as (±)-Retro-2(cycl). We also report our computational studies explaining the lack of stereo preference and revealing a common pharmacophore of structurally distinct inhibitors of intracellular retrograde trafficking of RIPs. This pharmacophore comprises a central aromatic ring o-substituted by an aromatic ring and a moiety bearing an O or S atom attached to sp² C atom(s). These results offer new insights into lead identification and optimization for RIP antidote development to minimize the global health threat caused by ribosome-inactivating proteins.

Indexed as

AnimalsCell LineChlorocebus aethiopsProtein TransportRibosome Inactivating ProteinsRicinSmall Molecule LibrariesStereoisomerismVero CellsRibosome Inactivating ProteinsRicinSmall Molecule Libraries

Identifiers

PMID24292269
PMCPMC3844963
OpenAlexW1980760227

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.