Evidence map›Paper›PMID 34418572›Full record

ArticleBioorganic & medicinal chemistry letters2021

Design, synthesis and analysis of novel sphingosine kinase-1 inhibitors to improve oral bioavailability.

Kendarius J Butler, Angel A Castro, Tiffany S Dwyer, Louise M Hardwick, Melody C Iacino, Sara G Manore, Kevin M Mays, Caylie A McGlade, Lisa N Hair, Erin W Parker and 8 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
0.1field-weighted citation impact, top 56% 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

0 citing papers in PubMed, 2 citations in OpenAlex.

No citing paper in PubMed yet.

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

18 authors at 2 institutions in 1 country.

Kendarius J ButlerWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Angel A CastroWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Tiffany S DwyerWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Louise M HardwickWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Melody C IacinoWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Sara G ManoreWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Kevin M MaysWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Caylie A McGladeWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Lisa N HairWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Erin W ParkerWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Mikala R SmithWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Morgan T TurnowWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Matthew R WilsonWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Stephanie R WoodsonWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
William E CothamUniversity of South Carolina, Department of Chemistry and Biochemistry, GSRC Rm 108M, Columbia, SC 29208, United States.
Michael D WallaUniversity of South Carolina, Department of Chemistry and Biochemistry, GSRC Rm 108M, Columbia, SC 29208, United States.
Jason C HurlbertWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
T Christian GrattanWinthrop University, Department of Chemistry, Physics and Geology, SIMS Building Rm 101, Rock Hill, SC 29733, United States.
Winthrop University · USUniversity of South Carolina · US

Funding

South Carolina IDeA Networks of Biomedical Research (SC INBRE V)P20GM103499 · NIGMS · UNIVERSITY OF SOUTH CAROLINA AT COLUMBIA · PI EDIE C GOLDSMITH · 2012 to 2026
$61.0M
NIGMS NIH HHS P20 GM103499
6 · The paper itself

Abstract

The sphingomyelin pathway is important in cell regulation and determining cellular fate. Inhibition of sphingosine kinase isoform 1 (SK1) within this pathway, leads to a buildup of sphingosine and ceramide, two molecules directly linked to cell apoptosis, while decreasing the intracellular concentration of sphingosine-1-phosphate (S1P), a molecule linked to cellular proliferation. Recently, an inhibitor capable of inhibiting SK1 in vitro was identified, but also shown to be ineffective in vivo. A set of compounds designed to assess the impact of synthetic modifications to the hydroxynaphthalene ring region of the template inhibitor with SK1 to obtain a compound with increased efficacy in vivo. Of these fifteen compounds, 4A was shown to have an IC

Indexed as

Drug DesignAdaptor Proteins, Signal TransducingEnzyme InhibitorsHumansInhibitory Concentration 50Models, MolecularMolecular Docking SimulationMolecular StructureProtein ConformationStructure-Activity RelationshipAdaptor Proteins, Signal TransducingEnzyme InhibitorsSPHKAP protein, humanBioorganic synthesisKinase inhibitionMicrowave synthesisSphingosine kinase

Identifiers

PMID34418572
PMCPMC8484043
OpenAlexW3193522970

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.