Evidence map›Paper›PMID 37832799›Full record

ArticleBioorganic & medicinal chemistry letters2023

Imidazole-based sphingosine-1-phosphate transporter Spns2 inhibitors.

Christopher W Shrader, Daniel Foster, Yugesh Kharel, Tao Huang, Kevin R Lynch, Webster L Santos

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.5field-weighted citation impact, top 32% 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

1 citing paper in PubMed, 3 citations in OpenAlex.

  1. 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

6 authors at 2 institutions in 1 country.

Christopher W ShraderDepartment of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA 24060, United States.
Daniel FosterDepartment of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA 24060, United States.
Yugesh KharelDepartment of Pharmacology, University of Virginia, Charlottesville, VA 22904, United States.
Tao HuangDepartment of Pharmacology, University of Virginia, Charlottesville, VA 22904, United States.
Kevin R LynchDepartment of Pharmacology, University of Virginia, Charlottesville, VA 22904, United States.
Webster L SantosDepartment of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA 24060, United States. Electronic address: santosw@vt.edu.
University of Virginia · USVirginia Tech · US

Funding

Controlling the flux of sphingosine-1-phosphate in vivoR01AI144026 · NIAID · UNIVERSITY OF VIRGINIA · PI LYNCH, KEVIN R., SANTOS, WEBSTER L · 2019 to 2023
$3.5M
NIAID NIH HHS R01 AI144026
6 · The paper itself

Abstract

Sphingosine-1-phosphate (S1P) is a chemotactic lipid that influences immune cell positioning. S1P concentration gradients are necessary for proper egress of lymphocytes from the thymus and secondary lymphoid tissues. This trafficking is interdicted by S1P receptor modulators, and it is expected that S1P transporter (Spns2) inhibitors, by reshaping S1P concentration gradients, will do the same. We previously reported SLF1081851 as a prototype Spns2 inhibitor, which provided a scaffold to investigate the importance of the oxadiazole core and the terminal amine. In this report, we disclose a structure-activity relationship study by incorporating imidazole as both a linker and surrogate for a positive charge in SLF1081851. In vitro inhibition of Spns2-dependent S1P transport in HeLa cells identified 7b as an inhibitor with an IC

Indexed as

LysophospholipidsSphingosineAnion Transport ProteinsHeLa CellsHumansImidazolesAnion Transport ProteinsImidazolesLysophospholipidsSphingosinesphingosine 1-phosphateSpns2 protein, humanSphingolipidsSphingosine-1-phosphateSpns2Structure–activity relationshipsTransporter inhibitor

Identifiers

PMID37832799
PMCPMC10842094
OpenAlexW4387521394

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.