Evidence map›Paper›PMID 33445156›Full record

ArticleEuropean journal of medicinal chemistry2021

Probing the substitution pattern of indole-based scaffold reveals potent and selective sphingosine kinase 2 inhibitors.

Molly Congdon, Russell G Fritzemeier, Yugesh Kharel, Anne M Brown, Vlad Serbulea, David R Bevan, Kevin R Lynch, Webster L Santos

Open access · greenAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.4field-weighted citation impact, top 39% 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

2 citing papers in PubMed, 9 citations in OpenAlex.

  1. Article
  2. 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

8 authors at 2 institutions in 1 country.

Molly CongdonDepartment of Chemistry, Virginia Tech, Blacksburg, VA, 24061, United States; Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA, 24061, United States.
Russell G FritzemeierDepartment of Chemistry, Virginia Tech, Blacksburg, VA, 24061, United States; Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA, 24061, United States.
Yugesh KharelDepartment of Pharmacology, University of Virginia, Charlottesville, VA, 22908, United States.
Anne M BrownVirginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA, 24061, United States; Department of Biochemistry, Virginia Tech, Blacksburg, VA, 24061, United States; Research and Informatics, University Libraries, Virginia Tech, Blacksburg, VA, 24061, United States.
Vlad SerbuleaDepartment of Pharmacology, University of Virginia, Charlottesville, VA, 22908, United States.
David R BevanVirginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA, 24061, United States; Department of Biochemistry, Virginia Tech, Blacksburg, VA, 24061, United States.
Kevin R LynchDepartment of Pharmacology, University of Virginia, Charlottesville, VA, 22908, United States.
Webster L SantosDepartment of Chemistry, Virginia Tech, Blacksburg, VA, 24061, United States; Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA, 24061, United States. Electronic address: santosw@vt.edu.
Virginia Tech · USUniversity of Virginia · US

Funding

Molecular Pharmacology of Sphingosine 1-PhosphateR01GM067958 · NIGMS · UNIVERSITY OF VIRGINIA CHARLOTTESVILLE · PI LYNCH, KEVIN R. · 2004 to 2014
$3.7M
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
In Vivo Probes of Sphingosine Kinase FunctionR01GM104366 · NIGMS · VIRGINIA POLYTECHNIC INST AND ST UNIV · PI LYNCH, KEVIN R., SANTOS, WEBSTER L · 2013 to 2015
$1.1M
NIGMS NIH HHS R01 GM067958NIGMS NIH HHS R01 GM104366
6 · The paper itself

Abstract

Elevated levels of sphingosine 1-phosphate (S1P) and increased expression of sphingosine kinase isoforms (SphK1 and SphK2) have been implicated in a variety of disease states including cancer, inflammation, and autoimmunity. Consequently, the S1P signaling axis has become an attractive target for drug discovery. Selective inhibition of either SphK1 or SphK2 has been demonstrated to be effective in modulating S1P levels in animal models. While SphK1 inhibitors have received much attention, the development of potent and selective SphK2 inhibitors are emerging. Previously, our group reported a SphK2 naphthalene-based selective inhibitor, SLC5081308, which displays approximately 7-fold selectivity for hSphK2 over hSphK1 and has a SphK2 K

Indexed as

Dose-Response Relationship, DrugEnzyme InhibitorsHumansIndolesMolecular Docking SimulationMolecular StructurePhosphotransferases (Alcohol Group Acceptor)Sphingosine KinaseStructure-Activity RelationshipEnzyme InhibitorsindoleIndolesPhosphotransferases (Alcohol Group Acceptor)Sphingosine Kinasesphingosine kinase 2, humanMolecular dockingSARSphingosineSphingosine 1-phosphateSphingosine kinaseSphK2

Identifiers

PMID33445156
PMCPMC8224985
OpenAlexW3118181710

What OpenQuestion holds

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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.