Evidence map›Paper›PMID 30530624›Full record

ArticleThe Journal of pharmacology and experimental therapeutics2019

Divergent Cytotoxic and Metabolically Stimulative Functions of Sigma-2 Receptors: Structure-Activity Relationships of 6-Acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[

Hilary E Nicholson, Walid F Alsharif, Anthony B Comeau, Christophe Mesangeau, Sebastiano Intagliata, Marco Mottinelli, Christopher R McCurdy, Wayne D Bowen

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

Article in The Journal of pharmacology and experimental therapeutics, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
1.4field-weighted citation impact, top 18% 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

13 citing papers in PubMed, 21 citations in OpenAlex.

  1. Article
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  5. Review
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  8. Exploring 1-adamantanamine as an alternative amine moiety for metabolically labile azepane ring in newly synthesized benzo[Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2020
    Article
  9. Article
  10. Article
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  12. Benzimidazolone-based selective σEuropean journal of medicinal chemistry · 2019
    Article
  13. 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

8 authors at 3 institutions in 1 country.

Hilary E NicholsonDepartment of Molecular Pharmacology, Physiology, and Biotechnology, Brown University, Providence, Rhode Island (H.E.N., A.B.C., W.D.B.); Department of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, Mississippi (W.F.A., C.M., C.R.M.); and Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida (S.I., M.M., C.R.M.).
Walid F AlsharifDepartment of Molecular Pharmacology, Physiology, and Biotechnology, Brown University, Providence, Rhode Island (H.E.N., A.B.C., W.D.B.); Department of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, Mississippi (W.F.A., C.M., C.R.M.); and Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida (S.I., M.M., C.R.M.).
Anthony B ComeauDepartment of Molecular Pharmacology, Physiology, and Biotechnology, Brown University, Providence, Rhode Island (H.E.N., A.B.C., W.D.B.); Department of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, Mississippi (W.F.A., C.M., C.R.M.); and Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida (S.I., M.M., C.R.M.).
Christophe MesangeauDepartment of Molecular Pharmacology, Physiology, and Biotechnology, Brown University, Providence, Rhode Island (H.E.N., A.B.C., W.D.B.); Department of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, Mississippi (W.F.A., C.M., C.R.M.); and Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida (S.I., M.M., C.R.M.).
Sebastiano IntagliataDepartment of Molecular Pharmacology, Physiology, and Biotechnology, Brown University, Providence, Rhode Island (H.E.N., A.B.C., W.D.B.); Department of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, Mississippi (W.F.A., C.M., C.R.M.); and Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida (S.I., M.M., C.R.M.).
Marco MottinelliDepartment of Molecular Pharmacology, Physiology, and Biotechnology, Brown University, Providence, Rhode Island (H.E.N., A.B.C., W.D.B.); Department of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, Mississippi (W.F.A., C.M., C.R.M.); and Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida (S.I., M.M., C.R.M.).
Christopher R McCurdyDepartment of Molecular Pharmacology, Physiology, and Biotechnology, Brown University, Providence, Rhode Island (H.E.N., A.B.C., W.D.B.); Department of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, Mississippi (W.F.A., C.M., C.R.M.); and Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida (S.I., M.M., C.R.M.).
Wayne D BowenDepartment of Molecular Pharmacology, Physiology, and Biotechnology, Brown University, Providence, Rhode Island (H.E.N., A.B.C., W.D.B.); Department of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, Mississippi (W.F.A., C.M., C.R.M.); and Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida (S.I., M.M., C.R.M.) Wayne_Bowen@brown.edu.
Brown University · USUniversity of Mississippi · USUniversity of Florida · US

Funding

Center of Research Excellence in Natural Products Neuroscience (CORE-NPN)P20GM104932 · NIGMS · UNIVERSITY OF MISSISSIPPI · PI MAJUMDAR, SOUMYAJIT · 2012 to 2016
$10.0M
Advancing the Culture of PhD Learning & Scholarship in Biology & Health SciencesR25GM083270 · NIGMS · BROWN UNIVERSITY · PI CAMPBELL, ANDREW G., HARRINGTON, ELIZABETH O · 2008 to 2021
$7.5M
Substance Abuse Intervention/Outcome Research TrainingT32DA016184 · NIDA · BROWN UNIVERSITY · PI Damaris J. Rohsenow, JENNIFER W. TIDEY · 2003 to 2026
$6.1M
Novel Pharmacologic Interventions for Drugs of AbuseR01DA023205 · NIDA · UNIVERSITY OF MISSISSIPPI · PI MCCURDY, CHRISTOPHER R · 2007 to 2011
$1.7M
Predoctoral Training Program in Trans-Disciplinary Pharmacological SciencesT32GM077995 · NIGMS · BROWN UNIVERSITY · PI OANCEA, ELENA · 2010 to 2020
$1.7M
NIDA NIH HHS R01 DA023205NIDA NIH HHS T32 DA016184NIGMS NIH HHS P20 GM104932NIGMS NIH HHS R25 GM083270NIGMS NIH HHS T32 GM077995
6 · The paper itself

Abstract

Sigma-2 receptors, recently identified as TMEM97, have been implicated in cancer and neurodegenerative disease. Structurally distinct sigma-2 receptor ligands induce cell death in tumor cells, linking sigma-2 receptors to apoptotic pathways. Recently, we reported that sigma-2 receptors can also stimulate glycolytic hallmarks, effects consistent with a prosurvival function and upregulation in cancer cells. Both apoptotic and metabolically stimulative effects were observed with compounds related to the canonical sigma-2 antagonist SN79. Here we investigate a series of 6-substituted SN79 analogs to assess the structural determinants governing these divergent effects. Substitutions on the benzoxazolone ring of the core SN79 structure resulted in high-affinity sigma-2 receptor ligands (

Indexed as

AnimalsBenzoxazolesCell Line, TumorCytotoxinsDose-Response Relationship, DrugHumansPiperazinesProtein BindingRatsReceptors, sigmaStructure-Activity Relationship6-acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo(d)oxazol-2(3H)-oneBenzoxazolesCytotoxinsPiperazinesReceptors, sigmasigma-2 receptor

Identifiers

PMID30530624
PMCPMC6346378
OpenAlexW2903880522

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.