Evidence map›Paper›PMID 34144027›Full record

ArticleEuropean journal of pharmacology2021

Identification and characterization of MAM03055A: A novel bivalent sigma-2 receptor/TMEM97 ligand with cytotoxic activity.

Cheri Z Liu, Marco Mottinelli, Hilary E Nicholson, Bridget M McVeigh, Neelum K Wong, Christopher R McCurdy, Wayne D Bowen

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

Article in European journal of pharmacology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
0.6field-weighted citation impact, top 33% 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

6 citing papers in PubMed, 11 citations in OpenAlex.

  1. Review
  2. Review
  3. Article
  4. Article
  5. Development of Fluorescent 4-[4-(3Journal of medicinal chemistry · 2023
    Article
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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

7 authors at 2 institutions in 1 country.

Cheri Z LiuDepartment of Molecular Pharmacology, Physiology, & Biotechnology, Brown University, Providence, RI, USA.
Marco MottinelliDepartment of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL, USA.
Hilary E NicholsonDepartment of Molecular Pharmacology, Physiology, & Biotechnology, Brown University, Providence, RI, USA.
Bridget M McVeighDepartment of Molecular Pharmacology, Physiology, & Biotechnology, Brown University, Providence, RI, USA.
Neelum K WongDepartment of Molecular Pharmacology, Physiology, & Biotechnology, Brown University, Providence, RI, USA.
Christopher R McCurdyDepartment of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL, USA.
Wayne D BowenDepartment of Molecular Pharmacology, Physiology, & Biotechnology, Brown University, Providence, RI, USA. Electronic address: wayne_bowen@brown.edu.
Brown University · USUniversity of Florida · US

Funding

Predoctoral Training Program in Trans-Disciplinary Pharmacological SciencesT32GM077995 · NIGMS · BROWN UNIVERSITY · PI OANCEA, ELENA · 2010 to 2020
$1.7M
Interdisciplinary training in pharmacological sciencesT32GM139793 · NIGMS · BROWN UNIVERSITY · PI Diana M Horrigan, Sean Edward Lawler · 2021 to 2026
$1.3M
NIGMS NIH HHS T32 GM077995NIGMS NIH HHS T32 GM139793
6 · The paper itself

Abstract

Sigma-2 receptor/transmembrane protein 97 (TMEM97) is upregulated in cancer cells compared to normal cells. Traditional sigma-2 receptor agonists induce apoptosis and autophagy, making them of interest in cancer therapy. Recently, we reported a novel metabolically stimulative function of the sigma-2 receptor, showing increased 3-(4,5 dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction and stimulation of glycolytic hallmarks. 6-Substituted analogs of the canonical sigma-2 receptor antagonist, 6-acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one (SN79), produce both metabolically stimulative and cytotoxic effects. Here, we compare the activities of two related compounds: 6-amino-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one (CM571), the 6-amino derivative of SN79, which binds with high affinity to both sigma-1 and sigma-2 receptors, and 1,3-bis(3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-6-yl)thiourea (MAM03055A), a homo-bivalent dimer of CM571. MAM03055A resulted from the degradation of 3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)-6-isothiocyanatobenzo[d]oxazol-2(3H)-one (CM572), the cytotoxic 6-isothiocyanato SN79 derivative. MAM03055A exhibited high affinity and strong preference for sigma-2 receptors (sigma-1 K

Indexed as

Antineoplastic AgentsBenzoxazolesCell Line, TumorCell SurvivalDrug Screening Assays, AntitumorHumansIsocyanatesMembrane ProteinsNeoplasmsReceptors, sigmaAntineoplastic AgentsBenzoxazolesCM572 compoundIsocyanatesMembrane ProteinsReceptors, sigmasigma-2 receptorTMEM97 protein, human1,3-bis(3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-6-yl)thiourea1,3-di-o-tolylguanidine1’-(4-(1-(4-fluorophenyl)-1H-indol-3-yl)butyl)-3H-spiro(2-benzofuran-1,4′-piperidine)3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)-6-isothiocyanatobenzo[d]oxazol-2(3H)-one3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide6-acetyl-3-(4-(4-(2-amino-4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one6-acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one6-amino-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-oneApoptosisCancer metabolismCM571CM572CM764DTGMAM03055AMTTNeuroblastomaProgesterone receptor membrane component 1Sigma-2 receptorSiramesineSN79TMEM97

Identifiers

PMID34144027
PMCPMC8736263
OpenAlexW3169559834

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.