Study of the relationship between sigma receptor expression levels and some common sigma ligand activity in cancer using human cancer cell lines of the nci-60 cell line panel
(2021) In Biomedicines 9(1). p.1-20- Abstract
Sigma (σ) receptors have attracted great interest since they are implicated in various cellular functions and biological processes and diseases, including various types of cancer. The receptor family consists of two subtypes: sigma-1 (σ1) and sigma-2 (σ2). Both σ receptor subtypes have been proposed as therapeutic targets for various types of cancers, and many studies have provided evidence that their selective ligands (agonists and antagonists) exhibit antiproliferative and cytotoxic activity. Still, the precise mechanism of action of both σ receptors and their ligands remains unclear and needs to be elucidated. In this study, we aimed to simultaneously determine the expression levels of both σ receptor subtypes in several human cancer... (More)
Sigma (σ) receptors have attracted great interest since they are implicated in various cellular functions and biological processes and diseases, including various types of cancer. The receptor family consists of two subtypes: sigma-1 (σ1) and sigma-2 (σ2). Both σ receptor subtypes have been proposed as therapeutic targets for various types of cancers, and many studies have provided evidence that their selective ligands (agonists and antagonists) exhibit antiproliferative and cytotoxic activity. Still, the precise mechanism of action of both σ receptors and their ligands remains unclear and needs to be elucidated. In this study, we aimed to simultaneously determine the expression levels of both σ receptor subtypes in several human cancer cell lines. Additionally, we investigated the in vitro antiproliferative activity of some widely used σ1 and σ2 ligands against those cell lines to study the relationship between σ receptor expression levels and σ ligand activity. Finally, we ran the NCI60 COMPARE algorithm to further elucidate the cytotoxic mechanism of action of the selected σ ligands studied herein.
(Less)
- author
- Sereti, Evangelia LU ; Tsimplouli, Chrisiida ; Kalaitsidou, Elisavet ; Sakellaridis, Nikos and Dimas, Konstantinos
- organization
- publishing date
- 2021-01
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- Cancer, NCI60 COMPARE analysis, PGRMC1, Sigma ligands, Sigma receptors, SIGMAR1, TMEM97
- in
- Biomedicines
- volume
- 9
- issue
- 1
- article number
- 38
- pages
- 20 pages
- publisher
- MDPI AG
- external identifiers
-
- scopus:85099795228
- pmid:33466391
- ISSN
- 2227-9059
- DOI
- 10.3390/biomedicines9010038
- language
- English
- LU publication?
- yes
- id
- 735ab69d-20ab-4c95-8eee-9e1a2686ffc4
- date added to LUP
- 2022-03-22 15:31:09
- date last changed
- 2024-06-21 02:42:55
@article{735ab69d-20ab-4c95-8eee-9e1a2686ffc4,
abstract = {{<p>Sigma (σ) receptors have attracted great interest since they are implicated in various cellular functions and biological processes and diseases, including various types of cancer. The receptor family consists of two subtypes: sigma-1 (σ1) and sigma-2 (σ2). Both σ receptor subtypes have been proposed as therapeutic targets for various types of cancers, and many studies have provided evidence that their selective ligands (agonists and antagonists) exhibit antiproliferative and cytotoxic activity. Still, the precise mechanism of action of both σ receptors and their ligands remains unclear and needs to be elucidated. In this study, we aimed to simultaneously determine the expression levels of both σ receptor subtypes in several human cancer cell lines. Additionally, we investigated the in vitro antiproliferative activity of some widely used σ1 and σ2 ligands against those cell lines to study the relationship between σ receptor expression levels and σ ligand activity. Finally, we ran the NCI60 COMPARE algorithm to further elucidate the cytotoxic mechanism of action of the selected σ ligands studied herein.</p>}},
author = {{Sereti, Evangelia and Tsimplouli, Chrisiida and Kalaitsidou, Elisavet and Sakellaridis, Nikos and Dimas, Konstantinos}},
issn = {{2227-9059}},
keywords = {{Cancer; NCI60 COMPARE analysis; PGRMC1; Sigma ligands; Sigma receptors; SIGMAR1; TMEM97}},
language = {{eng}},
number = {{1}},
pages = {{1--20}},
publisher = {{MDPI AG}},
series = {{Biomedicines}},
title = {{Study of the relationship between sigma receptor expression levels and some common sigma ligand activity in cancer using human cancer cell lines of the nci-60 cell line panel}},
url = {{http://dx.doi.org/10.3390/biomedicines9010038}},
doi = {{10.3390/biomedicines9010038}},
volume = {{9}},
year = {{2021}},
}