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Discovery of orphan olfactory receptor 6m1 as a new anticancer target in mcf-7 cells by a combination of surface plasmon resonance-based and cell-based systems

Title
Discovery of orphan olfactory receptor 6m1 as a new anticancer target in mcf-7 cells by a combination of surface plasmon resonance-based and cell-based systems
Authors
Choi Y.-R.Shim J.Park J.-H.Kim Y.-S.Kim M.-J.
Ewha Authors
김영석
SCOPUS Author ID
김영석scopusscopus
Issue Date
2021
Journal Title
Sensors
ISSN
1424-8220JCR Link
Citation
Sensors vol. 21, no. 10
Keywords
AnthraquinoneMCF-7 breast cancer cell lineOlfactory receptorOR6M1RutinSurface plasmon resonance
Publisher
MDPI AG
Indexed
SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
Olfactory receptors (ORs) account for 49% of all G protein-coupled receptors (GPCRs), which are important targets for drug discovery, and hence ORs may also be potential drug targets. Various ORs are expressed in breast cancer cells; however, most of them are orphan receptors, and thus, their functions are unknown. Herein, we present an experimental strategy using a surface plasmon resonance (SPR) system and a cell-based assay that allowed the identification of orphan OR6M1 as a new anticancer target in the MCF-7 breast cancer cell line. After the construction of stable OR6M1-expressing cells, the SPR-based screening of 108 chemicals for ligand activity was performed against OR6M1-expressing whole cells (primary screening) or membrane fragments (secondary screening). As a result, anthraquinone (AQ) and rutin were discovered to be new OR6M1 ligands. Based on calcium imaging in OR6M1-expressing Hana3A cells, AQ and rutin were classified as an OR6M1 agonist and antagonist, respectively. Cell viability and live/dead assays showed that AQ induced the death of MCF-7 cells, which was inhibited by rutin. Therefore, OR6M1 may be considered an anticancer target, and AQ may be considered a chemotherapeutic agent. This combined method can be widely used to discover the ligands and functions of other orphan GPCRs. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.
DOI
10.3390/s21103468
Appears in Collections:
공과대학 > 식품생명공학과 > Journal papers
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