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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
- 김영석
- Issue Date
- 2021
- Journal Title
- Sensors
- ISSN
- 1424-8220
- Citation
- Sensors vol. 21, no. 10
- Keywords
- Anthraquinone; MCF-7 breast cancer cell line; Olfactory receptor; OR6M1; Rutin; Surface plasmon resonance
- Publisher
- MDPI AG
- Indexed
- SCIE; 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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