Abstract
Olfactory receptor OR51E2, also known as a Prostate Specific G-Protein Receptor, is highly expressed in prostate cancer but its function is not well understood. Through in silico and in vitro analyses, we identified 24 agonists and 1 antagonist for this receptor. We detected that agonist 19-hydroxyandrostenedione, a product of the aromatase reaction, is endogenously produced upon receptor activation. We characterized the effects of receptor activation on metabolism using a prostate cancer cell line and demonstrated decreased intracellular anabolic signals and cell viability, induction of cell cycle arrest, and increased expression of neuronal markers. Furthermore, upregulation of neuron-specific enolase by agonist treatment was abolished in OR51E2-KO cells. The results of our study suggest that OR51E2 activation results in neuroendocrine trans-differentiation. These findings reveal a new role for OR51E2 and establish this G-protein coupled receptor as a novel therapeutic target in the treatment of prostate cancer.
Original language | English (US) |
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Article number | 162 |
Journal | Frontiers in Oncology |
Volume | 8 |
Issue number | MAY |
DOIs | |
State | Published - May 28 2018 |
Keywords
- 19-hydroxyandrostenedione
- Agonists
- Neuroendocrine trans-differentiation
- Neuron-specific enolase
- OR51E2
- Olfactory receptor
- PSGR
- Prostate cancer
ASJC Scopus subject areas
- Oncology
- Cancer Research