Target intelligence / Profile preview

Olfactory receptor 51E2 (OR51E2) (OR51E2)

Target
OR51E2
Molecular classification
G protein-coupled receptor, Olfactory receptor
01

Overview

Olfactory receptor 51E2 (OR51E2), frequently referred to by its mouse ortholog name Olfr78 or as Prostate-Specific G-Protein Coupled Receptor (PSGR), is a specialized chemosensor belonging to the G protein-coupled receptor family [1][3]. Although originally identified in the olfactory epithelium, it is notably expressed in the renal juxtaglomerular apparatus and vascular smooth muscle cells, where it senses short-chain fatty acids (SCFAs) like acetate and propionate produced by gut microbiota [1]. Activation of the receptor in the kidney triggers the release of renin, thereby playing a critical role in the regulation of systemic blood pressure and cardiovascular homeostasis [1]. Beyond its physiological role in the renal system, OR51E2 is highly overexpressed in prostate cancer, particularly in high-grade intraepithelial neoplasia and adenocarcinoma, which has led to its investigation as a diagnostic biomarker and therapeutic target [2]. In prostate cells, the receptor appears to modulate signaling pathways involved in cell proliferation and migration, often responding to ligands like beta-ionone or steroid metabolites [2][4]. Therapeutic strategies targeting OR51E2 aim to either modulate blood pressure in hypertensive patients or inhibit tumor growth in prostate cancer, though the dual functionality presents challenges for tissue-specific targeting [1][2]. Current research focuses on developing potent and selective small molecule agonists or antagonists to exploit these pathways for clinical benefit [4].

Other names
Olfr78PSGRProstate-specific G-protein coupled receptorHPRAJOR51E1P
02

Mechanism of action

The receptor acts as a G protein-coupled receptor that, upon binding ligands such as short-chain fatty acids, activates the Gs-adenylyl cyclase-cAMP signaling pathway to stimulate renin release in the kidney or modulate cell growth in the prostate.

03

Biological functions

Signal transductionRegulation of blood pressureRenin secretionChemoreceptionCell proliferation
04

Disease associations

HypertensionProstate cancerCardiovascular disease
05

Safety considerations

Potential for systemic blood pressure alterationsOff-target effects in the olfactory systemTissue-specific signaling variability
06

Interacting drugs

Acetate

3 more in the full profile.

07

Biomarkers

OR51E2 mRNA expressionProstate-specific G-protein coupled receptor (PSGR) protein levels

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