Target intelligence / Profile preview

Olfactory receptor (OR) (OR)

Target
OR
Molecular classification
G protein-coupled receptor, Class A GPCR, Rhodopsin-like GPCR, Receptor
01

Overview

Human olfactory receptors (ORs) represent the largest family of G protein-coupled receptors (GPCRs), with approximately 400 functional genes identified in the human genome (UniProt, 2024). While primarily known for their role in the olfactory epithelium where they detect volatile odorants to mediate the sense of smell, these receptors are also ectopically expressed in a wide variety of non-olfactory tissues including the skin, prostate, gut, and heart (Massberg & Hatt, 2018). In these peripheral tissues, ORs function as chemosensors that regulate physiological processes such as sperm chemotaxis, skin wound healing, and serotonin release in the gut (PubMed, 2023). Dysregulation of OR expression has been increasingly linked to various pathologies, particularly in oncology, where specific receptors like OR51E2 are overexpressed in prostate and breast cancers, promoting tumor progression (Rodriguez-Maria et al., 2023). Consequently, ORs are emerging as novel therapeutic targets and diagnostic biomarkers, though achieving drug selectivity remains a challenge due to the high structural similarity across the receptor family (NIH, 2023). Research into synthetic ligands, such as the sandalwood odorant Sandalore, has demonstrated clinical potential in stimulating hair growth and skin regeneration by targeting specific ORs (PubMed, 2019).

Other names
Odorant receptorOlfactory receptor familyORs
02

Mechanism of action

Agonism or antagonism of G protein-coupled receptors, typically coupled to the G-alpha-olf protein, which activates adenylyl cyclase to increase intracellular cAMP levels and open cyclic nucleotide-gated ion channels (UniProt, 2024; NIH, 2023).

03

Biological functions

Signal transductionChemosensationCell proliferationCell migrationApoptosis regulationHormone secretion
04

Disease associations

CancerNeurodegenerative diseaseMetabolic disorderInfectionAnosmia
05

Safety considerations

High sequence homology between family members leading to significant off-target cross-reactivityPotential for systemic side effects due to widespread ectopic expression in vital organs like the heart and lungsRisk of inducing anosmia or parosmia when targeting receptors in the nasal epithelium
06

Interacting drugs

Sandalore

4 more in the full profile.

07

Biomarkers

Olfactory receptor family 51 subfamily E member 2 (OR51E2/PSGR) for prostate cancerOlfactory threshold testingOR expression profiling in tumor biopsies

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