Target intelligence / Profile preview

Probable G protein-coupled receptor 160 (GPR160)

Target
GPR160
Molecular classification
G protein-coupled receptor, Receptor, Orphan receptor
01

Overview

Probable G protein-coupled receptor 160 (GPR160) is an orphan receptor protein of the GPCR superfamily, encoded in humans by the GPR160 gene (located at chromosome 3q26.2-q27), with a predicted length of 338 amino acids[1][4][5]. It is primarily classified as a class A (rhodopsin-like) GPCR. GPR160 is a membrane receptor, widely expressed with tissue-specific abundance, especially in reproductive organs and the gastrointestinal tract[1]. It is upregulated in several cancers, notably prostate cancer, with higher expression correlating with tumorigenic behavior and poor prognosis[1][3]. In experimental cellular and animal models, knockdown of GPR160 leads to cell cycle arrest, induction of apoptosis (mediated notably by caspase-1 and IL-6 upregulation), and growth inhibition in prostate cancer cells[1]. GPR160 has also been implicated in neuropathic pain perception and embryonic stem cell development[2]. As an orphan receptor, its endogenous ligand is unknown, which presents both challenges and opportunities for therapeutic discovery. There are currently no approved small-molecule drugs known to modulate GPR160 activity directly[1][3].

Other names
GPCR150hGPCR1GPCR1putative G protein-coupled receptor 160G-protein coupled receptor GPCR1probable G-protein coupled receptor 160G-protein coupled receptor 160
02

Mechanism of action

Drugs (e.g., shRNA/siRNA) that knock down GPR160 expression induce apoptosis and cell cycle arrest in certain cancer cell models, notably prostate cancer[1]. Caspase activation (particularly caspase 1, with involvement of caspases 3, 7, and 9 in some contexts) downstream of GPR160 depletion[1].

03

Biological functions

Signal transductionRegulation of programmed cell deathApoptosisRegulation of cell cycle (G2/M phase)Cytokine expression and cytokine receptor interactionPotential involvement in stem cell developmentInvolvement in the perception of neuropathic pain
04

Disease associations

Cancer (notably prostate cancer)Possible association with hematodermic neoplasmsPossible implication in neurodegenerative diseases and pain (neuropathic pain perception)
05

Safety considerations

No clinical safety data; potential concern with broad inhibition due to expression in multiple tissues (reproductive tissues, intestine, bone marrow, etc.)[1]Lack of known endogenous ligand and incomplete understanding of receptor function and tissue specificity may complicate therapeutic targeting[1][2]
06

Interacting drugs

No approved small-molecule drug known

1 more in the full profile.

07

Biomarkers

GPR160 transcription levels in tumors (e.g., prostate cancer upregulation)[1]Upregulation of IL-6 and caspase-1 in response to GPR160 knockdown[1]

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