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G protein-coupled receptor class C group 5 member A (GPRC5A) (GPRC5A)

Target
GPRC5A
Molecular classification
G protein-coupled receptor, Orphan receptor, Receptor
01

Overview

G protein-coupled receptor class C group 5 member A (GPRC5A), also known as Retinoic Acid-Induced Protein 3 (RAI3), is an orphan G protein-coupled receptor primarily expressed in the lung [1, 4]. It is uniquely characterized by its dual role in oncology, acting as a tumor suppressor in lung tissues while frequently being overexpressed and functioning as an oncogene in other cancers such as pancreatic, breast, and colorectal cancer [2, 3]. GPRC5A is induced by all-trans retinoic acid and plays a vital role in maintaining epithelial cell homeostasis and regulating signaling pathways including EGFR, STAT3, and NF-kappaB [1, 2]. As a therapeutic target, GPRC5A mRNA is being explored for RNA-based interventions, such as siRNA-mediated silencing in overexpressing tumors, or as a target for immunotherapy and cancer vaccines [3]. Its high expression in specific tissues makes it a potential biomarker for cancer progression and a candidate for precision medicine [4]. However, its complex role as both a suppressor and promoter of malignancy necessitates careful evaluation of the cellular context when developing GPRC5A-targeted therapies [2, 3].

Other names
Retinoic acid-induced protein 3RAI3Retinoic acid-induced gene 1 proteinRAIG1GPCR5AOrphan G protein-coupled receptor PEIG-1
02

Mechanism of action

Downregulation of protein expression via RNA interference (RNAi) or antisense oligonucleotides (ASOs) targeting the GPRC5A mRNA transcript [3].

03

Biological functions

Signal transductionCell proliferationLung developmentApoptosis regulationEpithelial cell homeostasis
04

Disease associations

CancerLung cancerPancreatic cancerBreast cancerColorectal cancer
05

Safety considerations

Potential for pulmonary toxicity due to high basal expression in lung tissue [2]Risk of accelerating tumor progression in contexts where GPRC5A acts as a tumor suppressor [3]Off-target effects associated with RNA-based delivery systems [4]
06

Biomarkers

GPRC5A mRNA expression levels [3]GPRC5A protein expression [1]Circulating GPRC5A mRNA [4]

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