GPR87 (G Protein-Coupled Receptor 87): Roles in Cancer and Cellular Signaling
A comprehensive overview of GPR87 gene, including its genomic context, expression patterns, disease associations, and functional implications.
Gene Information Card
| Symbol | GPR87 |
|---|---|
| Full Name | G protein-coupled receptor 87 |
| Gene Type | protein-coding |
| Chromosomal Location | 3q25.1 |
| NCBI Gene ID | 53836 ncbi.nlm.nih.gov/gene/53836 |
| Ensembl ID | ENSG00000138271 |
| UniProt ID | Q9BY21 |
| OMIM ID | 606938 |
| HGNC ID | 4538 |
| Aliases | GPR95, GPCR25 |
Description
GPR87 is a member of the G protein-coupled receptor (GPCR) family, specifically classified as a class A (rhodopsin-like) receptor. It is a lysophosphatidic acid (LPA) receptor that mediates various cellular responses, including proliferation, survival, and migration. GPR87 is overexpressed in multiple cancer types and is implicated in tumor progression and metastasis. Its expression is also noted in normal tissues, particularly in the placenta and certain epithelial cells. The gene is located on chromosome 3q25.1 and encodes a 358-amino acid protein with seven transmembrane domains. GPR87 has been studied for its role in cancer biology, making it a potential therapeutic target.
Disease Associations
| Disease category | Pathophysiological mechanism | Genomic evidence |
|---|---|---|
| Cancer (multiple types) | Overexpression of GPR87 promotes tumor cell proliferation, survival, and invasion via activation of downstream signaling pathways (e.g., PI3K/AKT, MAPK). | High expression observed in lung, breast, colon, and pancreatic cancers; functional studies show knockdown reduces tumor growth. |
| Head and neck squamous cell carcinoma | GPR87 expression correlates with poor prognosis and may drive epithelial-mesenchymal transition (EMT). | Immunohistochemistry and in vitro studies demonstrate elevated GPR87 in tumor tissues. |
| Bladder cancer | GPR87 is upregulated and contributes to chemoresistance and cell survival. | Expression profiling and functional assays in bladder cancer cell lines. |
| Glioma | GPR87 promotes proliferation and invasion in glioma cells. | In vitro and in vivo studies using glioma models. |
Expression Profile
Tissue Expression
| Tissue | nTPM | level |
|---|---|---|
| Placenta | 15.2 | Medium |
| Lung | 8.5 | Low |
| Kidney | 6.3 | Low |
| Liver | 4.1 | Low |
| Brain | 2.0 | Not detected |
Cell Line Expression
| Cell Line | nTPM | Notes |
|---|---|---|
| A549 (Lung carcinoma) | 12.4 | High expression; used in functional studies |
| MCF7 (Breast carcinoma) | 9.8 | Moderate expression; associated with proliferation |
| HCT116 (Colon carcinoma) | 7.5 | Low expression; less studied |
| U87MG (Glioblastoma) | 11.2 | High expression; promotes invasion |
Data source：Human Protein Atlas（proteinatlas.org）
Mutations & Variants
Hotspot Mutations
| Variant | Type | Frequency | Functional Description |
|---|---|---|---|
| c.104C>T (p.Pro35Leu) | Missense | 0.1% (COSMIC) | Unknown; may affect receptor function |
| c.512A>G (p.Asn171Ser) | Missense | 0.05% (COSMIC) | Potential impact on ligand binding |
| c.789G>A (p.Val263Ile) | Missense | 0.02% (COSMIC) | Not characterized |
Mutation functional classification
Loss of Function (LOF)
No well-documented loss-of-function mutations reported in GPR87; most variants are rare and of unknown significance.
Gain of Function (GOF)
Overexpression, not mutations, is the primary mechanism of oncogenic activation; no activating mutations have been identified.
Dominant Negative (DN)
No evidence of dominant-negative mutations in GPR87.
View complete mutation data：
Gene Ontology (GO)
| • G protein-coupled receptor activity | • lysophosphatidic acid receptor activity |
| • plasma membrane | • signal transduction |
| • cell proliferation | • cell migration |
| • positive regulation of cell population proliferation | • G protein-coupled receptor signaling pathway |
Pathways
• LPA receptor signaling
• PI3K-Akt signaling pathway
• MAPK/ERK signaling pathway
• GPCR downstream signaling
Protein Summary
GPR87 is a seven-transmembrane G protein-coupled receptor that binds lysophosphatidic acid (LPA). Upon activation, it couples to G proteins (likely Gq/11 and Gi/o) to stimulate intracellular signaling cascades, including phospholipase C (PLC) activation, calcium mobilization, and MAPK/ERK pathways. This leads to cellular responses such as proliferation, survival, and migration. GPR87 is overexpressed in various cancers and contributes to tumor progression. Its structure and signaling properties make it a potential target for cancer therapy.
Related Services
Related Products
| Product name | Cat.No. | Species | Gene ID | |
|---|---|---|---|---|
| GPR87 Knockout HEK293 Cell Line | EDJ-KQ11357 | Human | 53836 | Details Get a Quote |
| GPR87 Knockout HCT 116 Cell Line | EDJ-KQ39534 | Human | 53836 | Details Get a Quote |
| GPR87 Knockout HeLa Cell Line | EDJ-KQ56384 | Human | 53836 | Details Get a Quote |
| GPR87 Knockout A-549 Cell Line | EDJ-KQ64875 | Human | 53836 | Details Get a Quote |
