# GPR17 in Glioblastoma: Structure, Ligand Interactions, and Therapeutic Targeting

**Authors:** Ramalakshmi Satyanarayana, Sree Somala Chaitanya, Iswarya Suresh Kumar, Ramesh Thiyagarajan, Sureka Chandrabose, Kasim S. Abass, Saravanan Konda Mani, Anand Thirunavukarasou, Meenakshisundaram Kandhavelu

PMC · DOI: 10.1021/acsomega.5c04079 · ACS Omega · 2025-09-29

## TL;DR

This review explores GPR17's role in glioblastoma, focusing on its structure, ligand interactions, and potential as a therapeutic target for this aggressive brain cancer.

## Contribution

The paper provides a comprehensive review of GPR17's biology and its emerging role as a therapeutic target in glioblastoma.

## Key findings

- GPR17 is overexpressed in glioblastoma and contributes to tumor progression and invasion.
- Understanding GPR17's structure and ligand interactions could lead to targeted therapies for glioblastoma.
- GPR17 plays a role in myelination, inflammation, and neuroprotection beyond its oncological relevance.

## Abstract

G protein-coupled receptor 17 (GPR17) is a crucial protein
encoded
by the GPR17 gene, which belongs to the G protein-coupled receptor
(GPCR) family. It serves a pivotal function in cellular responses
to various stimuli. GPR17 is found in various organs, including the
brain, spinal cord, kidneys, liver, and immune cells. It is especially
prevalent in oligodendrocytes, underscoring its significance in myelination.
GPR17 is involved in myelination, inflammation, and neuroprotection.
Recent studies highlight the therapeutic potential of targeting GPR17
in glioblastoma, a highly aggressive brain cancer, as it is overexpressed
in tumor tissues and plays a critical role in tumor progression and
invasion. Understanding the structure of GPR17 and its interactions
with ligands and functional signaling pathways is crucial for developing
targeted therapeutics for conditions involving myelin degradation,
neuroinflammation, and immune dysregulation. To guide this exploration,
this review is organized into distinct sections covering the sequence
and structural features of GPR17, its natural and synthetic ligands,
its role in glioblastoma progression, its associated signaling pathways,
and the potential of using GPR17 as a therapeutic target. Each section
in the review consolidates current findings to offer an integrated
view of GPR17 biology and its translational relevance in oncology.

## Linked entities

- **Genes:** GPR17 (G protein-coupled receptor 17) [NCBI Gene 2840]
- **Proteins:** GPR17 (G protein-coupled receptor 17)
- **Diseases:** glioblastoma (MONDO:0018177)

## Full-text entities

- **Genes:** GPR17 (G protein-coupled receptor 17) [NCBI Gene 2840], CXCR6 (C-X-C motif chemokine receptor 6) [NCBI Gene 10663] {aka BONZO, CD186, CDw186, STRL33, TYMSTR}
- **Diseases:** tumor (MESH:D009369), inflammation (MESH:D007249), neuroinflammation (MESH:D000090862), immune dysregulation (OMIM:614878), brain cancer (MESH:D001932), Glioblastoma (MESH:D005909)

## Full text

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## Figures

4 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12529388/full.md

## References

74 references — full list in the complete paper: https://tomesphere.com/paper/PMC12529388/full.md

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Source: https://tomesphere.com/paper/PMC12529388