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Updated: Feb 8, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Regulation of prostate cancer by hormone-responsive G protein-coupled receptors
Wei Wang1, Zhao-Xia Chen1, Dong-Yu Guo1
1Department of Clinical Laboratory, Xiamen Huli Guoyu Clinic, Co., Ltd., Xiamen, China.
Abstract:
Regulation of prostate cancer by androgen and androgen receptor (AR), and blockade of AR signaling by AR antagonists and steroidogenic enzyme inhibitors have been extensively studied. G protein-coupled receptors (GPCRs) are a family of membrane receptors that regulate almost all physiological processes. Nearly 40% of FDA-approved drugs in the market target GPCRs. A variety of GPCRs that mediate reproductive function have been demonstrated to be involved in the regulation of prostate cancer. These GPCRs include gonadotropin-releasing hormone receptor, luteinizing hormone receptor, follicle-stimulating hormone receptor, relaxin receptor, ghrelin receptor, and kisspeptin receptor. We highlight here GPCR regulation of prostate cancer by these GPCRs. Further therapeutic approaches targeting these GPCRs for the treatment of prostate cancer are summarized.
Insights
G protein-coupled receptors (GPCRs) regulate prostate cancer. Targeting reproductive function-mediating GPCRs offers new therapeutic strategies for prostate cancer treatment.
Area of Science:
- Endocrinology
- Oncology
- Pharmacology
Background:
- Prostate cancer progression is linked to androgen and androgen receptor (AR) signaling.
- AR antagonists and steroidogenic enzyme inhibitors are established therapeutic strategies.
- G protein-coupled receptors (GPCRs) are crucial regulators of physiological processes and drug targets.
Purpose of the Study:
- To review the role of GPCRs in prostate cancer regulation.
- To highlight specific GPCRs involved in prostate cancer, including those mediating reproductive functions.
- To summarize potential therapeutic strategies targeting GPCRs for prostate cancer treatment.
Main Methods:
- Literature review focusing on GPCRs and prostate cancer.
- Identification of GPCRs involved in reproductive functions and their link to prostate cancer.
- Summary of current and emerging therapeutic approaches targeting GPCRs.
Main Results:
- Several GPCRs, including gonadotropin-releasing hormone receptor, luteinizing hormone receptor, follicle-stimulating hormone receptor, relaxin receptor, ghrelin receptor, and kisspeptin receptor, are implicated in prostate cancer.
- These GPCRs play a regulatory role in prostate cancer development and progression.
- Targeting these GPCRs presents novel therapeutic opportunities.
Conclusions:
- GPCRs represent a significant regulatory network in prostate cancer.
- Targeting specific GPCRs involved in reproductive functions offers promising avenues for novel prostate cancer therapies.
- Further research into GPCR-targeted therapies could lead to improved treatment outcomes.
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