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Peer-reviewedCC BY 4.0International Journal of Molecular Sciences

G Protein-Coupled Receptors in Prostate Cancer: Pathophysiological Implications and Potential for Innovative Therapeutics

  • Andre Sarmento-Cabral1,2
  • Vicente Herrero-Aguayo1,2
  • Prudencio Sáez-Martínez1,2,3
  • Emilia Alors-Pérez1,2
  • Antonio J. León-González1,2,4
  • Juan L. López-Cánovas1,2
  • Antonio J. Montero-Hidalgo1,2,5,6
  • Manuel D. Gahete1,2,7
  • Juan M. Jiménez-Vacas1,2,8
  • Raúl M. Luque1,2,7
8 affiliations
  1. 1Department of Cell Biology, Physiology, and Immunology, University of Córdoba, 14014 Córdoba, Spain
  2. 2Maimonides Institute for Biomedical Research of Córdoba (IMIBIC), Hospital Universitario Reina Sofía (HURS), 14004 Córdoba, Spain
  3. 3Universidad Europea de Madrid, Faculty of Biomedical and Health Sciences, Department of Pharmacy and Nutrition, 28670 Madrid, Spain
  4. 4Department of Pharmacology, Faculty of Pharmacy, University of Seville, 41012 Seville, Spain
  5. 5Department of Medicine and Life Sciences, Universitat Pompeu Fabra, 08003 Barcelona, Spain
  6. 6Centre for Genomic Regulation (CRG), The Barcelona Institute of Science and Technology, 08003 Barcelona, Spain
  7. 7Centro de Investigación Biomédica en Red de Fisiopatología de la Obesidad y Nutrición (CIBERobn), 28019 Madrid, Spain
  8. 8The Institute of Cancer Research, London SM2 5GP, UK
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Abstract

Prostate cancer (PCa) is one of the leading causes of cancer-related death among men worldwide. Considerable efforts have been devoted to developing more effective therapeutic strategies for PCa, particularly for metastatic castration-resistant prostate cancer (mCRPC), wherein resistance to androgen-receptor pathway inhibition remains a major clinical challenge. G protein-coupled receptors (GPCRs), the largest family of cell surface signaling receptors, regulate numerous physiological and pathological processes and represent major therapeutic targets across multiple diseases, including cancer. In PCa, hormone- and inflammation-related GPCRs have emerged as key regulators of tumor initiation, progression, therapeutic resistance, and metastasis. Accordingly, understanding the contribution of GPCR signaling to PCa biology may reveal novel opportunities for therapeutic intervention, particularly in mCRPC. In this review, we summarize the current knowledge on the expression and function of GPCRs in PCa development, progression, and metastasis, highlighting their potential as therapeutic targets and discussing opportunities for drug development, combination therapies, and drug repurposing.

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Cite

BibTeXRIS
BibTeX
@article{sarmentocabral2026proteincoupled,
  title = {{G Protein-Coupled Receptors in Prostate Cancer: Pathophysiological Implications and Potential for Innovative Therapeutics}},
  author = {Andre Sarmento-Cabral and Vicente Herrero-Aguayo and Prudencio Sáez-Martínez and Emilia Alors-Pérez and Antonio J. León-González and Juan L. López-Cánovas and Antonio J. Montero-Hidalgo and Manuel D. Gahete and Juan M. Jiménez-Vacas and Raúl M. Luque},
  journal = {International Journal of Molecular Sciences},
  year = {2026},
  month = oct,
  doi = {10.3390/ijms27209099},
  url = {https://www.mdpi.com/1422-0067/27/20/9099},
  note = {CC BY 4.0},
}
RIS
TY  - JOUR
TI  - G Protein-Coupled Receptors in Prostate Cancer: Pathophysiological Implications and Potential for Innovative Therapeutics
AU  - Andre Sarmento-Cabral
AU  - Vicente Herrero-Aguayo
AU  - Prudencio Sáez-Martínez
AU  - Emilia Alors-Pérez
AU  - Antonio J. León-González
AU  - Juan L. López-Cánovas
AU  - Antonio J. Montero-Hidalgo
AU  - Manuel D. Gahete
AU  - Juan M. Jiménez-Vacas
AU  - Raúl M. Luque
PY  - 2026
DA  - 2026/10/14
JO  - International Journal of Molecular Sciences
DO  - 10.3390/ijms27209099
UR  - https://www.mdpi.com/1422-0067/27/20/9099
AB  - Prostate cancer (PCa) is one of the leading causes of cancer-related death among men worldwide. Considerable efforts have been devoted to developing more effective therapeutic strategies for PCa, particularly for metastatic castration-resistant prostate cancer (mCRPC), wherein resistance to androgen-receptor pathway inhibition remains a major clinical challenge. G protein-coupled receptors (GPCRs), the largest family of cell surface signaling receptors, regulate numerous physiological and pathological processes and represent major therapeutic targets across multiple diseases, including cancer. In PCa, hormone- and inflammation-related GPCRs have emerged as key regulators of tumor initiation, progression, therapeutic resistance, and metastasis. Accordingly, understanding the contribution of GPCR signaling to PCa biology may reveal novel opportunities for therapeutic intervention, particularly in mCRPC. In this review, we summarize the current knowledge on the expression and function of GPCRs in PCa development, progression, and metastasis, highlighting their potential as therapeutic targets and discussing opportunities for drug development, combination therapies, and drug repurposing.
SN  - 1422-0067
ER  -