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Review
. 2025 Apr;1880(2):189266.
doi: 10.1016/j.bbcan.2025.189266. Epub 2025 Jan 27.

An update on regulation and function of G protein-coupled receptors in cancer: A promising strategy for cancer therapy

Affiliations
Review

An update on regulation and function of G protein-coupled receptors in cancer: A promising strategy for cancer therapy

Lin Li et al. Biochim Biophys Acta Rev Cancer. 2025 Apr.

Abstract

G protein-coupled receptors (GPCRs) are a large family of cell surface receptors that play a crucial role in signal transduction and cellular communication. GPCR proteins are involved in a wide range of physiological processes, including cell growth, migration, and survival. Dysregulation of GPCR protein expression has been implicated in the pathogenesis of various diseases, including cancer, and GPCR proteins have been shown to modulate these processes in various types of cancer, highlighting their importance as potential therapeutic targets. In this review, we summarize the expression regulation of GPCRs in cancer cells, update the various ways by which the abnormal expression of GPCR protein affects the behavior of tumor cells, and discuss the current research directions and potentially facing problems of strategies on GPCR-targeting therapy.

Keywords: Cancer; Expression; Function; GPCR; Therapy.

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Conflict of interest statement

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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