G Protein-Coupled Receptors in Cancer Progression

A special issue of Cancers (ISSN 2072-6694). This special issue belongs to the section "Tumor Microenvironment".

Deadline for manuscript submissions: 30 October 2025 | Viewed by 1566

Special Issue Editor


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Guest Editor
Department of Neuroscience and Pharmacology, Carver College of Medicine, University of Iowa, Iowa City, IA, USA
Interests: G protein-coupled receptors; signal transduction; tumor growth and metastasis; cancer stem cells

Special Issue Information

Dear Colleagues,

G protein-coupled receptors (GPCRs), the largest family of cell surface receptors, serve as critical regulators in a myriad of cellular processes. The dysregulation of GPCR signaling pathways has been implicated in fueling tumor growth, invasion, and metastasis, thus highlighting their potential as promising therapeutic targets for cancer treatment. Numerous mutations within GPCRs and heterotrimeric G proteins have been identified, yet the full functional significance of these mutations remains incompletely understood. Moreover, despite the fact that over 30% of currently available drugs target GPCRs, their application in cancer treatment remains limited, underscoring the underexplored potential of GPCRs in the context of cancer research. Therefore, there is a compelling need to delve deeper into the intricate mechanisms governing GPCR signaling in the context of cancer progression. Such endeavors hold immense promise for unveiling novel therapeutic avenues that can effectively combat the multifaceted challenges posed by this complex disease.

With this imperative in mind, we are pleased to extend an invitation to you to contribute to our upcoming Special Issue entitled "Novel Insights into GPCR Signaling in Cancer Development". This special edition aims to compile the latest breakthroughs and pivotal discoveries in both basic and translational research concerning the role of GPCR signaling in cancer development. We eagerly welcome original research articles and comprehensive reviews that explore various aspects of this complex landscape. Topics of interest include, but are not limited to, elucidating the functions and molecular mechanisms of GPCRs and G proteins, investigating their mutations in the context of cancer development, and exploring innovative therapeutic modalities such as small-molecule inhibitors tailored to target GPCR signaling pathways in cancer.

We eagerly anticipate the submission of your invaluable contributions to enrich this Special Issue with diverse perspectives and groundbreaking insights.

Dr. Songhai Chen
Guest Editor

Manuscript Submission Information

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Keywords

  • GPCRs
  • heterotrimeric G proteins
  • signal transduction
  • mutations
  • cancer development

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Published Papers (1 paper)

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Research

11 pages, 7000 KiB  
Communication
SSTR2-Targeted Theranostics in Hepatocellular Carcinoma
by Majid Momeny, Solmaz AghaAmiri, Servando Hernandez Vargas, Belkacem Acidi, Sukhen C. Ghosh, Tyler M. Bateman, Jack T. Adams, Vahid Khalaj, Ahmed O. Kaseb, Hop S. Tran Cao and Ali Azhdarinia
Cancers 2025, 17(2), 162; https://doi.org/10.3390/cancers17020162 - 7 Jan 2025
Viewed by 1124
Abstract
Background: While the clinical use of radiolabeled somatostatin analogs is well established in neuroendocrine tumors, there is growing interest in expanding their application to other somatostatin receptor 2 (SSTR2)-expressing cancers. This study investigates the potential utility of SSTR2-targeted theranostics in hepatocellular carcinoma (HCC). [...] Read more.
Background: While the clinical use of radiolabeled somatostatin analogs is well established in neuroendocrine tumors, there is growing interest in expanding their application to other somatostatin receptor 2 (SSTR2)-expressing cancers. This study investigates the potential utility of SSTR2-targeted theranostics in hepatocellular carcinoma (HCC). Methods: SSTR2 expression in HCC cell lines and clinical samples was evaluated using qRT-PCR, Western blot analysis, and a public dataset. 67Ga-DOTATATE uptake was measured, 177Lu-DOTATATE cytotoxicity was assessed, and 68Ga-DOTATATE tumor targeting was evaluated in HCC animal models and a patient via PET/CT imaging. Results: SSTR2 expression was confirmed in HCC cell lines and clinical samples. Radioligand uptake studies demonstrated SSTR2-mediated 67Ga-DOTATATE uptake. 177Lu-DOTATATE treatment reduced cell proliferation and enhanced the anti-tumor efficacy of the multikinase inhibitor sorafenib. 68Ga-DOTATATE PET/CT scans successfully identified tumors in HCC animal models and spinal metastases in a patient with HCC. Conclusion: These findings provide evidence that SSTR2-based theranostics could have significant implications for the detection and treatment of HCC. Full article
(This article belongs to the Special Issue G Protein-Coupled Receptors in Cancer Progression)
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