Research Progress of CXCR4-Targeting Radioligands for Oncologic Imaging
1Key Laboratory for Experimental Teratology of the Ministry of Education and Research Center for Experimental Nuclear Medicine, School of Basic Medical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, China.
Abstract:
C-X-C motif chemokine receptor 4 (CXCR4) plays a key role in various physiological functions, such as immune processes and disease development, and can influence angiogenesis, proliferation, and distant metastasis in tumors. Recently, several radioligands, including peptides, small molecules, and nanoclusters, have been developed to target CXCR4 for diagnostic purposes, thereby providing new diagnostic strategies based on CXCR4. Herein, we focus on the recent research progress of CXCR4-targeting radioligands for tumor diagnosis. We discuss their application in the diagnosis of hematological tumors, such as lymphomas, multiple myelomas, chronic lymphocytic leukemias, and myeloproliferative tumors, as well as nonhematological tumors, including tumors of the esophagus, breast, and central nervous system. Additionally, we explored the theranostic applications of CXCR4-targeting radioligands in tumors. Targeting CXCR4 using nuclear medicine shows promise as a method for tumor diagnosis, and further research is warranted to enhance its clinical applicability.
Insights
Radioligands targeting C-X-C motif chemokine receptor 4 (CXCR4) show promise for diagnosing various cancers. These CXCR4-targeting agents are advancing tumor diagnosis and theranostics, particularly in hematological and nonhematological malignancies.
Area of Science:
- Oncology
- Nuclear Medicine
- Molecular Imaging
Background:
- C-X-C motif chemokine receptor 4 (CXCR4) is implicated in critical physiological processes and tumor progression, including metastasis.
- CXCR4 influences tumor angiogenesis, proliferation, and the development of distant metastases.
- Recent advancements have led to the development of diverse radioligands targeting CXCR4 for diagnostic applications.
Purpose of the Study:
- To review recent research on CXCR4-targeting radioligands for tumor diagnosis.
- To discuss the application of these radioligands in diagnosing various hematological and nonhematological tumors.
- To explore the potential theranostic applications of CXCR4-targeting radioligands in oncology.
Main Methods:
- Literature review of recent research progress in CXCR4-targeting radioligands.
- Analysis of radioligand applications in the diagnosis of hematological tumors (lymphomas, multiple myeloma, CLL, myeloproliferative tumors).
- Evaluation of radioligand utility in nonhematological tumors (esophageal, breast, CNS) and theranostic applications.
Main Results:
- Development of various radioligands (peptides, small molecules, nanoclusters) for CXCR4-based tumor diagnosis.
- Demonstrated utility of CXCR4-targeting radioligands in diagnosing a spectrum of hematological malignancies.
- Evidence of application in diagnosing nonhematological tumors and emerging theranostic potential.
Conclusions:
- Targeting CXCR4 with nuclear medicine offers a promising avenue for tumor diagnosis.
- CXCR4-targeting radioligands have shown significant potential in both diagnostic and theranostic oncology applications.
- Further research is essential to optimize and enhance the clinical applicability of these agents.


