C-X-C motif趋化因子受体4（CXCR4）在各种生理功能中起着关键作用，如免疫过程和疾病发展，并可以影响肿瘤的血管生成、增殖和远处转移。最近，已经开发了几种用于靶向CXCR4进行诊断的放射性配体，包括肽、小分子和纳米团簇，从而为基于CXCR4的新诊断策略提供了可能。在本文中，我们重点关注CXCR4靶向放射性配体在肿瘤诊断中的最新研究进展。我们讨论了它们在血液系统肿瘤（如淋巴瘤、多发性骨髓瘤、慢性淋巴细胞白血病和骨髓增生性肿瘤）以及非血液系统肿瘤（包括食管、乳腺和中枢神经系统肿瘤）的诊断中的应用。此外，我们还探讨了CXCR4靶向放射性配体在肿瘤治疗诊断一体化应用（theranostic applications）方面的应用。使用核医学靶向CXCR4作用显示出作为肿瘤诊断方法的前景，并需要进一步研究以提高其临床适用性。 版权所有 © 2023 The Korean Society of Radiology.

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.Copyright © 2023 The Korean Society of Radiology.