{"title":"新型肿瘤成像C-X-C趋化因子受体4靶向放射性示踪剂的合成与评价。","authors":"Yanzhi Wang, Jingyue Gao, Yuze Ma, Yuan Pan, Kunyao Wang, Wenqi Zhao and Feng Gao*, ","doi":"10.1021/acs.jmedchem.5c00735","DOIUrl":null,"url":null,"abstract":"<p >C-X-C chemokine receptor 4 (CXCR4), which is overexpressed in various cancers, has been considered as an important target for cancer theranostics. In this study, a series of small molecule radiotracers targeting CXCR4 were developed and obtained with high radiochemical purity (>95%). Among seven radiotracers, [<sup>68</sup>Ga]Ga-SDNUM04 showed favorable binding affinity (<i>K</i><sub>d</sub> = 32.21 ± 0.71 nM), tumor uptake (SUV<sub>mean</sub> = 0.63 ± 0.02) and tumor-to-liver ratio (T/L = 1.07). In addition, [<sup>68</sup>Ga]Ga-SDNUM04 exhibited satisfactory imaging outcomes and biodistribution properties in various CXCR4-positive tumors, making it a promising radiotracer for the clinical diagnosis of CXCR4-positive cancers.</p>","PeriodicalId":46,"journal":{"name":"Journal of Medicinal Chemistry","volume":"68 16","pages":"17221–17235"},"PeriodicalIF":6.8000,"publicationDate":"2025-08-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and Evaluation of Novel C-X-C Chemokine Receptor 4-Targeted Radiotracers for Oncological Imaging\",\"authors\":\"Yanzhi Wang, Jingyue Gao, Yuze Ma, Yuan Pan, Kunyao Wang, Wenqi Zhao and Feng Gao*, \",\"doi\":\"10.1021/acs.jmedchem.5c00735\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >C-X-C chemokine receptor 4 (CXCR4), which is overexpressed in various cancers, has been considered as an important target for cancer theranostics. In this study, a series of small molecule radiotracers targeting CXCR4 were developed and obtained with high radiochemical purity (>95%). Among seven radiotracers, [<sup>68</sup>Ga]Ga-SDNUM04 showed favorable binding affinity (<i>K</i><sub>d</sub> = 32.21 ± 0.71 nM), tumor uptake (SUV<sub>mean</sub> = 0.63 ± 0.02) and tumor-to-liver ratio (T/L = 1.07). In addition, [<sup>68</sup>Ga]Ga-SDNUM04 exhibited satisfactory imaging outcomes and biodistribution properties in various CXCR4-positive tumors, making it a promising radiotracer for the clinical diagnosis of CXCR4-positive cancers.</p>\",\"PeriodicalId\":46,\"journal\":{\"name\":\"Journal of Medicinal Chemistry\",\"volume\":\"68 16\",\"pages\":\"17221–17235\"},\"PeriodicalIF\":6.8000,\"publicationDate\":\"2025-08-19\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Medicinal Chemistry\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://pubs.acs.org/doi/10.1021/acs.jmedchem.5c00735\",\"RegionNum\":1,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://pubs.acs.org/doi/10.1021/acs.jmedchem.5c00735","RegionNum":1,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Synthesis and Evaluation of Novel C-X-C Chemokine Receptor 4-Targeted Radiotracers for Oncological Imaging
C-X-C chemokine receptor 4 (CXCR4), which is overexpressed in various cancers, has been considered as an important target for cancer theranostics. In this study, a series of small molecule radiotracers targeting CXCR4 were developed and obtained with high radiochemical purity (>95%). Among seven radiotracers, [68Ga]Ga-SDNUM04 showed favorable binding affinity (Kd = 32.21 ± 0.71 nM), tumor uptake (SUVmean = 0.63 ± 0.02) and tumor-to-liver ratio (T/L = 1.07). In addition, [68Ga]Ga-SDNUM04 exhibited satisfactory imaging outcomes and biodistribution properties in various CXCR4-positive tumors, making it a promising radiotracer for the clinical diagnosis of CXCR4-positive cancers.
期刊介绍：
The Journal of Medicinal Chemistry is a prestigious biweekly peer-reviewed publication that focuses on the multifaceted field of medicinal chemistry. Since its inception in 1959 as the Journal of Medicinal and Pharmaceutical Chemistry, it has evolved to become a cornerstone in the dissemination of research findings related to the design, synthesis, and development of therapeutic agents.
The Journal of Medicinal Chemistry is recognized for its significant impact in the scientific community, as evidenced by its 2022 impact factor of 7.3. This metric reflects the journal's influence and the importance of its content in shaping the future of drug discovery and development. The journal serves as a vital resource for chemists, pharmacologists, and other researchers interested in the molecular mechanisms of drug action and the optimization of therapeutic compounds.
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