Molecular imaging of ectopic metabotropic glutamate 1 receptor in melanoma with a positron emission tomography radioprobe 18 F-FITM.
Molecular imaging of ectopic metabotropic glutamate 1 receptor in melanoma with a positron emission tomography radioprobe 18 F-FITM.
复制标题
使用正电子发射断层扫描放射性探针 18 F-FITM 对黑色素瘤中异位代谢型谷氨酸 1 受体进行分子成像。
DOI：
10.1002/ijc.28842
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发表时间：
2014
影响因子：
6.4
通讯作者：
Zhang MR.
中科院分区：
文献类型：
--
作者：
Xie L;Yui J;Fujinaga M;Hatori A;Yamasaki T;Kumata K;Wakizaka H;Furutsuka K;Takei M;Jin ZH;Furukawa T;Kawamura K;Zhang MR.
使用具有特定放射性探针的正电子发射断层扫描（PET）的肿瘤成像将促进个体化癌症管理。有证据表明，异位表达的代谢型谷氨酸1（mGlu1）受体独立地诱导黑素细胞癌变，因此它正成为黑色素瘤个性化诊断和治疗策略的重要靶点。在这里，我们报告了一种基于癌蛋白的PET成像平台在黑色素瘤中的开发，用于使用新型mGlu1特异性放射性探针4 - 18 F-氟-N-[4-[6-（异丙基氨基）嘧啶-4-基]-1，3-噻唑-2-基]-N-甲基苯甲酰胺（18 F-FITM）对mGlu1进行无创可视化和定量。18 F-FITM显示出优异的药代动力学，即在mGlu1阳性黑色素瘤中与mGlu1阴性肝癌和正常组织中的密集和特异性蓄积。此外，放射性的蓄积水平对应于肿瘤的程度以及黑素瘤和黑素瘤转移中mGlu1蛋白表达的水平。作为一种无创的个性化诊断工具，18F-FI TM PET成像平台有望为制定个性化治疗策略、临床试验、患者管理和了解mGlu1触发的黑色素瘤肿瘤学事件开辟新途径。
Oncoimaging using positron emission tomography (PET) with a specific radioprobe would facilitate individualized cancer management. Evidence indicates that ectopically expressed metabotropic glutamate 1 (mGlu1) receptor independently induces melanocyte carcinogenesis, and it is therefore becoming an important target for personalized diagnosis and treatment strategies for melanomas. Here, we report the development of an oncoprotein‐based PET imaging platform in melanomas for noninvasive visualization and quantification of mGlu1 with a novel mGlu1‐specific radioprobe, 4‐18F‐fluoro‐N‐[4‐[6‐(isopropyl amino)pyrimidin‐4‐yl]‐1,3‐thiazol‐2‐yl]‐N‐methylbenzamide (18F‐FITM).18F‐FITM shows excellent pharmacokinetics, namely the dense and specific accumulation in mGlu1‐positive melanomasversusmGlu1‐negative hepatoma and normal tissues. Furthermore, the accumulation levels of radioactivity corresponded to the extent of tumor and to levels of mGlu1 protein expression in melanomas and melanoma metastasis. The18F‐FITM PET imaging platform, as a noninvasive personalized diagnostic tool, is expected to open a new avenue for defining individualized therapeutic strategies, clinical trials, patient management and understanding mGlu1‐triggered oncologic events in melanomas.