(68)Ga-DOTA-GGNle-CycMSH(hex) targets the melanocortin-1 receptor for melanoma imaging.
(68)Ga-DOTA-GGNle-CycMSH(hex) targets the melanocortin-1 receptor for melanoma imaging.
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DOI：
10.1126/scitranslmed.aau4445
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发表时间：
2018-11-07
影响因子：
17.1
通讯作者：
Miao Y
中科院分区：
文献类型：
--
作者：
Yang J;Xu J;Gonzalez R;Lindner T;Kratochwil C;Miao Y
黑素皮质素-1受体（MC 1 R）是黑色素瘤成像和治疗的分子靶点，因为它在啮齿动物和人黑色素瘤细胞上过表达。在此，我们用鼠和人黑素瘤细胞以及鼠和异种移植肿瘤评估了68 Ga-DOTA-GGNle-CycMSHhex和Cy5.5-GGNle-CycMSHhex的MC 1 R靶向和特异性。68 Ga-DOTA-GGNle-CycMSHhex首次在人体中用作成像探针，以评估放射性核素治疗晚期黑色素瘤患者的可能性。68 Ga-DOTA-GGNle-CycMSHhex和Cy5.5-GGNle-CycMSHhex在鼠和人黑素瘤细胞中以及在鼠黑素瘤和人黑素瘤异种移植肿瘤中显示MC 1 R特异性靶向性质。B16/F10和M21黑色素瘤病变都可以通过使用68 Ga-DOTA-GGNle-CycMSHhex的正电子发射断层扫描（PET）容易地成像。患者中黑色素瘤脑转移的首次人体图像证明了MC 1 R作为黑色素瘤成像的分子靶标的临床相关性，突出了68 Ga-DOTA-GGNle-CycMSHhex作为MC 1 R靶向黑色素瘤成像探针的潜力，并强调了开发MC 1 R靶向治疗剂用于治疗转移性黑色素瘤患者的必要性。68 Ga-DOTA-GGNle-CycMSHhex是一种放射性标记的黑皮质素-1受体靶向成像探针，可在首次人体试验中检测黑色素瘤。
Melanocortin-1 receptor (MC1R) is a molecular target for melanoma imaging and therapy due to its overexpression on rodent and human melanoma cells. Here we evaluated the MC1R targeting and specificity of 68Ga-DOTA-GGNle-CycMSHhex and Cy5.5-GGNle-CycMSHhex with murine and human melanoma cells, and murine and xenografted tumors. 68Ga-DOTA-GGNle-CycMSHhex was used first-in-human as an imaging probe to evaluate the possibility of radionuclide therapy in advanced stage melanoma patients. 68Ga-DOTA-GGNle-CycMSHhex and Cy5.5-GGNle-CycMSHhex displayed MC1R-specific targeting properties in murine and human melanoma cells, as well as in murine melanoma and human melanoma-xenografted tumors. Both B16/F10 and M21 melanoma lesions could be easily imaged by positron emission tomography (PET) using 68Ga-DOTA-GGNle-CycMSHhex. The first-in-human images of melanoma brain metastases in patients demonstrated the clinical relevance of MC1R as a molecular target for melanoma imaging, highlighting the potential of 68Ga-DOTA-GGNle-CycMSHhex as a MC1R-targeting melanoma imaging probe and underscoring the need to develop MC1R-targeting therapeutic agents for treating patients with metastatic melanomas. 68Ga-DOTA-GGNle-CycMSHhex, a radiolabeled melanocortin-1 receptor-targeting imaging probe, detects melanoma in first-in-human testing..
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DOI：
10.1056/nejmoa1003466
发表时间：
2010-08-19
期刊：
The New England journal of medicine
影响因子：
--
作者：
Hodi FS;O'Day SJ;McDermott DF;Weber RW;Sosman JA;Haanen JB;Gonzalez R;Robert C;Schadendorf D;Hassel JC;Akerley W;van den Eertwegh AJ;Lutzky J;Lorigan P;Vaubel JM;Linette GP;Hogg D;Ottensmeier CH;Lebbé C;Peschel C;Quirt I;Clark JI;Wolchok JD;Weber JS;Tian J;Yellin MJ;Nichol GM;Hoos A;Urba WJ
通讯作者：
Urba WJ
DOI：
10.2967/jnumed.110.086009
发表时间：
2011-04
期刊：
Journal of nuclear medicine : official publication, Society of Nuclear Medicine
影响因子：
--
作者：
Guo H;Yang J;Gallazzi F;Miao Y
通讯作者：
Miao Y
影响因子：
2.7
作者：
Liu, Liqin;Xu, Jingli;Miao, Yubin
通讯作者：
Miao, Yubin
影响因子：
3.5
作者：
Yang, Jianquan;Hu, Chien-An A.;Miao, Yubin
通讯作者：
Miao, Yubin
影响因子：
4.7
作者：
Miao, YB;Whitener, D;Quinn, TP
通讯作者：
Quinn, TP