具有肿瘤治疗潜力的二聚 FAPI。

IF 2 Q3 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING American journal of nuclear medicine and molecular imaging Pub Date : 2021-12-15 eCollection Date: 2021-01-01

Chunxia Qin, Yangmeihui Song, Weibo Cai, Xiaoli Lan

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引用次数: 0

摘要

放射性核素标记的成纤维细胞活化蛋白抑制剂（FAPIs）是近年来流行的核成像探针。它对肿瘤诊断具有重要意义，在肿瘤治疗方面也大有可为。然而，如何进一步提高肿瘤摄取率、延长肿瘤存留时间，从而提高疗效、减少副作用，还需要对探针进行优化。在本期 AJNMMI 杂志上，Moon 等人报道了两种方酰胺偶联 FAPI 共轭物（DOTA.(SA.FAPi)2 和 DOTAGA.(SA.FAPi)2），并用 68Ga 标记了它们。所得到的示踪剂显示出更高的肿瘤蓄积性和持久保留性，从而推动了 PET 成像的发展。使用二聚体结构为开发 FAP 抑制剂的放射治疗类似物提供了一种可行的策略。

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Dimeric FAPI with potential for tumor theranostics.

Radionuclide-labeled fibroblast activation protein inhibitors (FAPIs) are popular nuclear imaging probes in recent years. It's of great significance for tumor diagnosis and has great potential in tumor treatment. However, optimization of the probes is needed to further increase tumor uptake and prolong tumor retention for improved treatment efficacy and fewer side effects. In this issue of AJNMMI, Moon et al. reported two squaramide coupled FAPI conjugates (DOTA.(SA.FAPi)₂ and DOTAGA.(SA.FAPi)₂) and labeled them with ⁶⁸Ga. The resulted tracers showed increased tumor accumulation and persistent retention, which led to an advance in PET imaging. The use of dimeric structures provides a feasible strategy to develop radiotherapeutic analogs of FAP inhibitors.

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来源期刊

American journal of nuclear medicine and molecular imaging RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING-

自引率

4.00%

发文量

期刊介绍： The scope of AJNMMI encompasses all areas of molecular imaging, including but not limited to: positron emission tomography (PET), single-photon emission computed tomography (SPECT), molecular magnetic resonance imaging, magnetic resonance spectroscopy, optical bioluminescence, optical fluorescence, targeted ultrasound, photoacoustic imaging, etc. AJNMMI welcomes original and review articles on both clinical investigation and preclinical research. Occasionally, special topic issues, short communications, editorials, and invited perspectives will also be published. Manuscripts, including figures and tables, must be original and not under consideration by another journal.