Imaging the Distribution of Gastrin-Releasing Peptide Receptors in Cancer

Imaging the Distribution of Gastrin-Releasing Peptide Receptors in Cancer
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DOI:
10.2967/jnumed.119.234971
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发表时间:
2020-06-01
影响因子:
9.3
通讯作者:
Iagaru, Andrei
Iagaru, Andrei
中科院分区:
医学1区
文献类型:
--
作者:
Baratto, Lucia;Duan, Heying;Iagaru, Andrei

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使用选择性分子靶向肿瘤表达的受体用于诊断、治疗或诊断和治疗(治疗不确定性)目的是肿瘤学应用中有前途的方法。在过去十年中,这类做法显著增加。靶向放射性药物的肽如胃泌素释放肽受体是具有快速血液清除和尿排泄的小分子。它们表现出良好的组织扩散性、低免疫原性和与其靶细胞表面受体的高度选择性结合。它们也很容易生产。胃泌素释放肽受体是蛙皮素家族的一部分,在许多肿瘤中过表达,包括乳腺癌和前列腺癌,因此代表了未来开发的有吸引力的靶点。
Targeting tumor-expressed receptors using selective molecules for diagnostic, therapeutic, or both diagnostic and therapeutic (theragnostic) purposes is a promising approach in oncologic applications. Such approaches have increased significantly over the past decade. Peptides such as gastrin-releasing peptide receptors targeting radiopharmaceuticals are small molecules with fast blood clearance and urinary excretion. They demonstrate good tissue diffusion, low immunogenicity, and highly selective binding to their target cell-surface receptors. They are also easily produced. Gastrin-releasing peptide receptors, part of the bombesin family, are overexpressed in many tumors, including breast and prostate cancer, and therefore represent an attractive target for future development.