Comparative cell uptake study of FITC‑/177Lu‑labeled RM26 monomer, dimer and trimer on PC‑3: improving binding affinity of gastrin releasing peptide receptor (GRPR) antagonist via bivalency. trivalency.
Comparative cell uptake study of FITC‑/177Lu‑labeled RM26 monomer, dimer and trimer on PC‑3: improving binding affinity of gastrin releasing peptide receptor (GRPR) antagonist via bivalency. trivalency.
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PC-3 上 FITC/Lu-177 标记的 RM26 单体、二聚体和三聚体的比较细胞摄取研究：通过二价/三价提高胃泌素释放肽受体 (GRPR) 拮抗剂的结合亲和力
DOI：
10.1007/s10967-018-6396-x
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发表时间：
--
影响因子：
1.6
通讯作者：
赵鹏
中科院分区：
文献类型：
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作者：
卓连刚;杨夏;廖伟;王静;王海麟;吕敏丽;王关全;宋虎;冯悦;陈跃;魏洪源;杨宇川;赵鹏
胃泌素释放肽受体（GRPRs）在多种肿瘤中的过度表达，为GRPR靶向肿瘤放射学诊断和治疗提供了可能。在最近的报道中，GPPR拮抗剂表现出比激动剂更上级的特异性靶向亲和力。然而，拮抗剂在其结合亲和力和生物分布特性方面存在许多缺点。在这项研究中，我们设计了二聚体/三聚体拮抗剂，以解决放射治疗的要求。结果表明，RM 26的二聚体和三聚体衍生物都出现了渐进的改善。本研究为改善GRPR拮抗剂类似物的肿瘤蓄积特性提供了有效的策略。
The gastrin releasing peptide receptors (GRPRs) overexpress in various tumors, which provided the opportunity for GRPR targeted tumor radiological diagnosis and therapy. In recent reports, the GPPR antagonists presented superior specific targeting affinity over the agonists. However, antagonists suffer from many shortcomings regarding their binding affinity and biodistribution properties. In this study, we designed the dimer/trimer antagonists to address the radiotherapy requirements. The results showed both of dimer and trimer RM26 derivatives appeared a progressive improvement. This study provided an efficient strategy to improve the tumor accumulation properties for the GRPR antagonist analogs.