Structure-activity relationships of 2',5'-oligoadenylate analogue modifications of prostate-specific membrane antigen (PSMA) antagonists.
Structure-activity relationships of 2',5'-oligoadenylate analogue modifications of prostate-specific membrane antigen (PSMA) antagonists.
复制标题
前列腺特异性膜抗原 (PSMA) 拮抗剂的 2,5-寡腺苷酸类似物修饰的结构-活性关系。
DOI：
10.1080/15257770.2012.671988
复制
发表时间：
2012
期刊：
影响因子：
--
通讯作者：
Heston,WarrenDW
中科院分区：
文献类型：
--
作者：
Wang,Xinning;Tian,Haibin;Lee,Zhenghong;Heston,WarrenDW
Prostate-specific membrane antigen (PSMA) is an ideal biomarker for prostate cancer. A previously reported 2-5A conjugate RBI1033 (3) showed binding affinity more than 10 times higher than the parent urea-based compound (S)-2-(3-((S)-5-amino-1-carboxypentyl)ureido) pentanedioic acid (1). The purpose of this work is to further optimize the structure of3to identify highly selective ligands of PSMA. It was found that conjugates having 2-5A in their structure showed extraordinary improved binding affinity to PSMA compared with compound1. Removal of 2-5A significantly reduced its biological activity. The results will provide a path to agents for targeted imaging and treatment of prostate cancer.
