1374847-75-2Relevant academic research and scientific papers
Structure-activity relationships of 2′,5′-oligoadenylate analogue modifications of prostate-specific membrane antigen (PSMA) antagonists
Wang, Xinning,Tian, Haibin,Lee, Zhenghong,Heston, Warren D. W.
, p. 432 - 444 (2012/08/14)
□ 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 of 3 to 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 compound 1. 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. Copyright Taylor and Francis Group, LLC.
