1374847-68-3

Upstream product

• 64987-85-5 4-(N-maleimidomethyl)cyclohexane-1-carboxylic acid N-succinimidyl ester 
• 1374749-52-6 2',5'-oligoadenylate trimer{[(2R,5R)-5-(6-amino-9H-purin-9-yl)-4-[({[2R,5R-5-(6-amino-9H-purin-yl)-4-[({[2R,5R-5-(6-amino-9H-purinyl)-4-({[(6-aminohexyl)oxy](hydroxy)phosphoryl}oxy)-3-hydroxyoxolan-2-yl]-methoxy}(hydroxy)phosphoryl)oxy]-3-hydroxyoxolan-2-yl]methoxy}(hydroxy)phosphoryl)oxy]-3-hydroxyoxolan-2-yl]methoxy}phosphonic acid 

Downstream Products

• 1374847-69-4 2-[({2-[(1-{[4-({6-[({[(2R,5R)-2-(6-amino-9H-purin-9-yl)-5-{[({[(2R, 5R)-2-(6-amino-9H-purin-9-yl)-5-{[({[(2R,5R)-2-(6-amino-9H-purin-9-yl)-4-hydroxy-5-[(phosphonooxy)methyl]oxolan-3-yl]oxy}(hydroxy)phosphoryl)oxy]methyl}-4-hy-droxyoxolan-3-yl]oxy}(hydroxy)phosphoryl)oxy]methyl}-4-hydroxyoxolan-3-yl]oxy} (hydroxy)phosphoryl)oxy]hexyl}carbamoyl)cyclohexyl]methyl}-2,5-dioxopyrrolidin-3-yl)sulfanyl]-1-carboxyethyl}carbamoyl)amino]pentanedioic acid 

Relevant academic research and scientific papers

Structure-activity relationships of 2′,5′-oligoadenylate analogue modifications of prostate-specific membrane antigen (PSMA) antagonists

□ 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.