Synthesis of Novel Europium-Labeled Estradiol Derivatives for Time-Resolved Fluoroimmunoassays

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• 作者：Niko Meltola ; Piitu Jauria ; Petri Saviranta ; and Heikki Mikola
• 刊名：Bioconjugate Chemistry
• 出版年：1999
• 出版时间：May 1999
• 年：1999
• 卷：10
• 期：3
• 页码：325 - 331
• 全文大小：125K
• 年卷期：v.10,no.3(May 1999)
• ISSN：1520-4812

文摘

The O-(5-carboxypentyl)-, O-(4-aminobutyl)-, O-(6-aminohexyl)oximes of 2- and 4-formylestradiol aswell as the 4-carboxyethylthioether derivative of estradiol were synthesized. These estradiol derivativeswere characterized using IR-, ¹H-, and ¹³C NMR spectroscopy. All synthesized estradiol derivativeswere labeled with europium chelates. These "tracers" were purified and tested in a competitive time-resolved fluoroimmunoassay with monoclonal antibody (SSI 57-2) raised against the 6-O-(carboxymethyl)oxime-bovine serum albumin derivative of estradiol. All the tested europium-labeled estradiol-4-derivatives were bound by the antibody, whereas tracers linked via position 2 were not recognizedby this antibody. It was observed that tracers conjugated via C-4 gave more sensitive standard curvesthan tracers conjugated via C-6. Especially, the estradiol-4-thioether derivative was found to be highlyuseful in time-resolved fluoroimmunoassays of estradiol while using this antibody.