کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10730519 | 1042560 | 2009 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Automated synthesis of an 18F-labelled pyridine-based alkylating agent for high yield oligonucleotide conjugation
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
فیزیک و نجوم
تشعشع
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چکیده انگلیسی
Alkylating agents have been shown to be very promising for the radiolabelling of oligonucleotides with fluorine-18. In this report we describe the fully automated synthesis of 2-bromo-N-[3-(2-[18F]fluoropyridin-3-yloxy)propyl]acetamide ([18F]FPyBrA) utilizing a modular synthesis unit. Reaction conditions for the coupling of this pyridine-based alkylating agent at the 5Ⲡend of a fully phosphorothioated random 20-mer DNA sequence were optimized to achieve very high radiochemical yields (>90%) and a maximum specific activity of 5-6 GBq/μmoL. The potential for rapid purification by solid phase extraction without need of chromatographic isolation of the radiolabelled oligonucleotide presents an overall benefit for the application of oligonucleotides in preclinical studies and potential clinical applications.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Applied Radiation and Isotopes - Volume 67, Issue 9, September 2009, Pages 1670-1675
Journal: Applied Radiation and Isotopes - Volume 67, Issue 9, September 2009, Pages 1670-1675
نویسندگان
Elisabeth von Guggenberg, Jayden A. Sader, John S. Wilson, Soraya Shahhosseini, Ingrid Koslowsky, Frank Wuest, John R. Mercer,