In Vivo Bone-Targeting of Bis(phosphonate)-Conjugated Double Helical RNA Monitored by Positron Emission Tomography

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• 作者：Satish Jadhav ; Meeri Käkelä ; Matthieu Bourgery ; Kiira Rimpilä ; Heidi Liljenbäck ; Riikka Siitonen ; Jussi Mäkilä ; Tiina Laitala-Leinonen ; Päivi Poijärvi-Virta ; Harri Lönnberg ; Anne Roivainen ; Pasi Virta
• 刊名：Molecular Pharmaceutics
• 出版年：2016
• 出版时间：July 5, 2016
• 年：2016
• 卷：13
• 期：7
• 页码：2588-2595
• 全文大小：516K
• 年卷期：0
• ISSN：1543-8392

文摘

A bis(phosphonate) conjugate of 2′-O-methyl oligoribonucleotide (microRNA-21) was synthesized and used as a bone-targeting carrier in the systemic delivery of a ⁶⁸Ga-1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA)-chelated 2′-O-methyl oligoribonucleotide (anti-microRNA-21). The whole-body biodistribution of the double helical RNA was monitored by positron emission tomography (PET), which verified the expected bis(phosphonate)-induced bone accumulation in healthy rats.