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



: 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

Publisher: AMER CHEMICAL SOC

: 2016

: Molecular Pharmaceutics

: MOLECULAR PHARMACEUTICS

: MOL PHARMACEUT

: 13

: 7

: 2588

: 2595

: 8

: 1543-8384

DOI: https://doi.org/10.1021/acs.molpharmaceut.6b00261


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 Ga-68-1,4,7-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.



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