The groups of Marvin Caruthers (University of Colorado at Boulder, USA) and Michael Gait (Medical Research Council Centre, Cambridge, UK) describe a new chemical synthesis and biological properties of 2’-O-methyl oligoribonucleotides (ORNs) containing internucleotide linkages modified with phosphonoacetate (PACE) and thiophosphonoacetate (thioPACE) groups.
ThioPACE modifications were found to greatly improve the efficiency of cell uptake and the potency of a 2′-O-Me-ORN miRNA122 inhibitor, showing that this class of modifications has great potential for applications in RNA therapeutics research.
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Synthesis and biological activity of phosphonoacetate- and thiophosphonoacetate-modified 2′-O-methyl oligoribonucleotides
Richard N. Threlfall, Adrian G. Torres, Angelika Krivenko, Michael J. Gait and Marvin H. Caruthers
Org. Biomol. Chem., 2012, Advance Article
DOI: 10.1039/C1OB06614E
