Chirality matters: stereo-defined phosphorothioate linkages at the termini of small interfering RNAs improve pharmacology in vivo.

In contrast, the PS absolute configuration on the sense strand did not show a clear trend with regards to its influence on the in vitro activity for the siRNAs evaluated in this study (Figure 4 Ad). siRNAs with unique PS stereochemistries confer increased potency in vivo Based on the in vitro activity data, the most promising siRNA PS configuration was R/R-S followed by S/R-S, whereas both R/S-R and S/S-R were detrimental.

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