bims-limsir Biomed News
on Lipophilic modified siRNAs
Issue of 2023‒02‒26
two papers selected by
Ivan V. Chernikov
Institute of Сhemical Biology and Fundamental Medicine of the SB RAS


  1. Org Biomol Chem. 2023 Feb 20.
      With the recent success of GalNAc and the need for extra-hepatic RNAi delivery systems, other receptor-targeting ligands, like folate, have gained increased attention. The folate receptor is an important molecular target in cancer research, as it is overexpressed on numerous tumours while having limited expression in non-malignant tissues. Despite the promise of folate conjugation as a delivery platform in cancer therapeutics, its application in RNAi has been limited by sophisticated, and often expensive, chemistry. Here, we report a straightforward and cost-effective strategy to synthesize a novel folate derivative phosphoramidite for siRNA incorporation. In the absence of a transfection carrier, these siRNAs were selectively taken up by folate receptor-expressing cancer cell lines and displayed potent gene-silencing activity.
    DOI:  https://doi.org/10.1039/d3ob00093a
  2. Nature. 2023 Feb 22.
      RNA silencing relies on specific and efficient processing of double-stranded RNA by Dicer, which yields microRNAs (miRNAs) and small interfering RNAs (siRNAs)1,2. However, our current knowledge of the specificity of Dicer is limited to the secondary structures of its substrates: a double-stranded RNA of approximately 22 base pairs with a 2-nucleotide 3' overhang and a terminal loop3-11. Here we found evidence pointing to an additional sequence-dependent determinant beyond these structural properties. To systematically interrogate the features of precursor miRNAs (pre-miRNAs), we carried out massively parallel assays with pre-miRNA variants and human DICER (also known as DICER1). Our analyses revealed a deeply conserved cis-acting element, termed the 'GYM motif' (paired G, paired pyrimidine and mismatched C or A), near the cleavage site. The GYM motif promotes processing at a specific position and can override the previously identified 'ruler'-like counting mechanisms from the 5' and 3' ends of pre-miRNA3-6. Consistently, integrating this motif into short hairpin RNA or Dicer-substrate siRNA potentiates RNA interference. Furthermore, we find that the C-terminal double-stranded RNA-binding domain (dsRBD) of DICER recognizes the GYM motif. Alterations in the dsRBD reduce processing and change cleavage sites in a motif-dependent fashion, affecting the miRNA repertoire in cells. In particular, the cancer-associated R1855L substitution in the dsRBD strongly impairs GYM motif recognition. This study uncovers an ancient principle of substrate recognition by metazoan Dicer and implicates its potential in the design of RNA therapeutics.
    DOI:  https://doi.org/10.1038/s41586-023-05722-4