Prof. Jyoti Chattopadhyaya from Uppsala University and colleagues from India have synthesised modified siRNAs targetting the TAR region of HIV-1, some of which exhibit a four-fold enhanced half-life in serum over the native unmodified siRNA. The best compound synthesised had an IC50 more than three-fold lower than that of the native and two-fold lower than that of the existing locked nucleic acid (LNA) modified counterpart. The strategy to chemically modify the native siRNAs by substitution with the jcLNA can be considered as a significant development, leading to both enhanced siRNA efficiency and serum stability over that of the native. Read more in MedChemComm.
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