HIV has proved a difficult disease to treat, constantly mutating to evade the drugs used to treat it. An alternative line of research to traditional drug therapies is the use of siRNA techniques, in which carefully crafted segments of genetic code interfere with the viral genetic code directly, disrupting the infection.
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.
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Carba-LNA modified siRNAs targeting HIV-1 TAR region downregulate HIV-1 replication successfully with enhanced potency
Suman Dutta, Nipa Bhaduri, Neha Rastogi, Sunita G. Chandel, Jaya Kishore Vandavasi, Ram Shankar Upadhayaya and Jyoti Chattopadhyaya
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C0MD00225A
