doi:10.1038/nindia.2009.293 Published online 21 September 2009
Researchers have designed a new type of small molecule that inhibits the activity of ribonuclease A (RNase A), an enzyme that aids in proliferation of cancer cells1. Known as nucleoside-dibasic acid conjugates, the small inhibiting molecules prove to be promising drug candidates for a wide range of cancers.
The RNase A helps in forming new blood vessel to nourish cancer cells. There are a number of RNase inhibitors which cannot be transferred through cell membrane. The researchers synthesised a series of nucleoside-dibasic acid conjugates and tested their efficacy in inhibiting the activity of RNase A.
The major advantage of nucleoside-dibasic acid conjugates is their low ionic character facilitating better transportation through biological membranes unlike nucleosides functionalised with phosphate or pyrophosphate.
"Our study shows that nucleoside-dibasic acid conjugates can inhibit RNA-degrading activity of RNase A," says Tanmaya Pathak, one of the researchers from the department of chemistry of Indian Institute of Technology, Kharagpur. Inhibitors of such enzymatic activity could be useful as potential drug molecules, he says.
- Debnath, J. et al. Inhibition of ribonuclease A by nucleoside–dibasic acid conjugates. Bioorg. Med. Chem. 17, 6491-6495 (2009) | Article |