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Improved version of an anti-cancer drug

In 2013, Prof Sathees Raghavan and his group at IISc discovered a highly promising anti-cancer drug – a small molecule that targets cancerous cells and arrests the biochemical pathways meant for repairing DNA, leading to cell death. In order to facilitate its entry inside the cells, the group has now come up with an improved version of SCR7, called “ESCR7”.

In a recent study, a group led by Prof Raghavan and Prof. Jinu George has modified the SCR7 by encapsulating it in a polymer. The new compound, ESCR7, is much more efficient than its predecessor.

“Here we report the synthesis and characterization of an improved version of SCR7, called ESCR7, which was developed by encapsulating it in a nano-carrier, so as to improve its bio-availability. Using different cell biology assays, we show that ESCR7 is around 5 times more efficient than its parent compound, in induction of toxicity in cancer cells”, said Prof. Sathees, summarising his research. The study was the result of collaboration between Indian Institute of Science, Bangalore, Sacred Heart College, Kochi, Bhabha Atomic Research Centre, Mumbai, KLE University, Bangalore and was published in the journal Macromolecular Bioscience.

Prof Raghavan was awarded the Shanti Swarup Bhatnagar Prize 2013 for his and his group’s work, leading to the discovery of SCR7 (5,6-Bis(benzylideneamino)-2-mercaptopyrimidin-4-ol). It acts by binding to a protein found in mammals called Ligase IV, which arrests the DNA repair pathway. Prof. Sathees and his team demonstrated that SCR7 can be effective in treating different types of cancer on its own, and when paired with conventional cancer treatments like chemotherapy and radiation.

“Encapsulation of drug in nano sized carriers like polymers or artificially synthesised molecules helps in easy transport of the drugs to target cells through the blood stream, and also prevents the drug from getting degraded before being released”, said Supriya Vartak, one of the authors from Indian Institute of Science. This allows for the use of smaller doses of the drugs. SCR7 was encapsulated within a polymer material known as “Pluronic block copolymers”. This increased its solubility in water and thus its bio-availability ie. the body’s ability to absorb and utilise the drug.

About the authors:

Dr. Sathees C. Raghavan is an Associate Professor in the Department of Biochemistry, Indian Institute of Science, Bangalore. Dr. Jinu George is an Assistant Professor in the Department of Chemistry, Sacred Heart College Thevara at Kochi, Kerala.

Contact:

Sathees Raghavan: http://biochem.iisc.ernet.in/sathees.htm080 2293 2674 (office); sathees@biochem.iisc.ernet.in, sathees.chukkuru@gmail.com,

Jinu George: jinujacobv@gmail.com

The paper appeared in the journal Macromolecular Bioscience during December 2014. http://onlinelibrary.wiley.com/doi/10.1002/mabi.201400480/abstract