GRN163

What is GRN163L?
GRN163L is a telomerase inhibitor that targets active part of the telomerase RNA component. GRN163L has been shown to inhibit telomerase in cancer cells in many cancer cell lines. These include areas such as the cervix, lung, colon and many others.[1]



How does it work?
Inhibiting telomerase allows the telomeres of the mutated cancer cell to begin to wear. The ability for cancer cells to continuously reproduce is what separates them from normal cells and makes cancer such a deadly malfunction. Therefore allowing the telomeres of cancer cells shorten leads to arrested growth and finally apoptosis and death for cancer.[2]

How effective is it?
As of 2005 GRN163L has been cleared by the U.S. Food and Drug Administration to enter clinical testing. GRN163L has been to significantly decrease tumour growth in mice. If used in combination with radiation therapy GRN163L could significantly increase the effectiveness.[3]

By Peter Knipler //last edited 7/11/2011 //

References:
[1] Djojosubroto W.M, Allison C. C, Ning G, Sonja Schaetzlein, Michael P. Manns, Sergei Gryaznov, Calvin B.H, and Lenhard K.H. "Telomerase Antagonists GRN163 and GRN163L Inhibit Tumor Growth and Increase Chemosensitivity of Human Hepatoma." //Hepatology // 42.5 (2005): 1127-136. //Wiley Online Library //. Web. 06 Nov. 2011. []

[2] Calvin, Harley B. "Telomerase and Cancer Therapeutics." //Medscape News Today //. 23 June 2008. Web. 6 Nov. 2011. []

[3] Gomez-Millan J, Goldblatt E.M, Gryaznov S.M, Mendonca M.S and Herbert B.S. "Specific telomere dysfunction induced by GRN163L increases radiation sensitivity in breast cancer cells." Epub 1.67 (2006): 897-905.