2nd Generation FT Inhibitors
A novel delivery strategy enables highly charged FTase inhibitors to penetrate cell membranes for effective anticancer treatment by preventing Ras protein localization.
A type of mutated constitutively active protein, Ras, is seen in a significant number of cancers. There is a great deal of interest in preventing the Ras protein from localizing on cell membranes as an anticancer treatment. One way to prevent localization is to inhibit farnesyltransferase (FTase), the enzyme responsible for facilitating Ras attachment to the cell membrane. Traditional FTase inhibitors are highly charged and incapable of traversing the cell membrane to enter the cell.
Purdue University researchers have developed a strategy for intracellular delivery of the monophosphates of such FT inhibitors, which could provide an effective therapeutic approach.
Advantages:
-Intracellular delivery of inhibitors
-Enables absolute quantification of known compounds and relative quantification of unknown compounds in most cases using a single liquid chromatography-mass spectrometry (LC-MS) run
Potential Applications:
-Medical/Healthcare
-Cancer Treatment
-Biotechnology
TRL: 3
Intellectual Property:
Provisional-Patent, 2007-08-31, United States | PCT-Patent, 2008-08-29, WO | Utility Patent, 2010-02-25, United States
Keywords: Ras protein, constitutively active protein, farnesyltransferase inhibitor, FTase inhibitor, intracellular delivery, monophosphates, anticancer treatment, cancer therapy, biotechnology, liquid chromatography-mass spectrometry, Anticancer, Biotechnology, Cancer, Enzymes