Maynor Michelle, Scott Sarah A, Rickert Emily L, Gibbs Richard A
Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, IN 47907, USA.
Bioorg Med Chem Lett. 2008 Mar 15;18(6):1889-92. doi: 10.1016/j.bmcl.2008.02.014. Epub 2008 Feb 12.
Protein prenyl transferases have been a focus of anti-cancer drug discovery in recent years due to their roles in post-translational modification of small GTP binding proteins. Attention is now turning to the development of GGTase I inhibitors. Here, we present the synthesis and biological evaluation of four GGPP analogs versus mammalian GGTase I and the discovery that 7-allyl GGPP is a surprisingly efficient GGTase I substrate.