Patents by Inventor H. Lee Moffitt Cancer Center and Research Institute, Inc.

H. Lee Moffitt Cancer Center and Research Institute, Inc. has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • DUAL INHIBITORS OF FARNESYLTRANSFERASE AND GERANYLGERANYLTRANSFERASE I
    Publication number: 20130190355
    Abstract: Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC50 value of 25 nM and a whole cell H-Ras processing IC50 value of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I).
    Type: Application
    Filed: March 11, 2013
    Publication date: July 25, 2013
    Applicants: Yale University, H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: H. Lee Moffitt Cancer Center and Research Institute, Inc., Yale University