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Full-Text Articles in Medicine and Health Sciences
Stilbene Analogs And Methods Of Treating Cancer, David Watt, Chunming Liu, Vitaliy M. Sviripa, Wen Zhang
Stilbene Analogs And Methods Of Treating Cancer, David Watt, Chunming Liu, Vitaliy M. Sviripa, Wen Zhang
Molecular and Cellular Biochemistry Faculty Patents
Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed.
For the complete abstract, please download this patent.
Farnesyl Pyrophosphate Analogs, Hans Peter Spielmann, Douglas A. Andres, Kareem A.H. Chehade
Farnesyl Pyrophosphate Analogs, Hans Peter Spielmann, Douglas A. Andres, Kareem A.H. Chehade
Molecular and Cellular Biochemistry Faculty Patents
The post-translational addition of a farnesyl moiety to the Ras oncoprotein is essential for its membrane localization and is required for both its biological activity and ability to induce malignant transformation. The present invention describes design and synthesis of a farnesylpyrophosphate (FPP) analog, 8-anilinogeranyl pyrophosphate (AGPP) that is transferred to Ras by farnesyltransferase (FTase), in which the ω-terminal isoprene unit of the farnesyl group has been replaced with an aniline functionality. AGPP potently inhibited FTase activity in vitro (IC50=0.6 μM) and is highly selective showing little inhibitory activity against either geranylgeranyl-protein transferase type I (GGTase I) (IC50 …