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Medical Biochemistry

Molecular and Cellular Biochemistry Faculty Patents

Analogs

Publication Year

Articles 1 - 2 of 2

Full-Text Articles in Medicine and Health Sciences

Stilbene Analogs And Methods Of Treating Cancer, David Watt, Chunming Liu, Vitaliy M. Sviripa, Wen Zhang Mar 2014

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 Sep 2001

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 …