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Development of SHIP activators: Potentially selective cancer therapy.

TitleDevelopment of SHIP activators: Potentially selective cancer therapy.
Publication TypeConference Paper
Year of Publication2010
AuthorsMeimetis, LG, Nodwell, M, Wang, C, Yang, L, Mui, AL, Ong, C, Krystal, G, Andersen, RJ
Date Published2010///
PublisherAmerican Chemical Society
Abstract

An exciting avenue for drug development was recently uncovered with the discovery of the enzyme SHIP (SH2-contg. inositol 5’-phosphatase) in the PI3K pathway. SHIP is an ideal drug target, because it is only expressed in blood cells. Turning off aberrant PI3K signaling in cancer cells, by activation of SHIP, has been proposed to be a promising approach to treating blood cancers such as multiple myeloma, while minimizing off target effects. An extensive natural product screening program for SHIP activators identified the meroterpenoid pelorol as a promising lead compd. The work to be presented will describe the logical design and synthesis of drug candidates based on the lead structure of the natural product pelorol. Biol. data, including enzyme and cell based assays, in vivo studies of the candidate mols., and evaluation of enzyme-drug candidate interactions using STD (satn. transfer difference) NMR spectroscopy will also be described. [on SciFinder(R)]