HAYWARD, Calif., April 16 /PRNewswire-FirstCall/ -- Kosan Biosciences Incorporated (Nasdaq: KOSN) presented data on its novel, proprietary third-generation Hsp90 inhibitors demonstrating a high degree of target specificity, strong binding affinity and potency, a long lifetime in tumor tissue and significant antitumor activity and safety in murine xenograft and orthotopic models.
Hsp90 is a protein chaperone that acts to stabilize and/or activate a number of proteins required for cellular signaling pathways, including several known determinants of carcinogenesis such as HER2 (Erb2), B-Raf, c-Kit, Flt-3 and Raf-1. Hsp90 is effectively inhibited by benzoquinone ansamycins, such as geldanacmycin and its derivatives, which bind to the ATP binding site in the N-terminal domain. Kosan's lead Hsp90 inhibitor, tanespimycin (17-AAG), is a geldanamycin derivative. Kosan's third-generation Hsp90 inhibitors are non-benzoquinone ansamycins that have been genetically engineered to retain a high degree of specificity of tanespimycin for the ATP binding pocket of Hsp90 yet do not rely upon activation of the quinone moiety for maximal inhibitor activity. These third-generation Hsp90 inhibitors are highly potent molecules in tumor models with properties that significantly distinguish them from other Hsp90 inhibitors.
"Kosan's third-generation Hsp90 inhibitors expand our Hsp90 portfolio,
and represent opportunities for product diversification and life-cycle
extension," said Helen S. Kim, Kosan's President and Chief Executive
Officer. "Developing tanespimycin, our first generation Hsp90 inhibitor, in
multiple myeloma and in breast cancer, is Kosan's highest priority. We
believe that our next-generation molecules add value to our Hsp90 program
|SOURCE Kosan Biosciences Incorporated|
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