CHAPTER 8: Discovery of NVP-AUY922
Published:23 Oct 2013
P. A. Brough, J. Schoepfer, A. Massey, and M. R. Jensen, in Inhibitors of Molecular Chaperones as Therapeutic Agents, ed. T. D. Machajewski and Z. Gao, The Royal Society of Chemistry, 2013, pp. 213-240.
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This chapter covers the identification and characterization of the novel Hsp90 inhibitor NVP-AUY922, which entered clinical trials in July 2007. The program leading to the identification of NVP-AUY922 (VER-52296) used complementary hit ID technologies such as HTS and fragment-based screening, relied heavily on structure-based design and required the design of new assays and probes to drive the compound optimization. In vivo characterization in tumor-bearing animals assisted in compound selection for pre-clinical studies.