Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity

…, J Brekken, K Lundgren, R Grecko…

文献索引：Kasibhatla, Srinivas R.; Hong, Kevin; Biamonte, Marco A.; Busch, David J.; Karjian, Patricia L.; Sensintaffar, John L.; Kamal, Adeela; Lough, Rachel E.; Brekken, John; Lundgren, Karen; Grecko, Roy; Timony, Gregg A.; Ran, Yingqing; Mansfield, Robert; Fritz, Lawrence C.; Ulm, Edgar; Burrows, Francis J.; Boehm, Marcus F. Journal of Medicinal Chemistry, 2007 , vol. 50, # 12 p. 2767 - 2778

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被引用次数: 106

摘要

Heat shock protein 90 (Hsp90) is a molecular chaperone protein implicated in stabilizing the conformation and maintaining the function of many cell-signaling proteins. Many oncogenic proteins are more dependent on Hsp90 in maintaining their conformation, stability, and maturation than their normal counterparts. Furthermore, recent data show that Hsp90 exists in an activated form in malignant cells but in a latent inactive form in normal tissues, ...