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Bioorganic & medicinal chemistry letters

Targeting the hydrophobic region of Hsp90's ATP binding pocket with novel 1, 3, 5-triazines

T Lee, YH Seo

文献索引:Lee, Taeho; Seo, Young Ho Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 23 p. 6427 - 6431

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被引用次数: 9

摘要

Abstract Heat shock protein 90 (Hsp90) is a molecular chaperone that plays an important role in regulating the maturation and stabilization of many oncogenic proteins. In an attempt to discover a new class of Hsp90 inhibitors, a series of 1, 3, 5-triazine compounds were rationally designed, synthesized, and their biological activities were evaluated. Compound 3b was found to degrade Hsp90's client proteins of Her2, Met and Akt and to induce the ...