A Small Molecule RAS-Mimetic Disrupts RAS Association with Effector Proteins to Block Signaling
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- 作者：Sai Krishna Athuluri-Divakar1 ; 2 ; Rodrigo Vasquez-Del Carpio1 ; 2 ; Kaushik Dutta3 ; Stacey J. Baker1 ; 2 ; Stephen C. Cosenza1 ; 2 ; Indranil Basu5 ; Yogesh K. Gupta1 ; 2 ; M.V. Ramana Reddy1 ; 2 ; Lynn Ueno4 ; Jonathan R. Hart4 ; Peter K. Vogt4 ; David Mulholland1 ; 2 ; Chandan Guha5 ; Aneel K. Aggarwal1 ; 2 ; E. Premkumar Reddy1 ; 2 ; ep.reddy@mssm.edu" class="auth_mail" title="E-mail the corresponding author
- 关键词：MAPK ; PI3K ; RAF ; RAS ; RAS-binding domain ; rigosertib
- 刊名：Cell
- 出版年：2016
- 出版时间：21 April 2016
- 年：2016
- 卷：165
- 期：3
- 页码：643-655
- 全文大小：5413 K
文摘
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Rigosertib binds to the RAS-binding domains (RBDs) of multiple RAS effectors
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Binding of rigosertib to RAF-RBD inhibits RAS-RAF interaction and impairs the kinase
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Rigosertib inhibits MEK-ERK pathway activated by growth factors and oncogenic RAS