Cover Picture: Deactivation of Mcl‐1 by Dual‐Function Small‐Molecule Inhibitors Targeting the Bcl‐2 Homology 3 Domain and Facilitating Mcl‐1 Ubiquitination (Angew. Chem. Int. Ed. 46/2016). Issue 46 (18th October 2016)

• Record Type: Journal Article
• Authors: Song, Ting; Wang, Ziqian; Ji, Fangling; Feng, Yingang; Fan, Yudan; Chai, Gaobo; Li, Xiangqian; Li, Zhiqiang; Zhang, Zhichao
• Is Part Of: Angewandte Chemie international edition. Volume 55:Issue 46(2016)
• Page Start: 14179
• Page End: 14179
• Publication Date: 2016-10-18
• Subjects: apoptosis -- conformation analysis -- drug design -- inhibitors -- structure elucidation; Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201609560
• Languages: English
• ISSNs: 1433-7851

Abstract

Abstract : Promotion of Mcl‐1 protein binding to the ubiquitin ligase Mule to catalyze its ubiquitination could enhance an apoptotic signaling pathway in cancer cells. In their Communication onpage 14250 ff. Z. Zhang and co‐workers identify a compound that zips these two proteins together by driving a non‐helical QRN motif on Mc1‐1 to adopt a helical conformation.