An Anthraquinone Scaffold for Putative, Two-Face Bim BH3 alpha-Helix Mimic

doi:10.1021/jm301504b

QIBEBT-IR > 代谢物组学研究组

	An Anthraquinone Scaffold for Putative, Two-Face Bim BH3 alpha-Helix Mimic
	Zhang, Zhichao 1; Li, Xiangqian 1,2; Song, Ting 3; Zhao, Yan 3; Feng, Yingang4
	2012-12-13
发表期刊	JOURNAL OF MEDICINAL CHEMISTRY
卷号	55 期号:23 页码:10735-10741
摘要	Bim BH3 peptide features an alpha-helix with hotspot residues on multiple faces. Compound 5 (6-bromo-2,3-dihydroxyanthracene-9,10-dione), which adopts a rigid-plan amphipathic conformation, was designed and evaluated as a scaffold to mimic two faces of Bim a-helix. It reproduced the functionalities of both D67 and 165 on two opposing helical sides. Moreover, it maintained the two-faced binding mode during further evolution. A putative BH3 a-helix mimic and nanomolar Bcl-2/Mcl-1 dual inhibitor, 6, was obtained based on the structure of 5.
文章类型	Article
WOS标题词	Science & Technology ; Life Sciences & Biomedicine
DOI	10.1021/jm301504b
关键词[WOS]	BCL-2 FAMILY ; PROTEINS ; ANTAGONISTS ; INHIBITORS ; DISCOVERY ; APOPTOSIS ; BCL-X(L) ; DESIGN ; DEATH ; MCL-1
收录类别	SCI ; IC
语种	英语
WOS研究方向	Pharmacology & Pharmacy
WOS类目	Chemistry, Medicinal
WOS记录号	WOS:000312227300036
引用统计	被引频次：29[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	http://ir.qibebt.ac.cn/handle/337004/6387
专题	代谢物组学研究组
作者单位	1.Dalian Univ Technol, Sch Chem, State Key Lab Fine Chem, Dalian 116012, Peoples R China 2.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China 3.Dalian Univ Technol, Sch Life Sci & Technol, Dalian 116024, Peoples R China 4.Chinese Acad Sci, Qingdao Inst BioEnergy & Bioproc Technol, Qingdao 266101, Peoples R China
推荐引用方式 GB/T 7714	Zhang, Zhichao,Li, Xiangqian,Song, Ting,et al. An Anthraquinone Scaffold for Putative, Two-Face Bim BH3 alpha-Helix Mimic[J]. JOURNAL OF MEDICINAL CHEMISTRY,2012,55(23):10735-10741.
APA	Zhang, Zhichao,Li, Xiangqian,Song, Ting,Zhao, Yan,&Feng, Yingang.(2012).An Anthraquinone Scaffold for Putative, Two-Face Bim BH3 alpha-Helix Mimic.JOURNAL OF MEDICINAL CHEMISTRY,55(23),10735-10741.
MLA	Zhang, Zhichao,et al."An Anthraquinone Scaffold for Putative, Two-Face Bim BH3 alpha-Helix Mimic".JOURNAL OF MEDICINAL CHEMISTRY 55.23(2012):10735-10741.