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学科主题: 药学
题名:
Novel X-linked inhibitor of apoptosis protein inhibitors as probes of apoptosis in biology and medicine
作者: Hu, Qi1; Nie, Aihua2; Welsh, Kate3; Crisostomo, Fernando R. Pinacho3; Zhu, Xuejun3; Li, Zhengxiang1; An, Jing3; Reed, John C.3; Zhang, Liangren1; Huang, Ziwei3,4
关键词: XIAP-BIR3 ; AVPI ; proline mimetic ; exo-2-azabicyclo[2.2.1] heptanes-3-carboxylic acid
刊名: EXPERIMENTAL BIOLOGY AND MEDICINE
发表日期: 2011-02-01
DOI: 10.1258/ebm.2010.010284
卷: 236, 期:2, 页:247-251
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Medicine, Research & Experimental
研究领域[WOS]: Research & Experimental Medicine
关键词[WOS]: AUTOMATED DOCKING ; PROLYL ; XIAP ; ISOMERIZATION ; SMAC/DIABLO ; CANCER ; SUPPRESSION ; FRAGMENTS ; CASPASES ; PEPTIDE
英文摘要:

We report here a series of new inhibitors of the X-linked inhibitor of apoptosis protein (XIAP protein) based on the SMAC-tetrapeptide AVPI. The structural novelty of these molecules is the presence of the proline mimetic exo-2-azabicyclo[2.2.1]heptane-3-carboxylic acid, leading to analogs with similar activity to the natural ligand peptide. The structure-activity relationship and computational docking studies support the convenience of this unnatural amino acid as a building block to develop new peptides or small molecules targeting the XIAP-BIR3 domain.

语种: 英语
所属项目编号: 90713005 ; U01-CA113318 ; CA055164
项目资助者: National Natural Science Foundation of China ; Ray light Corporation ; NIH NCDDG ; NIH
WOS记录号: WOS:000290122600017
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/61872
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Beijing Inst Pharmacol & Toxicol, Dept Med Chem, Beijing 100850, Peoples R China
3.Univ Calif San Diego, Burnham Inst Med Res, La Jolla, CA 92037 USA
4.Univ Calif San Diego, Dept Pathol, La Jolla, CA 92037 USA

Recommended Citation:
Hu, Qi,Nie, Aihua,Welsh, Kate,et al. Novel X-linked inhibitor of apoptosis protein inhibitors as probes of apoptosis in biology and medicine[J]. EXPERIMENTAL BIOLOGY AND MEDICINE,2011,236(2):247-251.
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