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Novel X-linked inhibitor of apoptosis protein inhibitors as probes of apoptosis in biology and medicine
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
2011-02-01
DOI10.1258/ebm.2010.010284
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
WOS记录号WOS:000290122600017
项目编号90713005 ; U01-CA113318 ; CA055164
资助机构National Natural Science Foundation of China ; Ray light Corporation ; NIH NCDDG ; NIH
引用统计
被引频次:1[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/61872
专题北京大学药学院
北京大学药学院_药物化学系
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
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GB/T 7714
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.
APA Hu, Qi.,Nie, Aihua.,Welsh, Kate.,Crisostomo, Fernando R. Pinacho.,Zhu, Xuejun.,...&Huang, Ziwei.(2011).Novel X-linked inhibitor of apoptosis protein inhibitors as probes of apoptosis in biology and medicine.EXPERIMENTAL BIOLOGY AND MEDICINE,236(2),247-251.
MLA Hu, Qi,et al."Novel X-linked inhibitor of apoptosis protein inhibitors as probes of apoptosis in biology and medicine".EXPERIMENTAL BIOLOGY AND MEDICINE 236.2(2011):247-251.
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