Understanding an Apoptosis Signal

了解细胞凋亡信号

• 批准号: 7115799
• 负责人: George L McLendon
• 金额: $ 27.37万
• 依托单位: DUKE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2000
• 资助国家: 美国
• 起止时间: 2000-02-01 至 2007-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7115799
• 关键词: HeLa cells; X ray crystallography; antineoplastics; apoptosis; binding proteins; biological signal transduction; biomimetics; biotechnology; cysteine endopeptidases; cytochrome c; cytoplasm; enzyme activity; gene expression; intracellular transport; membrane potentials; mitochondrial membrane; neoplasm /cancer photoradiation therapy; neoplasm /cancer radiodiagnosis; neoplastic cell; nuclear magnetic resonance spectroscopy; peptides; protein localization; protein structure function; protein transport

DESCRIPTION (provided by applicant): The protein 'Smac' (or Smac/Diablo) plays an important role in programmed cell death, (apoptosis) by down regulating the inhibitor of apoptosis (lAP) proteins, which are overexpressed in many cancers. The proposed studies first examine how Smac is mobilized within the death pathway under various death stimuli. Furthermore, we explore the utility of Smac small molecule peptide mimics for use in diagnostic imaging of cancers via novel molecular targeting. We also explore the use of Smac mimetics as general, small molecule as anticancer agents to avert, or kill tumor cells.

描述（由申请人提供）：蛋白质“Smac”（或 Smac/Diablo）通过下调在许多癌症中过度表达的细胞凋亡抑制剂（IAP）蛋白，在程序性细胞死亡（细胞凋亡）中发挥重要作用。 拟议的研究首先检查 Smac 在各种死亡刺激下如何在死亡途径中被动员。此外，我们还探索了 Smac 小分子肽模拟物通过新型分子靶向在癌症诊断成像中的用途。我们还探索使用 Smac 模拟物作为通用小分子抗癌剂来避免或杀死肿瘤细胞。

项目成果

Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP.

• DOI: 10.1016/j.bmc.2007.02.010
• 发表时间: 2007-04
• 期刊: Bioorganic & medicinal chemistry
• 影响因子: 3.5
• 作者: A. D. Wist;L. Gu;S. Riedl;Yigong Shi;G. Mclendon