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NOVEL CYCLIC-PEPTIDE-BASED ANTIMITOTICS

NOVEL CYCLIC-PEPTIDE-BASED ANTIMITOTICS
新型环肽抗有丝分裂剂
批准号：
6385060
负责人：
Robert SCOTT LOKEY
金额：
$0.56万
依托单位：
HARVARD MEDICAL SCHOOL
依托单位国家：
美国
项目类别：
财政年份：
2001
资助国家：
美国
项目状态：
未结题
起止时间：
2001-07-01 至
来源：
https://reporter.nih.gov/project-details/6385060
关键词：
antimitotics chemical structure function cyclic peptides cyclins cytotoxicity membrane permeability peptide chemical synthesis peptide library

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中文摘要
翻译
我们将合成一个小的七肽支架文库，以探索支架构象对环化和细胞通透性的影响。我们将选择几种新的细胞渗透性的循环支架来精加工到潜在的蛋白质配体的库中，并在一些不同的分析中筛选它们对细胞周期的影响。将选择几个活性化合物进行进一步的研究。我们特别感兴趣的是那些通过直接干扰细胞周期蛋白B的降解或通过靶向有丝分裂纺锤体的组件从而触发有丝分裂检查点途径来阻止细胞有丝分裂的化合物。
英文摘要
We will synthesize a small library of heptapeptide scaffolds to explore the effects of scaffold conformation on cyclization and cell permeability. We will select several novel cell-permeable cyclic scaffolds for elaboration into libraries of potential protein ligands and screen them for effects on the cell cycle in a number of different assays. Several active compounds will be chosen for further study. We are particularly interested in compounds that arrest cells in mitosis by directly perturbing the degradation of cyclin B or by targeting components of the mitotic spindle and thus triggering the mitotic checkpoint pathway.
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会议论文
Advancing the basic science of membrane permeability in macrocyclic peptides
Upgrade of core imaging instrumentation and robotics for the UCSC Chemical Screening Center
Cyclic peptide permeability
Cyclic peptide permeability
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