肽修饰
螯合肽
What is Chelating Peptides?
Coupling peptides to metal chelators (例如. 刀塔, 使用, ETC。) offers an attractive avenue for cancer tissue imaging or therapies that transport oncotoxins to cancer cells. The interleukin 13 signalling molecule alpha 2 (IL13RA2) is a signalling molecule that is overexpressed in most malignant gliomas (GBMs) but is absent in normal cells. Targeting ligands that bind such a signalling molecule may provide a new avenue for the treatment of malignant gliomas (GBMs). Because IL13RA2 is intrinsically bound to IL13, this signalling molecule is an attractive target in therapies that translocate cancer cytotoxic molecules to malignant glioma (GBMs) cells.Peptide-1 linear (Pep-1L) 已评估其以靶向方式结合 IL13RA2 的能力, 并通过螯合修饰, Peptide-1 线性 (Pep-1L) 可以转运细胞毒素 Actinium-225, Ac-225, 恶性胶质瘤 (GBMs) 细胞.
螯合肽服务
常用列表
癌细胞表达或过度表达特定信号分子导致了可以靶向这些信号分子的肽合成的发展, 和 MOL Changes 提供广泛的肽螯合剂修饰, 包括DOTA和DTPA.
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删节
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姓名
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|---|---|
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刀塔 |
1,4,7,10-四氮杂环十二烷-N,氮,氮,N-四乙酸 |
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使用 |
1,4,7-三氮杂环壬烷-N,氮,N-三乙酸 |
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阿姨 |
1,4,8,11-四氮杂环十四烷-1,4,8,11-四乙酸 |
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DTPA |
二乙烯三胺五乙酸 |
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国际开发协会 |
亚氨基二乙酸 |
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CB-TE2A |
4,11-之二(carboxymethyl)-1,4,8,11-tetraazabicyclo[6.6.2]hexadecane |
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DiAmSar |
1,8-二氨基-3,6,10,13,16,19-六氮杂双环[6,6,6]-eicosane |
精选引文
New Insights in the Design of Bioactive Peptides and Chelating Agents for Imaging and Therapy in Oncology
Many synthetic peptides have been developed for diagnosis and therapy of human cancers based on their ability to target specific receptors on cancer cell surface or to penetrate the cell membrane. Chemical modifications of amino acid chains have significantly improved the biological activity, the stability and efficacy of peptide analogues currently employed as anticancer drugs or as molecular imaging tracers. The stability of somatostatin, integrins and bombesin analogues in the human body have been significantly increased by cyclization and/or insertion of non-natural amino acids in the peptide sequences. 而且, the overall pharmacokinetic properties of such analogues and others (including cholecystokinin, 血管活性肠肽和神经降压素类似物) 通过聚乙二醇化和糖基化得到改善. 此外, 这些肽类似物与新接头和双功能螯合剂的缀合 (比如AAZTA, 阿姨, 陷阱, 号码等), 产生的放射性标记部分具有更长的半衰期和更高的同源受体结合亲和力. 这篇综述描述了氨基酸序列中引入的最重要和最新的化学修饰以及接头和新的双功能螯合剂，这些修饰显着提高了用于肿瘤诊断和治疗的肽的特异性和敏感性.
肽修饰
丰富的多肽修饰经验, 为肽研究提供多种可行的途径.
