2,2'-Bisindoles in Peptides and Protein Kinase Inhibitors

这个启动补助金奖给加州大学欧文分校将 支持大卫教授的研究。货车范兰肯。 的主题 研究是合成与研究相关的偶联吲哚 蛋白质结构和蛋白激酶抑制剂。 的特定 目的是从3-取代吲哚合成2，2 '-双吲哚 在一般的酸催化条件下，然后氧化。 双吲哚与小肽段的连接可以作为模型 用于以后对全尺寸蛋白质的研究。 这样的翻译后 修饰可以稳定二级结构并引入独特的 光谱手柄 另一个目标是将这种化学物质用于 蛋白激酶抑制剂的仿生合成。 这项研究将促进对 蛋白质的结构/功能关系。

This starter grant award to the University of California at Irvine will support the research of Professor David L. Van Vranken. The theme of the research is the synthesis of coupled indoles that are relevant to studies of protein structure and protein kinase inhibitors. The particular objective is the synthesis of 2,2'-bisindoles from 3-substituted indoles under conditions of general acid catalysis, followed by oxidation. Linkage of the bisindoles to small peptide segments may serve as a model for later studies in full-sized proteins. Such a posttranslational modification could stabilize secondary structure and introduce a unique spectroscopic handle. A further goal is to use this chemistry in a biomimetic synthesis of protein kinase inhibitors. This research will advance the fundamental understanding of the structure/function relationship in proteins.