公开(公告)号：US5637759A

公开(公告)日：1997-06-10

申请号：US923226

申请日：1992-07-30

申请人： John E. Hearst ,  Tariq M. Rana ,  Matt Ban

发明人： John E. Hearst ,  Tariq M. Rana ,  Matt Ban

IPC分类号： A61K49/14 ,  C07C271/22 ,  C07C261/00

CPC分类号： A61K49/085 ,  A61K49/10 ,  A61K49/14 ,  C07C271/22 ,  C07C2103/18

摘要： Novel organic compounds and metal ion-containing amino acid chelates are described which are useful in solid phase synthesis of polypeptides and as magnetic resonance imaging (MRI) enhancing agents. The present invention also relates to a convenient and straightforward method to synthesize a metal-ligating amino acid suitable as MRI enhancing agents or for introducing a strong metal binding site at any chosen position in a peptide. Some compounds are designed to be compatible with N-.alpha.-Fmoc peptide synthesis strategy, and can easily be prepared on large scale. Thus, flexible linkers of different lengths and containing various structures can be placed between the .alpha.-carbon backbone of peptides and metal binding moieties. These peptides will provide a variety of affinity cleaving reagents which can be directed against protein or nucleic acid targets. Therefore, these molecules can serve as an important tool to study protein folding, protein-protein and protein-nucleic acid interactions.

摘要翻译： 描述了新的有机化合物和含金属离子的氨基酸螯合物，其可用于多相固相合成和磁共振成像（MRI）增强剂。 本发明还涉及合成适合作为MRI增强剂的金属结合氨基酸或在肽中任何选定位置引入强金属结合位点的方便且直接的方法。 一些化合物被设计为与N-α-Fmoc肽合成策略相容，并且可以容易地大规模制备。 因此，可以将不同长度和包含各种结构的柔性接头置于肽的α-碳骨架和金属结合部分之间。 这些肽将提供可针对蛋白质或核酸靶标的多种亲和力切割试剂。 因此，这些分子可以作为研究蛋白质折叠，蛋白质 - 蛋白质和蛋白质 - 核酸相互作用的重要工具。