首页> 外国专利> CRYSTALS OF AN AURORA-A TPX2 COMPLEX, TPX2 BINDING SITE OF AURORA-A, AURORA-A LIGANDS AND THEIR USE

CRYSTALS OF AN AURORA-A TPX2 COMPLEX, TPX2 BINDING SITE OF AURORA-A, AURORA-A LIGANDS AND THEIR USE

机译:Aurora-A TPX2复合物的晶体,Aurora-A,Aurora-A配体的TPX2结合位点及其用途

摘要

The present invention relates to crystals of phosphorylated Aurora-A kinasefragment alone and in complex with a ligand, amino acid residues 1-43 of humanTPX2. This invention also relates to methods for designing and selectingligands, in particular allosteric inhibitors of Aurora-A, that bind to theAurora-A kinase and their use. Further, the present invention relates tocertain indene and indole derivatives.The present invention relates tocrystals of phosphorylated Aurora-A kinase alone and in complex with a ligand,amino acid residues 1-43 of human TPX2. This invention also relates to methodsfor designing and selecting ligands that bind to the Aurora-A kinase and theiruse. Further, the present invention relates to certain indene and indolederivative.
机译:本发明涉及磷酸化的Aurora-A激酶的晶体片段单独且与配体复合时,人的氨基酸残基1-43TPX2。本发明还涉及用于设计和选择的方法。与Aurora-A结合的配体,特别是Aurora-A的变构抑制剂Aurora-A激酶及其用途。此外,本发明涉及某些茚和吲哚衍生物。本发明涉及磷酸化的Aurora-A激酶的单独晶体以及与配体的复合晶体,人TPX2的氨基酸残基1-43。本发明还涉及方法用于设计和选择与Aurora-A激酶及其配体结合的配体采用。此外,本发明涉及某些茚和吲哚。衍生物。

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