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Polypeptides derived from vitamin D nuclear receptors and their use for screening for vitamin D analogues in particular

机译:衍生自维生素D核受体的多肽及其在筛选维生素D类似物中的用途

摘要

Polypeptides derived from vitamin D nuclear receptor, which nuclear receptor comprises a ligand-binding domain, or LBD, which contains a flexible insertion domain. The polypeptides are charactarised in that the LBD flexible insertion domain is modified by substituting or suppressing at least 30 acids. The invention also concerns the use of the polypeptides in particular for screening synthetic vitamin D analogues or for producing tests (double or triple hybrid) for identifying other proteins (activator, repressor, . . . ) interacting with the vitamin D receptor using constructs containing the polypeptide used with Gal4 for example, or for analyzing three dimensional structures of complexes formed between the polypeptides and a particular molecule by crystallography or NMR.
机译:衍生自维生素D核受体的多肽,该核受体包含配体结合结构域或LBD,其包含柔性插入结构域。所述多肽的特征在于,通过取代或抑制至少30个酸来修饰LBD柔性插入结构域。本发明还涉及所述多肽的用途,特别是用于筛选合成的维生素D类似物或用于产生测试(双重或三重杂交)以鉴定使用含有维生素D受体的构建物与所述维生素D受体相互作用的其他蛋白质(活化剂,阻遏物...)的用途。多肽与Gal4一起使用,或用于通过晶体学或NMR分析多肽与特定分子之间形成的复合物的三维结构。

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