公开(公告)号：US20060094081A1

公开(公告)日：2006-05-04

申请号：US11255147

申请日：2005-10-20

Applicant: Carsten Schubert ,  Barry Springer ,  Ingrid Deckman ,  Raymond Patch ,  Geoffrey Struble ,  Hongchang Ma ,  Celine Schalk-Hihi ,  Benjamin Brandt ,  Ioanna Petrounia

Inventor： Carsten Schubert ,  Barry Springer ,  Ingrid Deckman ,  Raymond Patch ,  Geoffrey Struble ,  Hongchang Ma ,  Celine Schalk-Hihi ,  Benjamin Brandt ,  Ioanna Petrounia

IPC: G06F19/00 ,  C07H21/04 ,  C12P21/06 ,  C12N9/12

CPC classification number: C07K14/7153 ,  C07K2299/00 ,  C07K2319/00 ,  C30B7/00 ,  G16B15/00 ,  G16B20/00 ,  G16B50/00

Abstract: The present invention includes a crystal structure of the kinase domain of c-fms and a methodology to produce diffraction quality crystals of the c-fms kinase domain by heterologous substitution of the kinase insert domain. Also included in the invention is the structure of the c-fms kinase domain in liganded form for use in the discovery of inhibitors of c-fms for the treatment of diseases caused by inappropriate activity of c-fms. The present invention includes descriptions of the X-ray diffraction patterns of the crystals. The diffraction patterns allow the three dimensional structure of c-fms to be determined at atomic resolution so that ligand binding sites on can be identified and the interactions of ligands with amino acid residues can be modeled.

Abstract translation: 本发明包括c-fms的激酶结构域的晶体结构和通过激酶插入结构域的异源取代产生c-fms激酶结构域的衍射质量晶体的方法。 本发明还包括配体形式的c-fms激酶结构域用于发现c-fms抑制剂用于治疗由c-fms的不适当活性引起的疾病的结构。 本发明包括晶体的X射线衍射图案的描述。 衍射图允许以原子分辨率确定c-fms的三维结构，从而可以鉴定配体结合位点，并且可以建模与配体与氨基酸残基的相互作用。