公开(公告)号：US08877893B2

公开(公告)日：2014-11-04

申请号：US12645958

申请日：2009-12-23

申请人： Timothy A. Springer ,  Bing Hao Luo

发明人： Timothy A. Springer ,  Bing Hao Luo

IPC分类号： C07K14/00 ,  G01N33/566 ,  C07K14/705

CPC分类号： G01N33/5032 ,  C07K14/70546 ,  G01N33/566 ,  G01N33/6872 ,  G01N2333/70546 ,  G01N2333/70557 ,  G01N2500/04

摘要： The methods and compositions described herein are based, in part, on the discovery that the introduction of a disulfide bond into an integrin polypeptide by the substitution of at least one cysteine residue in the polypeptide permits stabilization of the integrin in a “closed/inactive” state. This stabilizing disulfide bond permits integrins to be screened for a candidate molecule that can bind to the closed state. In particular, this approach can be used to screen for agents that bind to the closed state of an integrin polypeptide, and are useful as therapeutic treatments to prevent integrin activation.

摘要翻译： 本文描述的方法和组合物部分地基于以下发现：通过取代多肽中的至少一个半胱氨酸残基将二硫键引入整联蛋白多肽，使整联蛋白稳定在“闭合/不活动” 州。 这种稳定的二硫键允许整合素筛选可以结合到封闭状态的候选分子。 特别地，该方法可用于筛选结合整联蛋白多肽的闭合状态的试剂，并且可用作防止整联蛋白活化的治疗性处理。

公开(公告)号：US20100167418A1

公开(公告)日：2010-07-01

申请号：US12645958

申请日：2009-12-23

申请人： Timothy A. Springer ,  Bing Hao Luo

发明人： Timothy A. Springer ,  Bing Hao Luo

IPC分类号： G01N33/53 ,  C07K14/00

CPC分类号： G01N33/5032 ,  C07K14/70546 ,  G01N33/566 ,  G01N33/6872 ,  G01N2333/70546 ,  G01N2333/70557 ,  G01N2500/04

摘要： The methods and compositions described herein are based, in part, on the discovery that the introduction of a disulfide bond into an integrin polypeptide by the substitution of at least one cysteine residue in the polypeptide permits stabilization of the integrin in a “closed/inactive” state. This stabilizing disulfide bond permits integrins to be screened for a candidate molecule that can bind to the closed state. In particular, this approach can be used to screen for agents that bind to the closed state of an integrin polypeptide, and are useful as therapeutic treatments to prevent integrin activation.

摘要翻译： 本文描述的方法和组合物部分地基于以下发现：通过取代多肽中的至少一个半胱氨酸残基将二硫键引入整联蛋白多肽，可使整联蛋白稳定在“闭合/不活动” 州。 这种稳定的二硫键允许整合素筛选可以结合到封闭状态的候选分子。 特别地，该方法可用于筛选结合整联蛋白多肽的闭合状态的试剂，并且可用作防止整联蛋白活化的治疗性处理。