公开(公告)号：US07807430B2

公开(公告)日：2010-10-05

申请号：US12074543

申请日：2008-03-03

申请人： Stephen D Harrison ,  John A Hall ,  Maria Calderon-Cacia ,  Ziyang Zhong ,  Eric Y Fang ,  Doris G Coit ,  Steve H Nguyen ,  Angelica Medina-Selby

发明人： Stephen D Harrison ,  John A Hall ,  Maria Calderon-Cacia ,  Ziyang Zhong ,  Eric Y Fang ,  Doris G Coit ,  Steve H Nguyen ,  Angelica Medina-Selby

IPC分类号： C12N9/12 ,  C07K14/00 ,  C12P21/00 ,  C12N1/21 ,  C12N15/00 ,  C12N5/10 ,  C12Q1/48 ,  C07H21/00

CPC分类号： C12N9/1205 ,  C12Q1/485 ,  C12Y207/01037 ,  G01N2500/00

摘要： The invention provides truncated GSK3 polypeptides capable of crystallization, including GSK3α and GSK3β polypeptides, and use of these polypeptides to identify and optimize GSK3 inhibitors. Also provided are GSK3 polypeptides having at least one substituted amino acid that differs from wild-type GSK3, wherein the substituted amino acid is incapable of being phosphorylated. The invention finds use in providing methods of identifying and optimizing compounds useful for treating diseases mediated by GSK3 activity, including Alzheimer's disease, type 2 diabetes, and inflammation.

摘要翻译： 本发明提供能够结晶的截短的GSK3多肽，包括GSK3α和GSK3＆bgr; 多肽，以及使用这些多肽来鉴定和优化GSK3抑制剂。 还提供了具有与野生型GSK3不同的至少一个取代的氨基酸的GSK3多肽，其中取代的氨基酸不能被磷酸化。 本发明用于提供鉴定和优化用于治疗由GSK3活性介导的疾病（包括阿尔茨海默病，2型糖尿病和炎症）的化合物的方法。

公开(公告)号：US07195886B2

公开(公告)日：2007-03-27

申请号：US10733816

申请日：2003-12-10

申请人： Stephen D Harrison ,  John A Hall ,  Maria Calderon-Cacia ,  Ziyang Zhong ,  Eric Y Fang ,  Doris G Coit ,  Steve H Nguyen ,  Angelica Medina-Selby

发明人： Stephen D Harrison ,  John A Hall ,  Maria Calderon-Cacia ,  Ziyang Zhong ,  Eric Y Fang ,  Doris G Coit ,  Steve H Nguyen ,  Angelica Medina-Selby

IPC分类号： C12Q1/48 ,  G01N33/53 ,  G01N33/00 ,  G01N33/563 ,  C12P21/06 ,  C12P21/08 ,  C12N9/12 ,  C12N5/02 ,  C12N5/06 ,  C12N15/00 ,  C07K14/00

CPC分类号： C12N9/1205 ,  C12Q1/485 ,  C12Y207/01037 ,  G01N2500/00

摘要： The invention provides truncated GSK3 polypeptides capable of crystallization, including GSK3α and GSK3β polypeptides, and use of these polypeptides to identify and optimize GSK3 inhibitors. Also provided are GSK3 polypeptides having at least one substituted amino acid that differs from wild-type GSK3, wherein the substituted amino acid is incapable of being phosphorylated. The invention finds use in providing methods of identifying and optimizing compounds useful for treating diseases mediated by GSK3 activity, including Alzheimer's disease, type 2 diabetes, and inflammation.

公开(公告)号：US07135321B2

公开(公告)日：2006-11-14

申请号：US10689461

申请日：2003-10-20

申请人： Stephen D Harrison ,  John A Hall ,  Maria Calderon-Cacia ,  Ziyang Zhong ,  Eric Y Fang ,  Doris G Coit ,  Steve H Nguyen ,  Angelica Medina-Selby

发明人： Stephen D Harrison ,  John A Hall ,  Maria Calderon-Cacia ,  Ziyang Zhong ,  Eric Y Fang ,  Doris G Coit ,  Steve H Nguyen ,  Angelica Medina-Selby

IPC分类号： C12N9/12 ,  C12Q1/48 ,  C12P21/06 ,  C12N15/54 ,  C12N15/70 ,  C12N5/00 ,  C12N1/00 ,  C07H21/04

CPC分类号： C12N9/1205 ,  C12Q1/485 ,  C12Y207/01037 ,  G01N2500/00

摘要： The invention provides truncated GSK3 polypeptides capable of crystallization, including GSK3α and GSK3β polypeptides, and use of these polypeptides to identify and optimize GSK3 inhibitors. Also provided are GSK3 polypeptides having at least one substituted amino acid that differs from wild-type GSK3, wherein the substituted amino acid is incapable of being phosphorylated. The invention finds use in providing methods of identifying and optimizing compounds useful for treating diseases mediated by GSK3 activity, including Alzheimer's disease, type 2 diabetes, and inflammation.