公开(公告)号：US20080021082A1

公开(公告)日：2008-01-24

申请号：US11580001

申请日：2006-10-11

申请人： R. Guy ,  Irwin Kuntz ,  Jose Haresco ,  Naoaki Fujii ,  Kathleen Novak ,  David Stokoe ,  Biao He ,  Liang You ,  Zhidong Xu ,  David Jablons

发明人： R. Guy ,  Irwin Kuntz ,  Jose Haresco ,  Naoaki Fujii ,  Kathleen Novak ,  David Stokoe ,  Biao He ,  Liang You ,  Zhidong Xu ,  David Jablons

IPC分类号： A61K31/405 ,  A61K31/4184 ,  C07D209/18 ,  C07D235/04 ,  C07D403/02 ,  C07K14/47 ,  C12N5/06 ,  C12N5/08

CPC分类号： C07D209/12 ,  C07D209/18

摘要： Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and interactions between the PDZ domain in the Dishevelled (Dvl) protein and other proteins such as the Frizzled (Fz) protein, have the general formula The invention also includes combinatorial libraries, arrays and methods for screening and studying proteins using such compounds. Compounds of the invention have produced apoptosis in certain cell lines that overexpress the Dishevelled protein (Dvl); inhibiting Wnt signaling.

摘要翻译： 已经发现已经发现有效抑制PDZ结构域相互作用的新型化合物，特别是MAGI中PDZ结构域与致癌（肿瘤抑制基因）蛋白PTEN的相互作用以及Dishedvelled（Dvl）蛋白质中的PDZ结构域和其它蛋白质之间的相互作用 （Fz）蛋白，具有通式本发明还包括用于筛选和研究使用这些化合物的蛋白质的组合文库，阵列和方法。 本发明化合物在过表达蛋白质（Dv1）的某些细胞系中产生凋亡; 抑制Wnt信号。

公开(公告)号：US20050043385A1

公开(公告)日：2005-02-24

申请号：US10826175

申请日：2004-04-15

申请人： R. Guy ,  Irwin Kuntz ,  Jose Haresco ,  Naoaki Fujii ,  Kathleen Novak ,  David Stokoe ,  Biao He ,  Liang You ,  Zhidong Xu ,  David Jablons

发明人： R. Guy ,  Irwin Kuntz ,  Jose Haresco ,  Naoaki Fujii ,  Kathleen Novak ,  David Stokoe ,  Biao He ,  Liang You ,  Zhidong Xu ,  David Jablons

IPC分类号： A61K31/405 ,  A61K31/4184 ,  C07D209/18 ,  C07D235/04 ,  C07D403/02 ,  C12N20060101

CPC分类号： C07D209/12 ,  C07D209/18

摘要： Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and interactions between the PDZ domain in the Dishevelled (Dvl) protein and other proteins such as the Frizzled (Fz) protein, have the general formula The invention also includes combinatorial libraries, arrays and methods for screening and studying proteins using such compounds. Compounds of the invention have produced apoptosis in certain cell lines that overexpress the Dishevelled protein (Dvl); inhibiting Wnt signaling.

摘要翻译： 已经发现已经发现有效抑制PDZ结构域相互作用的新型化合物，特别是MAGI中PDZ结构域与致癌（肿瘤抑制基因）蛋白PTEN的相互作用以及Dishedvelled（Dvl）蛋白质中的PDZ结构域和其它蛋白质之间的相互作用 （Fz）蛋白，具有通式本发明还包括用于筛选和研究使用这些化合物的蛋白质的组合文库，阵列和方法。 本发明化合物在过表达蛋白质（Dv1）的某些细胞系中产生凋亡; 抑制Wnt信号。

公开(公告)号：US07601750B2

公开(公告)日：2009-10-13

申请号：US11580001

申请日：2006-10-11

申请人： R. Kiplin Guy ,  Irwin D. Kuntz ,  Jose Haresco ,  Naoaki Fujii ,  Kathleen P. Novak ,  David Stokoe ,  Biao He ,  Liang You ,  Zhidong Xu ,  David M. Jablons

发明人： R. Kiplin Guy ,  Irwin D. Kuntz ,  Jose Haresco ,  Naoaki Fujii ,  Kathleen P. Novak ,  David Stokoe ,  Biao He ,  Liang You ,  Zhidong Xu ,  David M. Jablons

IPC分类号： A61K31/404 ,  C07D209/04

CPC分类号： C07D209/12 ,  C07D209/18

摘要： Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and interactions between the PDZ domain in the Dishevelled (Dvl) protein and other proteins such as the Frizzled (Fz) protein, have the general formula The invention also includes combinatorial libraries, arrays and methods for screening and studying proteins using such compounds.Compounds of the invention have produced apoptosis in certain cell lines that overexpress the Dishevelled protein (Dvl); inhibiting Wnt signaling.

摘要翻译： 已经发现已经发现有效抑制PDZ结构域相互作用的新型化合物，特别是MAGI中PDZ结构域与致癌（肿瘤抑制基因）蛋白PTEN的相互作用以及Dishedvelled（Dvl）蛋白质中的PDZ结构域和其它蛋白质之间的相互作用 （Fz）蛋白，具有通式本发明还包括用于筛选和研究使用这些化合物的蛋白质的组合文库，阵列和方法。 本发明化合物在过表达蛋白质（Dv1）的某些细胞系中产生凋亡; 抑制Wnt信号。

公开(公告)号：US07141600B2

公开(公告)日：2006-11-28

申请号：US10826175

申请日：2004-04-15

申请人： R. Kiplin Guy ,  Irwin D. Kuntz ,  Jose Haresco ,  Naoaki Fujii ,  Kathleen P. Novak ,  David Stokoe ,  Biao He ,  Liang You ,  Zhidong Xu ,  David M. Jablons

发明人： R. Kiplin Guy ,  Irwin D. Kuntz ,  Jose Haresco ,  Naoaki Fujii ,  Kathleen P. Novak ,  David Stokoe ,  Biao He ,  Liang You ,  Zhidong Xu ,  David M. Jablons

IPC分类号： A61K31/404 ,  C07D209/12 ,  C07D209/30 ,  C07D209/04

CPC分类号： C07D209/12 ,  C07D209/18

摘要： Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and interactions between the PDZ domain in the Dishevelled (Dvl) protein and other proteins such as the Frizzled (Fz) protein, have the general formula The invention also includes combinatorial libraries, arrays and methods for screening and studying proteins using such compounds.Compounds of the invention have produced apoptosis in certain cell lines that overexpress the Dishevelled protein (Dvl); inhibiting Wnt signaling.

公开(公告)号：US06682920B1

公开(公告)日：2004-01-27

申请号：US09156793

申请日：1998-09-17

申请人： Len Stephens ,  Philip Hawkins ,  David Stokoe

发明人： Len Stephens ,  Philip Hawkins ,  David Stokoe

IPC分类号： C12N912

CPC分类号： C12N9/1205

摘要： Compositions and methods are described that are useful to assay for compouds that affect PKB kinase activity which have medical applications for the diagnosis and treatment of disease.

摘要翻译： 描述了可用于测定影响PKB激酶活性的化合物的组合物和方法，其具有用于诊断和治疗疾病的医学应用。