-
公开(公告)号：US08124392B2
公开(公告)日：2012-02-28
申请号：US12890826
申请日：2010-09-27
Applicant: Graham Cheetham , Ronald Knegtel , Lovorka Swenson , Joyce T. Coll , Suzanne Renwick , Peter Weber
Inventor： Graham Cheetham , Ronald Knegtel , Lovorka Swenson , Joyce T. Coll , Suzanne Renwick , Peter Weber
CPC classification number: C12N9/1205 , C07K2299/00
Abstract: The present invention provides crystalline molecules or molecular complexes which comprise binding pockets of Aurora-2 or its homologues. The invention also provides crystals comprising Aurora-2. The present invention also relates to a computer comprising a data storage medium encoded with the structural coordinates of Aurora-2 binding pockets and methods of using a computer to evaluate the ability of a compound to bind to the molecule or molecular complex. This invention also provides methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention provides methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to Aurora-2 or homologues thereof.
Abstract translation: 本发明提供包含Aurora-2或其同系物的结合口袋的结晶分子或分子复合物。 本发明还提供了包含Aurora-2的晶体。 本发明还涉及包含用Aurora-2结合口袋的结构座标编码的数据存储介质的计算机，以及使用计算机评价化合物结合分子或分子复合物的能力的方法。 本发明还提供了使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 此外，本发明提供了使用结构坐标筛选和设计结合Aurora-2或其同系物的化合物（包括抑制性化合物）的方法。
-
2.发明申请Inhibitors of GSK-3 and crystal structures of GSK-3beta protein and protein complexes 失效GSK-3的抑制剂和GSK-3β蛋白和蛋白质复合物的晶体结构公开(公告)号：US20080262205A1
公开(公告)日：2008-10-23
申请号：US12079917
申请日：2008-03-28
Applicant: Ernst ter Haar , Lovorka Swenson , Jeremy Green , Michael J. Arnost
Inventor： Ernst ter Haar , Lovorka Swenson , Jeremy Green , Michael J. Arnost
CPC classification number: C07D487/04 , C07K2299/00 , C12N9/1205 , G06F19/16
Abstract: The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.
Abstract translation: 本发明涉及GSK-3抑制剂及其制备方法。 本发明还提供包含抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病如糖尿病和阿尔茨海默氏病的方法。 此外，本发明涉及包含GSK-3β或其同源物的结合口袋的分子或分子复合物。 本发明涉及一种计算机，包括用这种结合口袋的结构坐标编码的数据存储介质。 本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 本发明涉及使用结构坐标来筛选和设计结合GSK-3β蛋白或其同系物的化合物的方法。 本发明还涉及可结晶组合物和包含GSK-3β蛋白或GSK-3β蛋白复合物的晶体。
-
公开(公告)号：US07809541B2
公开(公告)日：2010-10-05
申请号：US12070054
申请日：2008-02-13
Applicant: Graham Cheetham , Ronald Knegtel , Lovorka Swenson , Joyce T. Coll , Suzanne Renwick , Peter Weber
Inventor： Graham Cheetham , Ronald Knegtel , Lovorka Swenson , Joyce T. Coll , Suzanne Renwick , Peter Weber
CPC classification number: C12N9/1205 , C07K2299/00
Abstract: The present invention provides crystalline molecules or molecular complexes which comprise binding pockets of Aurora-2 or its homologues. The invention also provides crystals comprising Aurora-2. The present invention also relates to a computer comprising a data storage medium encoded with the structural coordinates of Aurora-2 binding pockets and methods of using a computer to evaluate the ability of a compound to bind to the molecule or molecular complex. This invention also provides methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention provides methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to Aurora-2 or homologues thereof.
Abstract translation: 本发明提供包含Aurora-2或其同系物的结合口袋的结晶分子或分子复合物。 本发明还提供了包含Aurora-2的晶体。 本发明还涉及包含用Aurora-2结合口袋的结构座标编码的数据存储介质的计算机，以及使用计算机评价化合物结合分子或分子复合物的能力的方法。 本发明还提供了使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 此外，本发明提供了使用结构坐标筛选和设计结合Aurora-2或其同系物的化合物（包括抑制性化合物）的方法。
-
4.发明授权Crystal structure of human Pim-1 kinase protein complexes and binding pockets thereof, and uses thereof in drug design 失效人类Pim-1激酶蛋白复合物及其结合口袋的晶体结构及其在药物设计中的应用公开(公告)号：US07666646B2
公开(公告)日：2010-02-23
申请号：US11242666
申请日：2005-10-04
Applicant: Marc Jacobs , Brian Hare , Lovorka Swenson
Inventor： Marc Jacobs , Brian Hare , Lovorka Swenson
IPC: C12N9/12
CPC classification number: G01N33/5748 , C07K2299/00 , C12N9/1205 , G01N33/573 , G01N33/6803 , G01N33/6842 , G01N2333/91205 , G01N2333/9121
Abstract: The present invention relates to the X-ray analysis of crystalline molecules or molecular complexes of human Pim-1. The present invention also relates to Pim-1-like binding pockets. The present invention provides a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to Pim-1 protein, Pim-1 protein complexes, or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising Pim-1 protein, Pim-1 protein complexes with adenosine, staurosporine or 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one and methods to produce these crystals.
Abstract translation: 本发明涉及人Pim-1的结晶分子或分子复合物的X射线分析。 本发明还涉及Pim-1样结合口袋。 本发明提供了一种计算机，其包括用这种结合口袋的结构坐标编码的数据存储介质。 本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 此外，本发明涉及使用结构坐标筛选和设计结合Pim-1蛋白，Pim-1蛋白复合物或其同系物的化合物（包括抑制性化合物）的方法。 本发明还涉及包含Pim-1蛋白，Pim-1蛋白复合物与腺苷，星形孢菌素或2-（4-吗啉基）-8-苯基-4H-1-苯并吡喃-4-酮的可结晶组合物和晶体以及产生 这些晶体。
-
公开(公告)号：US20090287422A1
公开(公告)日：2009-11-19
申请号：US12070054
申请日：2008-02-13
Applicant: Graham Cheetham , Ronald Knegtel , Lovorka Swenson , Joyce T. Coll , Suzanne Renwick , Peter Weber
Inventor： Graham Cheetham , Ronald Knegtel , Lovorka Swenson , Joyce T. Coll , Suzanne Renwick , Peter Weber
CPC classification number: C12N9/1205 , C07K2299/00
Abstract: The present invention provides crystalline molecules or molecular complexes which comprise binding pockets of Aurora-2 or its homologues. The invention also provides crystals comprising Aurora-2. The present invention also relates to a computer comprising a data storage medium encoded with the structural coordinates of Aurora-2 binding pockets and methods of using a computer to evaluate the ability of a compound to bind to the molecule or molecular complex. This invention also provides methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention provides methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to Aurora-2 or homologues thereof.
Abstract translation: 本发明提供包含Aurora-2或其同系物的结合口袋的结晶分子或分子复合物。 本发明还提供了包含Aurora-2的晶体。 本发明还涉及包含用Aurora-2结合口袋的结构座标编码的数据存储介质的计算机，以及使用计算机评价化合物结合分子或分子复合物的能力的方法。 本发明还提供了使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 此外，本发明提供了使用结构坐标筛选和设计结合Aurora-2或其同系物的化合物（包括抑制性化合物）的方法。
-
Patent Agency Ranking
6.发明授权Crystal structure of human JAK3 kinase domain complex and binding pockets thereof 失效人类JAK3激酶结构域复合物的晶体结构及其结合口袋公开(公告)号：US08712749B2
公开(公告)日：2014-04-29
申请号：US13479720
申请日：2012-05-24
Applicant: Harmon Zuccola , Marc Jacobs , Lovorka Swenson , Kumkum Saxena
Inventor： Harmon Zuccola , Marc Jacobs , Lovorka Swenson , Kumkum Saxena
CPC classification number: C12Q1/485 , C07K2299/00 , C12N9/1205 , G01N33/573 , G01N33/57496 , G01N33/6872 , G01N2500/00
Abstract: The present invention relates to human Janus Kinase 3 (JAK3) and JAK3-like binding pockets. The present invention provides a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to JAK3 protein or JAK3 protein homologues, or complexes thereof. The invention also relates to crystallizable compositions and crystals comprising JAK3 kinase domain and JAK3 kinase domain complexes with AMP-PNP.
Abstract translation: 本发明涉及人类Janus Kinase 3（JAK3）和JAK3样结合口袋。 本发明提供了一种计算机，其包括用这种结合口袋的结构坐标编码的数据存储介质。 本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 此外，本发明涉及使用结构坐标来筛选和设计结合JAK3蛋白或JAK3蛋白同源物的化合物（包括抑制性化合物）或其复合物的方法。 本发明还涉及包含具有AMP-PNP的JAK3激酶结构域和JAK3激酶结构域复合物的可结晶组合物和晶体。
-
7.发明申请CRYSTAL STRUCTURE OF HUMAN JAK3 KINASE DOMAIN COMPLEX AND BINDING POCKETS THEREOF 失效人类JAK3激酶复合体的结晶结构及其结合位点公开(公告)号：US20130137125A1
公开(公告)日：2013-05-30
申请号：US13479720
申请日：2012-05-24
Applicant: Harmon Zuccola , Marc Jacobs , Lovorka Swenson , Kumkum Saxena
Inventor： Harmon Zuccola , Marc Jacobs , Lovorka Swenson , Kumkum Saxena
IPC: C12Q1/48
CPC classification number: C12Q1/485 , C07K2299/00 , C12N9/1205 , G01N33/573 , G01N33/57496 , G01N33/6872 , G01N2500/00
Abstract: The present invention relates to human Janus Kinase 3 (JAK3) and JAK3-like binding pockets. The present invention provides a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to JAK3 protein or JAK3 protein homologues, or complexes thereof. The invention also relates to crystallizable compositions and crystals comprising JAK3 kinase domain and JAK3 kinase domain complexes with AMP-PNP.
Abstract translation: 本发明涉及人类Janus Kinase 3（JAK3）和JAK3样结合口袋。 本发明提供了一种计算机，其包括用这种结合口袋的结构坐标编码的数据存储介质。 本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 此外，本发明涉及使用结构坐标来筛选和设计结合JAK3蛋白或JAK3蛋白同源物的化合物（包括抑制性化合物）或其复合物的方法。 本发明还涉及包含具有AMP-PNP的JAK3激酶结构域和JAK3激酶结构域复合物的可结晶组合物和晶体。
-
8.发明授权Crystal structure of human JAK3 kinase domain complex and binding pockets thereof 失效人类JAK3激酶结构域复合物的晶体结构及其结合口袋公开(公告)号：US08192972B2
公开(公告)日：2012-06-05
申请号：US12471896
申请日：2009-05-26
Applicant: Harmon Zuccola , Marc Jacobs , Lovorka Swenson , Kumkum Saxena
Inventor： Harmon Zuccola , Marc Jacobs , Lovorka Swenson , Kumkum Saxena
CPC classification number: C12Q1/485 , C07K2299/00 , C12N9/1205 , G01N33/573 , G01N33/57496 , G01N33/6872 , G01N2500/00
Abstract: The present invention relates to human Janus Kinase 3 (JAK3) and JAK3-like binding pockets. The present invention provides a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to JAK3 protein or JAK3 protein homologues, or complexes thereof. The invention also relates to crystallizable compositions and crystals comprising JAK3 kinase domain and JAK3 kinase domain complexed with AMP-PNP.
Abstract translation: 本发明涉及人类Janus Kinase 3（JAK3）和JAK3样结合口袋。 本发明提供了一种计算机，其包括用这种结合口袋的结构坐标编码的数据存储介质。 本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 此外，本发明涉及使用结构坐标来筛选和设计结合JAK3蛋白或JAK3蛋白同源物的化合物（包括抑制性化合物）或其复合物的方法。 本发明还涉及可结晶组合物和包含与AMP-PNP复合的JAK3激酶结构域和JAK3激酶结构域的晶体。
-
9.发明申请Crystal structure of human PIM-1 kinase protein complexes and binding pockets thereof, and uses thereof in drug design 失效人类PIM-1激酶蛋白复合物及其结合口袋的晶体结构及其在药物设计中的应用公开(公告)号：US20070031956A1
公开(公告)日：2007-02-08
申请号：US11242666
申请日：2005-10-04
Applicant: Marc Jacobs , Brian Hare , Lovorka Swenson
Inventor： Marc Jacobs , Brian Hare , Lovorka Swenson
CPC classification number: G01N33/5748 , C07K2299/00 , C12N9/1205 , G01N33/573 , G01N33/6803 , G01N33/6842 , G01N2333/91205 , G01N2333/9121
Abstract: The present invention relates to the X-ray analysis of crystalline molecules or molecular complexes of human Pim-1. The present invention also relates to Pim-1-like binding pockets. The present invention provides a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to Pim-1 protein, Pim-1 protein complexes, or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising Pim-1 protein, Pim-1 protein complexes with adenosine, staurosporine or 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one and methods to produce these crystals.
Abstract translation: 本发明涉及人Pim-1的结晶分子或分子复合物的X射线分析。 本发明还涉及Pim-1样结合口袋。 本发明提供了一种计算机，其包括用这种结合口袋的结构坐标编码的数据存储介质。 本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 此外，本发明涉及使用结构坐标筛选和设计结合Pim-1蛋白，Pim-1蛋白复合物或其同系物的化合物（包括抑制性化合物）的方法。 本发明还涉及包含Pim-1蛋白，Pim-1蛋白复合物与腺苷，星形孢菌素或2-（4-吗啉基）-8-苯基-4H-1-苯并吡喃-4-酮的可结晶组合物和晶体以及产生 这些晶体。
-
公开(公告)号：US20060030018A1
公开(公告)日：2006-02-09
申请号：US11114979
申请日：2005-04-26
Applicant: Harmon Zuccola , Marc Jacobs , Lovorka Swenson , Kumkum Saxena
Inventor： Harmon Zuccola , Marc Jacobs , Lovorka Swenson , Kumkum Saxena
CPC classification number: C12Q1/485 , C07K2299/00 , C12N9/1205 , G01N33/573 , G01N33/57496 , G01N33/6872 , G01N2500/00
Abstract: The present invention relates to human Janus Kinase 3 (JAK3) and JAK3-like binding pockets. The present invention provides a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to JAK3 protein or JAK3 protein homologues, or complexes thereof. The invention also relates to crystallizable compositions and crystals comprising JAK3 kinase domain and JAK3 kinase domain complexed with AMP-PNP.
-
-
-
-
-
-
-
-
-
Search Results
22
records
(took 0.05 seconds)
