Invention Grant
US07666646B2 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
- Patent Title: Crystal structure of human Pim-1 kinase protein complexes and binding pockets thereof, and uses thereof in drug design
- Patent Title (中): 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
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Application No.: US11242666Application Date: 2005-10-04
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Publication No.: US07666646B2Publication Date: 2010-02-23
- Inventor: Marc Jacobs , Brian Hare , Lovorka Swenson
- Applicant: Marc Jacobs , Brian Hare , Lovorka Swenson
- Applicant Address: US MA Cambridge
- Assignee: Vertex Pharmaceuticals Incorporated
- Current Assignee: Vertex Pharmaceuticals Incorporated
- Current Assignee Address: US MA Cambridge
- Agency: Ropes & Gray, LLP
- Agent James F. Haley, Jr.; Raymond M. Doss
- Main IPC: C12N9/12
- IPC: C12N9/12
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.
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