CO-CRYSTAL STRUCTURES OF LIPID KINASES WITH SMALL MOLECULE INHIBITORS

脂质激酶与小分子抑制剂的共晶结构

• 批准号: 8362276
• 负责人: Chao Zhang
• 金额: $ 0.03万
• 依托单位: STANFORD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2011
• 资助国家: 美国
• 起止时间: 2011-03-01 至 2012-02-29
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8362276
• 关键词: Binding; Complex; Enzymes; Funding; Goals; Grant; Institution; Lipids; Malignant Neoplasms; National Center for Research Resources; Neoplasm Metastasis; Phosphotransferases; Principal Investigator; Process; Radiation; Research; Research Infrastructure; Resolution; Resources; Series; Source; Structure; Therapeutic Studies; United States National Institutes of Health; base; cost; human disease; inhibitor/antagonist; protein structure; scaffold; small molecule; structural biology; therapeutic target; tumorigenesis

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. Primary support for the subproject and the subproject's principal investigator may have been provided by other sources, including other NIH sources. The Total Cost listed for the subproject likely represents the estimated amount of Center infrastructure utilized by the subproject, not direct funding provided by the NCRR grant to the subproject or subproject staff. Our goal is to determine high resolution co-crystal structures of protein and lipid kinase therapeutic targets in complex with a series of inhibitors derived from our structure-based scaffold discovery platform. Our research relies heavily on the x-ray diffraction resources at institutions like SSRL in order to elucidate the molecular interactions of small molecule inhibitors in complex with kinase targets. These targets are important in diverse pathophysiological processes, such as tumorigenesis and metastasis. Targeting these enzymes with small molecule inhibitors enables the potential to treat human disease including cancers. For some kinase targets, we are not able to obtain co-crystals larger than 50 ?m which often leads to low-resolution diffraction with conventional x-ray sources. Therefore, access to a micro-focus beam line has the potential to be a valuable new resource for structure-based kinase therapy research.

这个子项目是利用这些资源的众多研究子项目之一