SMALL MOLECULES REGULATING PROTEIN-PROTEIN INTERACTIONS IN CANCER

调节癌症中蛋白质-蛋白质相互作用的小分子

• 批准号: 8362797
• 负责人: ARTHUR J. OLSON
• 金额: $ 3万
• 依托单位: UNIVERSITY OF CALIFORNIA, SAN DIEGO
• 依托单位国家: 美国
• 财政年份: 2011
• 资助国家: 美国
• 起止时间: 2011-05-01 至 2012-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8362797
• 关键词: 1-Phosphatidylinositol 3-Kinase; Affect; Area; Biomedical Computing; Characteristics; Chemicals; Collaborations; Funding; Goals; Grant; Malignant Neoplasms; National Center for Research Resources; Oncogenes; Pathway interactions; Principal Investigator; Regulation; Research; Research Infrastructure; Resources; Site; Source; Therapeutic; United States National Institutes of Health; cost; drug development; inhibitor/antagonist; programs; protein protein interaction; small molecule

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. (A) Objectives. Chemical modulation and inhibition of oncogene regulation and expression is a promising therapeutic approach to the treatment of many cancers. To advance this approach, our goal is the identification, optimization and characterization of small molecule inhibitors and stabilizers of protein-protein interactions affecting the Myc network and the PI 3-kinase (PI3K) pathway. Protein-protein interactions remain challenging targets for small molecules; progress in this area will open new opportunities for drug development. This collaboration will rely upon several advances in the AutoDock suite of programs that enable the discovery of drugable sites to modulate protein-protein interactions, and which factor in dynamic characteristics of these sites.

这个子项目是许多利用资源的研究子项目之一 由NIH/NCRR资助的中心拨款提供。子项目的主要支持 而子项目的主要调查员可能是由其他来源提供的， 包括其它NIH来源。 列出的子项目总成本可能 代表子项目使用的中心基础设施的估计数量， 而不是由NCRR赠款提供给子项目或子项目工作人员的直接资金。 (A)目标.癌基因调控和表达的化学调节和抑制是 一 这是一种治疗许多癌症的有前途的治疗方法。推进这一 方法， 我们的目标是鉴定、优化和表征小分子抑制剂 和 影响Myc网络和PI 3-激酶的蛋白质-蛋白质相互作用的稳定剂 （PI3K） 通路 蛋白质-蛋白质相互作用仍然是小分子的挑战性目标; 这一领域的进展将为药物开发带来新的机会。这项合作将 依赖于AutoDock程序套件中的几项进步，这些程序可以发现 药物位点调节蛋白质-蛋白质相互作用，并在动态因素 这些网站的特点。