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.

该副本是利用资源的众多研究子项目之一 由NIH/NCRR资助的中心赠款提供。对该子弹的主要支持 而且，副投影的主要研究员可能是其他来源提供的 包括其他NIH来源。 列出的总费用可能 代表subproject使用的中心基础架构的估计量， NCRR赠款不直接向子弹或副本人员提供的直接资金。 （a）目标。化学调节和对癌基因调节和表达的抑制是 一个 有前途的治疗方法来治疗许多癌症。推进这一点 方法， 我们的目标是小分子抑制剂的识别，优化和表征 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） 路径。 蛋白质 - 蛋白质相互作用仍然是小分子的挑战靶标。 该领域的进展将为药物开发开辟新的机会。这项合作将 依靠一系列计划中的几个进步，这些计划可以发现 可在调节蛋白质 - 蛋白质相互作用的可药物位点，哪个因素是动态的 这些站点的特征。