High Throughput Screening

高通量筛选

• 批准号: 7516326
• 负责人: William Steven Dalton
• 金额: $ 12.84万
• 依托单位: H. LEE MOFFITT CANCER CTR & RES INST
• 依托单位国家: 美国
• 财政年份: 2007
• 资助国家: 美国
• 起止时间: 2007-02-01 至 2012-01-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7516326
• 关键词: Binding; Biochemical; Cancer Patient; Chemicals; Chemistry; Core Facility; Data; Development; Funding; Goals; Lead; Libraries; Molecular Target; Non-Receptor Type 11 Protein Tyrosine Phosphatase; Process; Publications; Research Personnel; Resources; Screening procedure; Therapeutic; Work; aurora kinase; cancer cell; drug discovery; high throughput screening; inhibitor/antagonist; molecular modeling; multicatalytic endopeptidase complex; protein geranylgeranyltransferase; virtual

The goal of the High Throughput Screening & Chemistry Core Facility is to assist Moffitt researchers in identifying and optimizing chemical probes and new lead compounds that have the potential to benefit both biochemical mechanistic studies and drug discovery & development, which will ultimately provide therapeutic benefit to cancer patients. The Core is comprised of three functional units: 1) Experimental High Throughput Screening (HTS) 2) Virtual HTS and Molecular Modeling 3) Chemical Intermediates and Library Synthesis The three units work closely together to provide complementary approaches toward screening biomolecular targets and toward aiding the lead optimization process by serving as a resource for molecular modeling studies and initial lead optimization. High throughput screening and molecular modeling efforts at Moffitt have already resulted in preliminary data that was essential for obtaining NCI R01 funding as well as peerreviewed publications for Akt and STATS inhibitors. Furthermore, HTS efforts at Moffitt have also identified chemical probes that inhibit other molecular targets in cancer cells such as Aurora kinase, SHP2 phosphatase, the proteasome, geranylgeranyltransferase I as well as mdm2/p53, BclXL/Bax and Rb/Raf-1 binding.

高吞吐量筛查和化学核心设施的目的是协助莫菲特研究人员 识别和优化化学探针和新铅化合物，这些化合物有可能受益 生化机械研究和药物发现与开发，最终将提供治疗 对癌症患者的好处。 核心由三个功能单元组成： 1）实验高通量筛查（HTS） 2）虚拟HTS和分子建模 3）化学中间体和库合成 这三个单元紧密合作，为筛查生物分子提供互补的方法 通过作为分子建模的资源来实现目标并朝着帮助铅优化过程 研究和初始铅优化。高吞吐量筛查和莫菲特的分子建模工作 已经产生了初步数据，这对于获得NCI R01资金以及同行评审至关重要 AKT和统计抑制剂的出版物。此外，莫菲特的HTS努力也确定了 化学探针抑制癌细胞中其他分子靶标的化学探针，例如Aurora激酶SHP2 磷酸酶，蛋白酶体，香烷基凝集苷转移酶I以及MDM2/p53，BCLXL/BAX和RB/RAF-1 结合。