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.

高通量筛选和化学核心设施的目标是协助莫菲特研究人员 识别和优化有可能使双方受益的化学探针和新的先导化合物 生化机制研究以及药物发现和开发，最终将提供治疗 造福于癌症患者。 核心由三个功能单元组成： 1) 实验性高通量筛选（HTS） 2) 虚拟高温超导和分子建模 3) 化学中间体及文库合成 这三个单位紧密合作，为筛选生物分子提供互补的方法 目标并通过作为分子建模资源来帮助先导化合物优化过程 研究和初步先导优化。莫菲特的高通量筛选和分子建模工作 已经获得了对于获得 NCI R01 资金以及同行评审至关重要的初步数据 Akt 和 STATS 抑制剂的出版物。此外，莫菲特的 HTS 工作还确定了 抑制癌细胞中其他分子靶点的化学探针，例如极光激酶、SHP2 磷酸酶、蛋白酶体、香叶基香叶基转移酶 I 以及 mdm2/p53、BclXL/Bax 和 Rb/Raf-1 绑定。