Combinational Chemistry

组合化学

• 批准号: 8907682
• 负责人: Ralph W. deVere White
• 金额: $ 8.87万
• 依托单位: UNIVERSITY OF CALIFORNIA AT DAVIS
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/8907682
• 关键词: Area; Basic Science; Biological Assay; Cancer Center; Cancer Center Support Grant; Cell physiology; Chemicals; Chemistry; Collection; Development; Discipline; Extramural Activities; Funding; Glycopeptides; Grant; Lead; Libraries; Malignant Neoplasms; Methods; Microspheres; Organic Chemistry; Outcome; Peptide Library; Pharmaceutical Chemistry; Pharmaceutical Preparations; Process; Research; Research Personnel; Resource Sharing; Resources; Scientist; Source; Suggestion; Techniques; Technology; Therapeutic Agents; Training Support; Work; anticancer research; base; combinatorial; combinatorial chemistry; design; design and construction; drug discovery; imaging agent; investigator training; member; molecular imaging; molecular marker; peptidomimetics; ranpirnase; screening; small molecule; small molecule libraries; tool

Combinatorial library methods not only offer great potential for facilitating the drug discovery process but also provide powerful tools for basic research in various disciplines. These methods enable investigators to generate large number of chemical compounds that can be used as valuable source for the discovery of drug leads, molecular imaging agents, and capturing agents for molecular markers. In the area of basic research, large collections of chemical compounds can be used to probe their effects on specific cellular function. In the past 4 years, the combinatorial chemistry developing core has been assisting several Cancer Center investigators in the application of combinatorial chemistry to their research. These efforts have resulted in the submission and funding of several extramural grants. Based on the encouraging outcome and suggestion by our external advisory board, we plan to advance the combinatorial developing core to a full shared resource. The proposed combinatorial chemistry shared resource (CCSR7) will provide training and support for cancer center members to apply the ultra-high throughput one-bead-one-compound (OBOC) technologies for their research. Many OBOC combinatorial libraries (peptides, peptidomimetic, glycopeptides, small molecules, macrocyclic and glyco-organic libraries) will be designed and synthesized by the CCSR7 scientists. We have proposed to develop twenty-seven OBOC chemical libraries over the five year period. CCSR7 will also provide synthetic organic and medicinal chemistry expertise on working with the resource users for optimization of the lead compounds. CCSR7 will also provide synthetic organic and medicinal chemistry expertise on working with the resource users for optimization ofthe lead compounds.

组合图书馆的方法不仅为促进药物发现过程提供了巨大的潜力，而且为各种学科的基础研究提供了强大的工具。这些方法使研究人员能够生成大量的化合物，这些化合物可以用作发现药物铅，分子成像剂以及捕获分子标记的剂的宝贵来源。在基础研究领域，大量化合物可用于探测其对特定细胞功能的影响。在过去的四年中，开发核心的组合化学一直在协助几名癌症中心研究人员将组合化学应用于其研究。这些努力导致了几项壁外补助金的提交和资金。基于我们的外部咨询委员会的令人鼓舞的结果和建议，我们计划将发展核心的组合发展核心推向完整的共享资源。拟议的组合化学共享资源（CCSR7）将为癌症中心成员提供培训和支持，以应用超高吞吐量的一孔单孔（OBOC）技术进行研究。 CCSR7科学家将设计和合成许多oboc组合文库（肽，肽含量，糖肽，小分子，大分子，大分子和糖 - 有机库）。我们建议在五年内开发27个OBOC化学库。 CCSR7还将提供与资源使用者合作以优化铅化合物的合成有机和药物化学专业知识。 CCSR7还将提供与资源用户合作以优化铅化合物的合成有机和药物化学专业知识。