Small Molecule Drug Development Shared Resource

小分子药物开发共享资源

• 批准号: 9904149
• 负责人: Drew James Adams
• 金额: $ 7.78万
• 依托单位: CASE WESTERN RESERVE UNIVERSITY
• 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/9904149
• 关键词: Accounting; Address; Applications Grants; Automation; Biological Assay; Biotechnology; Cancer Center Support Grant; Clinic; Comprehensive Cancer Center; Consultations; Data; Doctor of Philosophy; Drug Utilization; Equipment; Extramural Activities; Future; Genetic; In Vitro; Infrastructure; Lead; Libraries; Link; Malignant Neoplasms; Manuscripts; Mission; Pathway interactions; Pharmaceutical Chemistry; Pharmacology; Proteomics; Research; Research Personnel; Resource Sharing; Scientist; Services; Therapeutic; Training; Universities; University Hospitals; Work; assay development; cheminformatics; cost; design; drug development; genome sciences; high throughput screening; in vivo; in vivo evaluation; innovation; instrument; interest; member; operation; professor; programs; screening; small molecule; small molecule libraries

SMALL MOLECULE DRUG DEVELOPMENT SHARED RESOURCES PROJECT SUMMARY/ABSTRACT The Small Molecule Drug Development Shared Resource (Drug Development SR) was established in September 2015 to address the lack of critical infrastructure enabling small molecule screening and the identification of small-molecule probes. The mission of the Drug Development SR is to enable investigators to optimize robust assays in 384-well format and to screen these assays across large chemical libraries to identify new small molecules that may be the starting point for innovative cancer therapeutics. In the first year, a wide range of investigators from Case Western Reserve University (CWRU), University Hospitals (UH), Cleveland Clinic (CC), a collaborator from Duke University, and a Cleveland biotech startup utilized the Drug Development SR, testifying to the large demand for small-molecule screening. Since its establishment, the Drug Development SR has worked with 17 investigators, approximately 65% of whom are Case CCC members, accounting for 79% of total usage, and representing 4 of the 7 Case CCC Programs. The Specific Aims of the Small Molecule Drug Development Shared Resource are to: 1. Provide assay development and high-throughput screening services, using both high-throughput and high- content approaches to screen libraries of known bioactive compounds (bioactives) and diverse screening libraries. 2. Share expertise to design and optimize robust high-throughput assays tailored to specific projects, by consultation between the PI, the Director, and the Managing Director to inform project design, execution, and troubleshooting. 3. Train new users, including PIs, research scientists, and trainees, in proper and safe operation of the SR's automation equipment at reasonable cost, and welcome/include their participation during assay development and execution. 4. Offer advice and guidance to advance hits to leads using cheminformatics and medicinal chemistry, by providing recommended strategies for prioritizing hits, and linking investigators with medicinal chemists. 5. Guide users toward SRs and potential collaborating investigators in Case CCC Programs with complementary capabilities relevant to drug development as projects evolve, including connections to researchers with expertise in proteomics, in vitro and in vivo pharmacology, and in vivo testing. Moving forward, the Drug Development SR aims to complete 3 or more full high-throughput screens per year and 6 or more pilot screens to maintain a pipeline of robust assays for future large-scale screens. Additionally, the facility will expand its equipment set to provide redundancy in several key instruments, and will expand its screening libraries to 100,000 small molecules to match typical screen sizes performed in other academic screening centers.

小分子药物开发共享资源 项目摘要/摘要 小分子药物开发共享资源（药物开发SR）是在 2015年9月解决缺乏关键基础设施，可以筛选小分子和 鉴定小分子探针。药物开发SR的任务是使研究人员能够 以384孔格式优化健壮的测定法，并在大型化学库中筛选这些测定 新的小分子可能是创新癌症治疗的起点。在第一年， Case Western Reserve University（CWRU），大学医院（UH），克利夫兰的调查人员范围 杜克大学的合作者和克利夫兰生物技术初创公司使用该药物的诊所（CC） 开发SR，证明了对小分子筛查的巨大需求。 自成立以来，药物开发SR与17位调查人员合作，约有65％ 他们是CACE CCC成员，占使用总使用量的79％，代表7个案例CCC中的4个 程序。小分子药物开发共享资源的具体目的是： 1。提供测定开发和高通量筛选服务，同时使用高通量和高通量 屏幕库的内容方法已知的生物活性化合物（生物活性剂）和多样的筛选 库。 2。共享专业知识，以设计和优化针对特定项目量身定制的强大高通量测定法 PI，董事和董事总经理之间的咨询，以告知项目设计，执行， 和故障排除。 3。培训新用户，包括PI，研究科学家和学员，适用于SR的正确操作 以合理的成本自动化设备，欢迎/包括他们在测定期间的参与 开发和执行。 4。提供建议和指导，以推动使用化学信息和药物化学的铅提升铅， 提供建议的策略来确定命中率，并将研究人员与药物化学家联系起来。 5。指导用户对SRS和潜在的合作调查人员，如果CCC计划与 随着项目的发展，与药物开发相关的互补功能，包括与 具有蛋白质组学，体外和体内药理学以及体内测试专业知识的研究人员。 向前迈进，药物开发SR旨在每年完成3个或更多完整的高通量屏幕 以及6个或更多的试点屏幕，以维护未来大规模屏幕的强大测定管道。此外， 该设施将扩大其设备设置，以提供几种关键仪器的冗余，并将扩展其 将库筛选到100,000个小分子，以匹配其他学术中执行的典型屏幕尺寸 筛选中心。