Chemical Library Screening

摘要-化学图书馆筛选共享资源 化学图书馆筛选（CLS）共享资源由癌症中心管理。该资源提供 中心科学家开发和进行小规模和大规模化学库筛选和执行的能力 用于产生调节生物化学和细胞的选择性探针/先导物的命中优化和验证 癌症的过程。此外，CLS还为教师提供技术，专业知识和基础设施 开发用于表征参与肿瘤起始和发病机制的细胞靶点的新型测定方法的资源 并促进用于抗肿瘤疗法的新先导分子的开发。CLS由四个专门的 但高度集成的设施：高通量检测开发（HT-AD），化合物管理和 高通量筛选（CM-HTS）、高含量筛选（HCS）和药物化学与药物 代谢/药代动力学（MedChem/DMPK）。这些设施实际上位于Conrad Prebys内 化学基因组学中心（Prebys中心）位于SBP，占地12，000多平方米。英尺实验室 空间和容纳大量的HTS和HCS分析开发和筛选仪器能力。 CLS拥有广泛的多样化和集中的小分子集合，几个集成的液体 处理系统和大量的检测仪器，能够以任何模式进行分析，包括 需要温度和CO2控制的基于活细胞图像的测定。Prebys中心从癌症中成长起来 中心的CLS共享资源，这是在2003年CCSG更新启动。这一支持得到了利用， 有几个大的补助金和慈善基金。最初获得资助，作为十个NIH分子之一 图书馆筛选网络综合中心，Prebys中心后来被选为四个NIH之一， 指定分子文库探针生产中心网络综合筛选中心。也是 NCI化学生物学联盟（CBC）的七个专门中心之一。尽管增长的 Prebys中心，CLS核心仍然是至关重要的中心研究人员，因为它提供了一个 重要的互动切入点，以确保他们从这些世界级的科学中获得最大的科学利益。 化学生物学和药物发现能力，使基础和转化科学 努力在过去的5年里，Core还为超过100个癌症检测开发项目提供了支持。 中心调查员，导致>25个完整的HTS活动，以支持早期翻译的目标。它提供 为代表所有三个项目的36名中心研究人员提供服务。所生成的数据支持24 16名中心成员和众多出版物的成功赠款，包括20篇合著的出版物 CLS员工

ABSTRACT – CHEMICAL LIBRARY SCREENING SHARED RESOURCE The Chemical Library Screening (CLS) Shared Resource is managed by the Cancer Center. This resource offers Center scientists the ability to develop and conduct small- and large-scale chemical library screens and perform hit optimization and validation for generating selective probes/leads modulating biochemical and cellular processes in cancer. In addition, CLS provides faculty with access to technology, expertise, and infrastructure resources to develop novel assays for characterizing cellular targets involved in tumor initiation and pathogenesis and to advance the development of new lead molecules for anti-tumor therapies. CLS consists of four specialized but highly integrated facilities: High-Throughput Assay Development (HT-AD), Compound Management and High-Throughput Screening (CM-HTS), High-Content Screening (HCS), and Medicinal Chemistry and Drug Metabolism/Pharmacokinetics (MedChem/DMPK). The facilities physically reside within the Conrad Prebys Center for Chemical Genomics (Prebys Center) at SBP, which occupies more than 12,000 sq. ft. of laboratory space and houses substantial HTS and HCS assay development and screening instrumentation capabilities. CLS has access to a broad spectrum of diverse and focused small-molecule collections, several integrated liquid handling systems, and a plethora of detection instruments, capable of performing assays in any mode, including live-cell image-based assays requiring temperature and CO2 control. The Prebys Center grew out of the Cancer Center's CLS Shared Resource, which was initiated in the 2003 CCSG renewal. This support has been leveraged with several large grant awards and philanthropic funds. Initially awarded a grant as one of ten NIH Molecular Libraries Screening Network Comprehensive Centers, the Prebys Center was later selected as one of four NIH- designated Molecular Libraries Probe Production Centers Network comprehensive screening centers. It is also one of seven dedicated Centers for the NCI Chemical Biology Consortium (CBC). Despite the growth of the Prebys Center, the CLS Core remains of crucial importance to Center investigators because it provides an important interactive entry point to ensure that they derive the maximum scientific benefit from these world class chemical biology and drug discovery capabilities, enabling both fundamental and translational scientific endeavors. In the past 5 years, the Core has additionally enabled >100 assay development projects for Cancer Center investigators, resulting in >25 full HTS campaigns to support the goal of early translation. It has provided services for 36 Center investigators representing all three programs. The data generated have supported 24 successful grants from 16 Center members and numerous publications, including 20 publications co-authored by CLS staff.