High Throughput Biology Core

高通量生物核心摘要 高吞吐量生物核心将为项目团队提供基于目标和表型的高吞吐量 筛选(HTS)活动，以确定各种易处理的化学物质和SAR(结构-活性 )-启用主要剂量-反应分析，用于铅的识别和优化工作。这将是 与病毒学核心密切合作(提供分子靶点假说并开发BSL2 适用于可翻译的体外表型分析系统的载体)和药物发现核心(帮助 为迭代HTS设计量身定制的筛查设备，并提供药物化学支持以实现铅 识别和优化)。高通量生物学核心，拥有成熟的内部专业知识 测试开发和小型化，精通各种重组蛋白表达系统， 复合和数据管理系统，以及最先进的筛选和自动化基础设施 包括BSL2 HTS功能，将使HTS能够识别药物发现的新化学起点，并 还要验证新目标。此外，高通量生物核心还将使药物化学成为可能 努力改善靶向效力和增强选择性，具有强大的支持SAR的初级剂量-反应 化验。这将有助于优化具有改进的物理化学性质的候选铅 期望的效力、选择性和ADME特性，最终提供安全有效的有前景的临床 候选人。总而言之，高通量生物学核心将使UNAPP的药物发现工作成为可能 通过帮助项目团队确定验证新目标所需的易处理的各种化学物质 并支持抗病毒药物的发现，最终选择最适合开发的候选药物。

HIGH-THROUGHPUT BIOLOGY CORE – ABSTRACT The High-Throughput Biology Core will support Project Teams with target-based and phenotypic high-throughput screening (HTS) campaigns to identify diverse tractable chemical matter and SAR (structure-activity relationship)-enabling primary dose-response assays for lead identification and optimization efforts. This will be achieved in close collaboration with the Virology Core (providing molecular target hypothesis and develop BSL2 suitable vectors for translatable in vitro phenotypic assay systems) and the Drug Discovery Core (helping to design tailored screening sets for iterative HTS and providing medicinal chemistry support to enable lead identification and optimization). The High-Throughput Biology Core, with established in-house expertise in assay development and miniaturization, proficiency in diverse recombinant protein expression systems, compound and data management systems, and state-of-the-art screening and automation infrastructure including BSL2 HTS capability, will enable HTS to identify new chemical starting points for drug discovery and also validate new targets. Further, the High-Throughput Biology Core will also enable medicinal chemistry efforts to improve on-target potency and enhance selectivity with robust SAR-enabling primary dose-response assays. This will facilitate the optimization of lead candidates with improved physiochemical properties having desirable potency, selectivity and ADME properties to ultimately deliver safe and efficacious promising clinical candidates. In summary, the High-Throughput Biology Core will enable UNAPP’s drug discovery efforts by helping Project Teams to identify tractable diverse chemical matter necessary to validate new targets and support antiviral drug discovery to ultimately select the best candidate for development.