Ultrahigh-throughput Identification of Molecular Targets of Natural Products

 说明(申请人提供)：天然产物是潜在药物的丰富来源。为了加速从天然产物中发现药物，必须确定它们的分子靶点，并从机械上阐明它们的生物利用度、毒性和治疗效果。然而，该领域仍然存在几个挑战。其中，目前还没有技术平台可以使用定量高通量筛查中通常遇到的少量样本或从生物和临床研究中获得的样本来进行从“Hits”到“Leads”的机械性研究。为了应对这些挑战，并响应RFA-AT-16-003，Neomeics Inc.建议完成其产品的开发，这是一个用于高通量和高含量天然产品生物分析的多重组学平台。第二阶段项目是建立在我们第一阶段项目产生的有希望的结果的基础上的。在第一阶段，我们开发了电喷雾质谱(ESI-MS)分析方法，从不同复杂性的文库中筛选分子靶标与天然产物之间的相互作用。在第二阶段，我们将通过与行业合作伙伴、学术合作者和商业顾问密切合作，完成用于商业化的多重组学分析的开发。一旦开发出来，Neomeics的Omics-芯片可能成为高通量鉴定血液或其他组织中天然产物分子靶标的通用平台，并为药物发现和开发奠定新的基础。

 DESCRIPTION (provided by applicant): Natural products are rich sources for potential drugs. To accelerate drug discovery from natural products, it is imperative to identify their molecular targets, and mechanistically elucidate their bioavailability, toxicity, and therapeutic effects. However, there remain several challenges in the field. Among them, there is currently no technical platform that could perform mechanistic studies from the "hits" to "leads" using the small volumes of samples that are typically encountered in quantitative high-throughput screening or obtained from biological and clinical studies. To tackle these challenges and in response to RFA-AT-16-003, Newomics Inc. proposes to complete development of its product, a multiomics platform for high-throughput and high-content bioassays of natural products. The Phase II project is built upon the promising results generated from our Phase I project. In Phase I, we have developed ESI-MS assays to screen the interactions between molecular targets and natural products from libraries with different complexity. In Phase II, we will complete development of multiomics assays for commercialization, through working closely with industry partners, academic collaborators, and business consultants. Once developed, Newomics' Omics-chip may become a universal platform for high-throughput identification of molecular targets of natural products in the blood or other tissues, and lay a new foundation for drug discovery and development.