SBIR Phase II: Development of Novel Dendrimer-based Technologies for Phosphorylation Analyses

这个小型企业创新研究（SBIR）第二阶段项目解决了对蛋白质磷酸化有效分析的未满足需求，这是一个将磷酸基团添加到蛋白质中以改变其功能的过程。蛋白质磷酸化是蛋白质的重要修饰，其异常与许多疾病有关。因此，定性或定量评估单个蛋白质或蛋白质类别的磷酸化状态已成为大多数生命科学研究实验室中常规但极其重要的步骤。现有技术存在重现性差、回收率低、成本高、选择性低、实验时间长等问题。在第二阶段项目期间开发的平台技术将通过提供有利可图的通用磷酸化分析方法来大大缓解这些缺点。这些技术将使一般的磷酸化检测，具有成本效益的癌症抑制剂筛选和激酶/磷酸酶活性定量用于新药发现。该项目更广泛的影响/商业潜力是开发平台技术，以改进一套生化测定，从而能够发现新的治疗靶点和药物。蛋白质磷酸化和激酶抑制剂作为药物靶点，目前处于研究和开发（R D）的高峰，占总药物发现费用的30%以上。这些研发活动可以大大受益于所提出的技术，由于其创新的设计和多功能的功能，以最佳的效率，并能够重现探索磷酸化事件在前所未有的深度。这些应该提供宝贵的工具，并解决许多生物科学研究实验室/设施在学术和工业环境的需求。

This Small Business Innovation Research (SBIR) Phase II project addresses the unmet needs for effective analysis of protein phosphorylation, a process where a phosphate group is added to a protein to change its function. Protein phosphorylation is a crucial modification of proteins; its abnormalities have been implicated in many diseases. Therefore, assessing the phosphorylation status of individual proteins or classes of proteins, qualitatively or quantitatively, has become a routine but extremely important step in the majority of life science research labs. Existing technologies have glaring deficiencies, including low reproducibility, poor recovery, high cost, reduced selectivity and prolonged experiment time. The platform technology to be developed during this Phase II project will greatly alleviate these shortcomings by providing lucrative, general approaches for phosphorylation analyses. The technologies will enable general phosphorylation detection, cost-effective cancer inhibitor screenings, and kinase/phosphatase activity quantitation for new drug discovery.The broader impact/commercial potential of this project is the development of platform technology to improve a set of biochemical assays, thus enabling the discovery of new therapeutic targets and drugs. Protein phosphorylation and kinase inhibitors as drug targets are currently at the peak of research and development (R&D), responsible for over 30% of the total drug discovery expenses. These R&D activities could greatly benefit from the proposed technologies due to their innovative design and versatile features for optimum efficiency, and the ability to reproducibly explore phosphorylation events in unprecedented depth. These should provide invaluable tools and address needs of many bioscience research labs/facilities in academic and industrial settings.