LUMINESCENT ANTIVIRAL DRUG DISCOVERY ASSAY

描述（由申请人提供）：SBIR I期项目的目标是开发一个新药发现平台，用于筛选新的病毒聚合酶抑制剂和研究预期药物化合物的作用机制。该项目的主要创新是提出了多酶测定的概念，该方法能够在单一实验中使用广泛使用的商业仪器（光度计）以实时检测模式使用小反应体积测量效率并确定病毒聚合酶抑制剂的作用机制。所提出的平台是上级超过现有的方法，因为它大大降低了试剂的成本，减少了测定时间从几天到几分钟，并适用于高通量格式的应用在大规模和小规模的药物发现项目。拟议的SBIR项目是为了响应NIH对旨在降低成本和提高临床前药物开发速度的新方法的呼吁。 公共卫生相关性：抗病毒治疗是潜在救生产品开发的重要前沿。在世界范围内，每年有数百万人遭受病毒感染。全世界约有3.6亿人患有B型肝炎病毒，这是肝癌的主要原因。全世界有超过1.7亿人感染丙型肝炎，这是急性肝脏炎症和肝癌的主要原因。全世界有4 200多万人感染了危及生命的人体免疫缺陷病毒（艾滋病毒），其中包括300多万儿童。为了满足日益增长的医疗需求，开发中的抗病毒化合物的数量稳步增加。拟议的SBIR项目将创建一个知识库并建立一项新技术，从而降低开发药物抗病毒产品的成本和时间，并在美国和世界各地产生巨大的健康影响。

DESCRIPTION (provided by applicant): The goal of this SBIR Phase I project is the development of a new drug discovery platform for screening new inhibitors of viral polymerases and for studying mechanisms of action of the prospective pharmaceutical compounds. The main innovation in this project is the proposed concept of a multi-enzyme assay, which is able to measure efficiency and identify the mechanism of action of a viral polymerase inhibitor in a single experiment using a small reaction volume in realtime detection mode using widely available commercial instruments (luminometers). The proposed platform is superior over the existing methods in that it substantially reduces the cost of reagents, reduces the assay time from days to minutes and is adaptable to high-throughput format for application in large and small scale drug discovery projects. The proposed SBIR project is in response to the NIH call for new approaches aimed at reducing costs and increasing speed of preclinical drug development. PUBLIC HEALTH RELEVANCE: Antiviral therapy represents an important frontier for development of potential lifesaving products. Worldwide, millions of people suffer from viral infections each year. Approximately 360 million people worldwide suffer from hepatitis B virus, the major cause of liver cancer. Worldwide more than 170 million people are infected with hepatitis C, the leading cause of acute liver inflammation and liver cancer. Around the world more than 42 million people are infected with lifethreatening human immunodeficiency virus (HIV), including more than 3 million children. To address the growing medical needs, there is a steady increase in the number of antiviral compounds in development. The proposed SBIR project will create a knowledge base and establish a new technology, which reduces the cost and time of developing pharmaceutical antiviral products with a large health impact in the USA and around the world.