SBIR Phase I: Development of a High Throughput Glycosyl-Scanning Platform

SBIR 第一阶段：高通量糖基扫描平台的开发

• 批准号: 1046741
• 负责人: James Prudent
• 金额: $ 15万
• 依托单位: centrose llc
• 依托单位国家: 美国
• 项目类别: Standard Grant
• 财政年份: 2011
• 资助国家: 美国
• 起止时间: 2011-01-01 至 2011-06-30
• 项目状态: 已结题
• 来源: https://www.nsf.gov/awardsearch/showAward?AWD_ID=1046741&HistoricalAwards=false
• 关键词: SBIR; Phase; Development; Throughput; Glycosyl

This Small Business Innovation Research Phase I project highlights a strategy for the development of the first integrated high throughput pipeline to synthesize and evaluate novel sugar-drug conjugates. The core innovation of this proposed phase I study is an enzyme catalyzed one-step glycosylation reaction that also presents a convenient colorimetric readout amenable to HT-screening. While this phase I study is focused upon the generation and evaluation of novel sugar-drug conjugates for anticancer activity, the fundamental glycosylation platform described can be applied to the synthesis any type of glycoconjugate. Thus, the methodology described has the potential to greatly advance our understanding and exploitation of the role of complex carbohydrates in biology, engineering and medicine.The broader/commercial impacts of this research are both immediate and long term. The immediate gain derives from the rapid generation of small molecule glycosides that, as potential drug discovery leads, will advance the field of medicine. The long term impact of the proposed research will stem from the availability of a technology platform for synthesizing complex carbohydrates that can be easily employed by the nonspecialist. With this technology platform, engineers, biologists, and/or physicians will be able to rapidly generate complex carbohydrates to be employed as novel reagents/scaffolds in material science, nanotechnology, engineering, glycobiology and medicine. Thus, successful development of the proposed pipeline described herein is anticipated to transform the role of sugars well beyond the area of therapeutic development.

这个小型企业创新研究阶段I项目强调了制定第一综合高吞吐量管道以合成和评估新型的糖 - 药物结合物的策略。这项拟议的I期研究的核心创新是一种酶催化的一步糖基化反应，它也提出了方便的比色读数，可容纳HT筛查。虽然该阶段I研究集中在新型糖 - 药物结合物以进行抗癌活性上，但所描述的基本糖基化平台可以应用于任何类型的糖缀合物的合成。因此，所描述的方法有可能极大地提高我们对复杂碳水化合物在生物学，工程和医学中的作用的理解和开发。这项研究的更广泛/商业影响既是直接又长期的。即时的收益来自小分子糖苷的迅速产生，因为潜在的药物发现导致了医学领域。拟议研究的长期影响将源于技术平台的可用性，用于合成非专业人士可以轻松使用的复杂碳水化合物。借助这个技术平台，工程师，生物学家和/或医生将能够迅速产生复杂的碳水化合物，以作为材料科学，纳米技术，工程，糖生物学和医学的新型试剂/支架。因此，预计本文所述的拟议管道的成功发展将改变糖的作用，远远超出了治疗性发育领域。