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.

这个小企业创新研究第一阶段项目强调了第一个集成高通量管道的开发战略，以合成和评估新型糖-药物缀合物。这项拟议的I期研究的核心创新是酶催化的一步糖基化反应，该反应还提供了适合HT筛选的方便的比色读数。虽然该I期研究的重点是产生和评价新型糖-药物缀合物的抗癌活性，但所述的基本糖基化平台可应用于合成任何类型的糖缀合物。因此，所描述的方法有可能大大提高我们的理解和利用复杂的碳水化合物在生物学，工程和medicine.The更广泛的/商业的影响，这项研究是直接和长期的作用。直接的收益来自于小分子糖苷的快速生成，作为潜在的药物发现的领导，将推进医学领域。拟议研究的长期影响将源于合成复杂碳水化合物的技术平台的可用性，该技术平台可以很容易地被非专业人员使用。有了这个技术平台，工程师，生物学家和/或医生将能够快速生成复杂的碳水化合物，用作材料科学，纳米技术，工程，糖生物学和医学中的新型试剂/支架。因此，预期本文所述的所提出的管道的成功开发将糖的作用转变为远远超出治疗开发的领域。