CAREER: Macromolecular glycosidase mimics

职业：大分子糖苷酶模拟物

• 批准号: 0746635
• 负责人: Susanne Striegler
• 金额: $ 58.22万
• 依托单位: Auburn University
• 依托单位国家: 美国
• 项目类别: Standard Grant
• 财政年份: 2008
• 资助国家: 美国
• 起止时间: 2008-06-01 至 2012-10-31
• 项目状态: 已结题
• 来源: https://www.nsf.gov/awardsearch/showAward?AWD_ID=0746635&HistoricalAwards=false
• 关键词: CAREER; Macromolecular; glycosidase; mimics

With the support of this CAREER Award from the Organic and Macromolecular Chemistry Program at the National Science Foundation, Professor Susanne Striegler, of the Department of Chemistry at Auburn University will focus on developing a novel method for selective glycosylation by examining templated microgels as catalysts. The studies planned utilize challenging syntheses of glycosides and metal complexes, and will employ inhibition assays to provide crucial information on the use of the designed transition state analogues as enzyme inhibitors. Modern spectroscopic and calorimetric methods will be applied to provide fundamental insights into the coordination behavior between the synthesized transition state analogues and copper(II) complexes. Emulsion polymerization will be employed to immobilize the azaglycoside-metal complex assemblies into templated microgels that will function as soluble, homogenous catalysts. The material obtained will be characterized by kinetic experiments to probe the metal complex accelerated glycoside cleavage, i.e. glycosyl transfer to water. The results of this study will provide the foundation for novel macromolecular catalysts as an alternative to conventional syntheses and enzymatic approaches and open new directions towards the synthesis of glycoconjugates with prospective pharmacological effect. With this CAREER award Professor Stiegler will significantly enhance the current knowledge on transition state analogues to act as both inhibitors of enzymes and templates for the preparation of advanced synthetic materials. Foundations are being laid for the development of sophisticated macromolecular catalysts, which transfer glycosyl moieties to complex acceptors other than water. The studies proposed also open new research directions for the preparation of efficient, macromolecular enzyme mimics based on coordinative bonds. The experimental demonstration mini-course will highlight the merits of chemistry and provide connections to daily life. Explanations of a visible phenomenon will spark interest for sciences in an audience that will include students from nearby, historically black high schools and colleges, e.g. Bullock County High School or Tuskegee University, their teachers and instructors, and other interested members of the public. Research opportunities in the PI's laboratory include a summer research project and a short organic synthesis course for students from local high schools. Hands-on experience in organic chemistry and networking opportunities will be offered to further manifest the students' interest in a career in chemistry. Graduate and undergraduate students involved in this program will be trained at the interface of chemistry and biology. They will obtain skills to perform (in)organic syntheses including polymerizations, conduct spectroscopic and calorimetric characterization of coordination events, and determine kinetic profiles of enzymes and synthetic catalysts. Additionally, they will participate in outreach programs to the general public with particular focus on the African-American students in rural Alabama.

在国家科学基金会有机和大分子化学计划的职业奖的支持下，奥本大学化学系的Susanne Striegler教授将专注于通过研究模板微凝胶作为催化剂来开发一种选择性糖基化的新方法。计划的研究利用具有挑战性的糖苷和金属络合物的合成，并将采用抑制试验，以提供关于使用所设计的过渡态类似物作为酶抑制剂的关键信息。现代光谱和量热方法将被应用到合成的过渡态类似物和铜（II）配合物之间的协调行为提供基本的见解。将采用乳液聚合将阿扎糖苷-金属络合物组装体包裹成模板化的微凝胶，其将用作可溶的均相催化剂。所获得的材料将通过动力学实验来表征，以探测金属络合物加速的糖苷裂解，即糖基转移到水中。本研究的结果将为新型大分子催化剂作为传统合成和酶法的替代方法提供基础，并为具有潜在药理作用的糖缀合物的合成开辟新的方向。有了这个CAREER奖教授斯蒂格勒将显着提高目前的知识过渡态类似物作为酶的抑制剂和模板制备先进的合成材料。正在为开发复杂的大分子催化剂奠定基础，这些催化剂将糖基部分转移到水以外的复杂受体。这些研究也为基于配位键的高效大分子酶模拟物的制备开辟了新的研究方向。实验示范迷你课程将突出化学的优点，并提供与日常生活的联系。对可见现象的描述将激发观众对科学的兴趣，这些观众将包括来自附近历史上的黑人高中和大学的学生，例如布洛克县高中或塔斯基吉大学，他们的教师和导师，以及其他感兴趣的公众成员。PI实验室的研究机会包括夏季研究项目和当地高中学生的短期有机合成课程。在有机化学和网络机会的实践经验将提供进一步体现学生在化学职业生涯的兴趣。参与该计划的研究生和本科生将在化学和生物学的接口进行培训。他们将获得执行（在）有机合成，包括聚合，进行配位事件的光谱和量热表征，并确定酶和合成催化剂的动力学曲线的技能。此外，他们还将参加面向公众的外联方案，特别关注亚拉巴马农村的非洲裔美国学生。