CAREER: Macromolecular glycosidase mimics

职业：大分子糖苷酶模拟物

• 批准号: 1244755
• 负责人: Susanne Striegler
• 金额: $ 17.44万
• 依托单位: University of Arkansas
• 依托单位国家: 美国
• 项目类别: Standard Grant
• 财政年份: 2012
• 资助国家: 美国
• 起止时间: 2012-05-15 至 2014-05-31
• 项目状态: 已结题
• 来源: https://www.nsf.gov/awardsearch/showAward?AWD_ID=1244755&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高分子化学项目职业奖的支持下，奥本大学化学系的 Susanne Striegler 教授将重点研究通过检查模板化微凝胶作为催化剂来开发一种选择性糖基化的新方法。计划的研究利用糖苷和金属络合物的挑战性合成，并将采用抑制测定法来提供有关使用设计的过渡态类似物作为酶抑制剂的重要信息。现代光谱和量热方法将用于为合成的过渡态类似物和铜（II）配合物之间的配位行为提供基本见解。乳液聚合将用于将氮杂糖苷-金属络合物组件固定到模板化微凝胶中，该微凝胶将充当可溶性均质催化剂。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糖苷裂解，即糖基转移到水中。这项研究的结果将为新型大分子催化剂作为传统合成和酶促方法的替代品奠定基础，并为合成具有前瞻性药理作用的糖复合物开辟新的方向。凭借这一职业奖，斯蒂格勒教授将显着增强目前关于过渡态类似物的知识，过渡态类似物既可以作为酶抑制剂，也可以作为先进合成材料制备的模板。正在为开发复杂的大分子催化剂奠定基础，该催化剂可将糖基部分转移到除水之外的复杂受体上。这些研究还为制备基于配位键的高效大分子酶模拟物开辟了新的研究方向。实验演示迷你课程将突出化学的优点并提供与日常生活的联系。对可见现象的解释将激发观众对科学的兴趣，其中包括来自附近历史悠久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、其教师和指导员以及其他感兴趣的公众。 PI 实验室的研究机会包括暑期研究项目和为当地高中学生开设的短期有机合成课程。将提供有机化学的实践经验和社交机会，以进一步体现学生对化学职业的兴趣。参与该项目的研究生和本科生将接受化学和生物学交叉领域的培训。他们将获得执行（无机）有机合成（包括聚合）的技能，对配位事件进行光谱和量热表征，并确定酶和合成催化剂的动力学曲线。此外，他们还将参加面向公众的外展计划，特别关注阿拉巴马州农村地区的非裔美国学生。