Sulfur(VI) Fluoride Exchange (SuFEx): new developments and biological applications

硫（VI）氟化物交换（SuFEx）：新进展和生物应用

• 批准号: 9009485
• 负责人: KARL BARRY SHARPLESS
• 金额: $ 53.9万
• 依托单位: SCRIPPS RESEARCH INSTITUTE, THE
• 依托单位国家: 美国
• 财政年份: 2016
• 资助国家: 美国
• 起止时间: 2016-01-01 至 2019-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/9009485
• 关键词: Biological; Carbon; Carboxylic Acids; Cells; Charge; Chemical Structure; Chemistry; Child; Development; Developmental Process; Disease; Embryo; Embryonic Development; Family; Fluoride Ion; Fluorides; Fluorine; Goals; Health; Hydrogen Bonding; Imidazole; In Vitro; Isotopes; Libraries; Methodology; Neurodevelopmental Disorder; Oxygen; Pathway interactions; Positron-Emission Tomography; Process; Production; Proteins; Protocols documentation; Reaction; Side; Sulfur; System; Water; Work; Zebrafish; adduct; aqueous; aspartylglutamate; biological research; developmental disease; functional group; improved; in vivo; molecular assembly/self assembly; novel therapeutics; radiotracer; screening; small molecule

 DESCRIPTION (provided by applicant): The objective of this project is to develop a new family of click chemistry reactions, termed Sulfur(VI) Fluoride Exchange (SuFEx) processes, and to utilize them in biological research. SuFEx relies on readily available materials and simple transformations to produce diverse chemical structures bearing the SVI-F motif, such as OSO2F (fluorosulfate) and SO2F (sulfonyl fluoride). New molecules originating from this chemistry will be used to develop probes functionalized with the 18FO2SO radiotracer for positron emission tomography. Small- molecule screening libraries will be constructed using this methodology to identify active compounds that perturb specific pathways in zebrafish embryogenesis.

 描述（由申请人提供）：该项目的目标是开发一系列新的点击化学反应，称为硫（VI）氟化物交换（SuFEx）过程，并将其应用于生物研究中，SuFEx 依赖于现成的材料和技术。简单的转化可产生带有 SVI-F 基序的多种化学结构，例如 OSO2F（氟硫酸盐）和 SO2F（磺酰氟）。开发用于正电子发射断层扫描的 18FO2SO 放射性示踪剂功能化的探针，将使用这种方法构建小分子筛选库，以识别扰乱斑马鱼胚胎发生中特定途径的活性化合物。