点击化学及生物正交反应.pptVIP

;;文献背景;点击化学—定义;点击化学—反应特征;正交试验设计：研究多因素多水平的又一种设计方法，它是根据正交性从全面试验中挑选出部分有代表性的点进行试验特点：“均匀分散，齐整可比”，高效率、快速、经济;点击化学—反应类型 1. STRATEGY OF CLICK CHEMISTRY AND BIOORTHOGONAL REACTIVITY 1.1.叠氮，炔烃环加成反应Azide-Alkyne Cycloaddition. 1.2.自由铜叠氮，炔烃环加成反应Copper-Free Azide-Alkyne Cycloaddition. 1.3. 道丁格连接反应Staudinger Ligation. 1.4.其他反应 Other Reactions. 1.5.比较生物正交反应条件Comparison of Bioorthogonal Reactions and Conditions.; 2. IMPACTS OF CLICK CHEMISTRY ON DRUG DEVELOPMENT ;Derivatization of Lipid Probes. Modification. Labeling of Nucleotides for Imaging DNA and RNA.; FIGURE 2: In situ combinatorial drug development. (A) General schematic for templated inhibitor development. Binding of reactants by the target enzyme leads to catalytic formation of the optimal inhibitor. (B) Application of this approach to the development of a potent bisubstrate inhibitor of acetylcholinesterase.;FIGURE 4: Incorporation of unnatural amino acids into proteins. (A) Noncanonical amino acids that have been introduced into proteins. (B) Schematic for unnatural amino acid mutagenesis using a genetically engineered tRNA synthetase.;FIGURE 5: Metabolic labeling of cell-surface glycans using bioorthogonal chemistry. (A) Azide and alkyne-derivatized sugars that successfully infiltrate biosynthetic pathways. (B) Schematic for the incorporation of simple sugar derivatives onto glycoproteins via metabolic pathways,followed by selective labeling through bioorthogonal chemistry.;展 望;Thanks for your attention