Drug Delivery

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  1. Mercapto-PEG-Acids for Bioconjugation 3.7.2 Mercapto-PEG-Acids S-Acetyl-PEG-acids and active esters provide a method for converting amino groups to a thiol, while incorporating PEG units. Conjugation with thiol reactive agents e.g., maleimides, vinyl sulfones or α-halo keto functionalized reaction partners increases the ...
  2. 1st Generation Click Chemistry 1. The Click Reaction Azido and alkyne functions can cyclise by an intramolecular CuI or Cu0 catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC). This so-called Click Reaction, developed by K. Barry Sharpless and Morton Meldal, has meanwhile grown to a widely used type of reaction ...
  3. 2nd Generation Click Chemistry a) Catalyst-free Click Reaction Cycloaddition reactions such as the [3+2] azide-alkyne and the [4+2] Diels-Alder reaction, are becoming common conjugation techniques. Applications range from imaging, drug design and development of sensors, thereby spanning the fields of chemical biology, ...
  4. Recombinant Incorporation of Amino Acids into Proteins a) Recombinant Incorporation of Amino Acids into Proteins Mutant or modified aminoacyl tRNA synthetases (aaRS) have been used to charge non-natural amino acids to the corresponding tRNA, which incorporates them into polypeptides or proteins during recombinant synthesis. As azido homoalanine ...
  5. Peptide Structure Stabilization by Click Chemistry b) Peptide Synthesis with Azido and Alkyne Amino Acids As Boc and Fmoc protected derivatives of both azido and alkyne amino acids are available, they can be introduced into peptide sequences through standard SPPS protocols, for example. In an α-helical secondary structure amino ...
  6. Azido-Masked Amino Function
  7. Carbohydrates for Click Chemistry Protein and lipid glycosilation is a life-governing and omnipresent process. Glycoconjugates display a multitude of biological effects from protein folding and stabilization, energy storage, cell surface interaction through molecular recognition motifs for cell-cell communication, and ...
  8. Click Chemistry in DNA Synthesis 7. Click Chemistry in DNA Synthesis a) Applications and Procedures in DNA Synthesis Due to its unique bioorthogonality the Click reaction is very useful also in any oligonucleotide synthesis. Simple or no workup and purification of the product are further advantages. However, the use of ...
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