Activation and masking of enzymatic activity on demand is of the highest importance in nature. It is achieved via chemical interconversion of enzymes and the corresponding zymogens through, for example, proteolytic processing or reversible phospho...
Precision and Controlled Modification of Proteins using Multifunctional Chemical Constructs
Von Wiley-VCH zur Verfügung gestellt
Bioconjugation of chemical entities to biologically active proteins has increased our insight in the inner workings of a cell and resulted in novel therapeutic agents. A current challenge is the efficient generation of homogeneous conjugates of native proteins, not only when isolated, but also when still present in their native environment. To do this, various features of protein-modifying enzymes have been combined in artificial constructs. In this concept, the current status of this approach is evaluated, and the interplay between designs and protein modification will be discussed. Particular focus is directed on the protein-binding anchor, the chemistry that is used for the modification, and the linker that connects these two units. Suggestions how to include additional elements such as a trigger-responsive switch that regulated protein modification are also presented.Zum Volltext
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