Enzyme-catalyzed peptide cyclization

Publication date: December 2017Source: Drug Discovery Today: Technologies, Volume 26Author(s): Marcel Schmidt, Ana Toplak, Peter J.L.M. Quaedflieg, Jan H. van Maarseveen, Timo NuijensThe recent advancement of peptide macrocycles as promising therapeutics creates a need for novel methodologies for their efficient synthesis and (large scale) production. Within this context, due to the favorable properties of biocatalysts, enzyme-mediated methodologies have gained great interest. Enzymes such as sortase A, butelase 1, peptiligase and omniligase-1 represent extremely powerful and valuable enzymatic tools for peptide ligation, since they can be applied to generate complex cyclic peptides with exquisite biological activity. Therefore, the use of enzymatic strategies will effectively supplement the scope of existing chemical methodologies and will accelerate the development of future cyclic peptide therapeutics. The advantages and disadvantages of the different enzymatic methodologies will be discussed in this review.Graphical abstract

Source: Drug Discovery Today: Technologies - July 10, 2018 Category: Drugs & Pharmacology Source Type: research