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Click Chemistry for Cyclic Peptide Drug Design.

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Click chemistry is a powerful tool in constraining peptides into their active conformations. This chapter presents recent advancements involving the use of copper-catalyzed [3 + 2] azide-alkyne cycloaddition (CuAAC), better known as… Click to show full abstract

Click chemistry is a powerful tool in constraining peptides into their active conformations. This chapter presents recent advancements involving the use of copper-catalyzed [3 + 2] azide-alkyne cycloaddition (CuAAC), better known as "click reaction" in the design and synthesis of cyclic peptide and cyclic peptidomimetic compounds. The usage of "click chemistry" reactions includes various topics: (a) mimicking peptide bonds; (b) synthesis of ordered structures; (c) ligation of peptidomimetic scaffolds; and most importantly in this chapter (d) cyclization of peptidomimetic scaffolds using the triazole ring as constraint of conformation.

Keywords: click chemistry; peptide drug; chemistry cyclic; cyclic peptide; chemistry; design

Journal Title: Methods in molecular biology
Year Published: 2019

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