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This review article highlights the strategies to successfully perform an efficient solid-phase synthesis of complex peptides including posttranslational modifications, fluorescent labels, and reporters or linking groups of exceptional value for biological studies of several important diseases. The solid-phase approach is the best alternative to synthesize these peptides rapidly and in high amounts. The key aspects that need to be considered when performing a peptide synthesis in solid phase of these molecules are discussed.

Solid-phase peptide synthesis: an overview focused on the preparation of biologically relevant peptides