A large proportion of protein–protein interactions (PPIs) occur between a short peptide and a
globular protein domain; the peptides involved in surface interactions play important roles …

The late‐stage modification of structurally complex peptides bears great potential for drug
discovery, crop protection, and the pharmaceutical industry, among others. Whereas …

In the past decade, multicomponent reactions have experienced a renaissance as powerful
peptide macrocyclization tools enabling the rapid creation of skeletal complexity and …

Despite the importance of stapled peptides for drug discovery, only few practical processes
to prepare cross‐linked peptides have been described; thus the structural diversity of …

The central dogma of modern biology underscores the pivotal roles proteins play in diverse
biological processes, the study of which necessitates advanced methods to produce …

This Review is devoted to the chemistry of macrocyclic peptides having heterocyclic
fragments in their structure. These motifs are present in many natural products and synthetic …

Peptide stapling is a method for designing macrocyclic alpha‐helical inhibitors of protein–
protein interactions. However, obtaining a cell‐active inhibitor can require significant …

Abstract The dual functionality of 1, 2, 4, 5‐tetrazine as a bioorthogonal reactive unit and a
luminescence quencher has shaped tetrazine‐based probes as attractive candidates for …

Drugs with a covalent mechanism of action benefit from enhanced potency, selectivity, and
in vivo efficacy. Historically, the only covalent drugs on the market have been covalent small …

Protein–protein interactions (PPIs) are tremendously important for the function of many
biological processes. However, because of the structure of many protein–protein interfaces …