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

Our ever‐increasing understanding of biological systems is providing a range of exciting
novel biological targets, whose modulation may enable novel therapeutic options for many …

This Review explores the class of plant-derived macrocyclic peptides called cyclotides. We
include an account of their discovery, characterization, and distribution in the plant kingdom …

Bioactive peptides have potential as drug leads, but turning them into drugs is a challenge
because of their typically poor metabolic stability. Molecular grafting is one approach to …

Despite recent success in computational design of structured cyclic peptides, de novo
design of cyclic peptides that bind to any protein functional site remains difficult. To address …

Bioorthogonal late‐stage diversification of structurally complex peptides has enormous
potential for drug discovery and molecular imaging. In recent years, transition‐metal …

Highlights•Cyclotides are ultra-stable and tolerant to sequence substitutions in all
loops.•Sequences grafted into a cyclotide scaffold are stabilized and generally maintain …

Asparaginyl endopeptidases (AEPs) catalyze the key backbone cyclization step during the
biosynthesis of plant-derived cyclic peptides. Here, we report the identification of two AEPs …

Bowman-Birk inhibitors (BBIs) are found primarily in seeds of legumes and in cereal grains.
These canonical inhibitors share a highly conserved nine-amino acids binding loop motif …

Nature‐derived cyclic peptides have proven to be a vast source of inspiration for advancing
modern pharmaceutical design and synthetic chemistry. The focus of this Review is …