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 …

Many proteins exert their biological activities through small exposed surface regions called
epitopes that are folded peptides of well‐defined three‐dimensional structures. Short …

The past two decades have witnessed the emergence of macrocycles, including macrocyclic
peptides, as a promising yet underexploited class of de novo drug candidates. Both …

Molecules that covalently bind macromolecular targets have found widespread applications
as activity-based probes and as irreversibly binding drugs. However, the general reactivity of …

Conspectus Cyclic peptides can bind to protein targets with high affinities and selectivities,
which makes them an attractive modality for the development of research reagents and …

Efficient and site‐specific modification of native peptides and proteins is desirable for
synthesizing antibody‐drug conjugates as well as for constructing chemically modified …

Targeting protein surfaces and protein–protein interactions (PPIs) with small molecules is a
frontier goal of chemical biology and provides attractive therapeutic opportunities in drug …

Macrocyclic compounds such as cyclic peptides have emerged as a new and exciting class
of drug candidates for inhibition of intracellular protein–protein interactions, which are …

Peptide display technologies are a powerful method for discovery of new bioactive
sequences, but linear sequences are often very unstable in a biological setting …

Macrocyclic peptides (MPs) have positioned themselves as a privileged class of compounds
for the discovery of therapeutics and development of chemical probes. Aided by the …