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 …

Bioconjugation chemistry has been used to prepare modified biomolecules with functions
beyond what nature intended. Central to these techniques is the development of highly …

Natural peptides show high degrees of specificity in their biological action. However, their
therapeutical profile is severely limited by their conformational freedom and metabolic …

With advances in sequencing technology, uncharacterized proteins and domains of
unknown function (DUFs) are rapidly accumulating in sequence databases and offer an …

Macrocycles are of increasing interest as chemical probes and drugs for intractable targets
like protein–protein interactions, but the determinants of their cell permeability and oral …

Chiral macrocycles are commonly found in nature and have strong binding affinity to their
targets. Thus, the development of efficient macrocyclization strategies is an important goal in …

The olefin metathesis reaction is finding increasing use in drug discovery and process
chemistry, with a number of applications now implemented at commercial manufacturing …

Many cyclic peptide natural products are larger and structurally more complex than
conventional small molecule drugs. Although some molecules in this class are known to …

Synthetic macrocycles derived from sequence-defined oligomers are a unique structural
class whose ring size, sequence and structure can be tuned via precise organization of the …

Interest in macrocycles as potential therapeutic agents has increased rapidly.
Macrocyclization of bioactive acyclic molecules provides a potential avenue to yield novel …