Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

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 …

Peptides are a growing therapeutic class due to their unique spatial characteristics that can
target traditionally “undruggable” protein–protein interactions and surfaces. Despite their …

Protein–protein interactions (PPIs) are involved at all levels of cellular organization, thus
making the development of PPI inhibitors extremely valuable. The identification of selective …

The selective chemical modification of biological molecules drives a good portion of modern
drug development and fundamental biological research. While a few early examples of …

Bioconjugation methodologies have proven to play a central enabling role in the recent
development of biotherapeutics and chemical biology approaches. Recent endeavours in …

Reactions based on transition metals have found wide use in organic synthesis, in particular
for the functionalization of small molecules,. However, there are very few reports of using …

Peptide stapling is a strategy for constraining short peptides typically in an alpha-helical
conformation. Stapling is carried out by covalently linking the side-chains of two amino …

To optimize drug candidates, modern medicinal chemists are increasingly turning to an
unconventional structural motif: small, strained ring systems. However, the difficulty of …

A noticeable increase in molecular complexity of drug targets has created an unmet need in
the therapeutic agents that are larger than traditional small molecules. Macrocycles, which …