Protein‐templated fragment ligation is a novel concept to support drug discovery and can
help to improve the efficacy of protein ligands. Protein‐templated fragment ligations are …

Fragment‐based drug design (FBDD) affords active compounds for biological targets. While
there are numerous reports on FBDD by fragment growing/optimization, fragment linking has …

The discovery of protein ligands, capable of forming a reversible covalent bond with amino
acid residues on a protein target of interest, may represent a general strategy for the …

Cysteine‐reactive small molecules are used as chemical probes of biological systems and
as medicines. Identifying high‐quality covalent ligands requires comprehensive kinetic …

Target‐directed dynamic combinatorial chemistry has emerged as a useful tool for hit
identification, but has not been widely used, in part due to challenges associated with …

Protein‐templated reactions enable the target‐guided formation of protein ligands from
reactive fragments, ideally with no background reaction. Herein, we investigate the …

Abstract Metal‐free triazole turns: 1, 5‐Disubstituted peptidyl triazoles are obtained
regioselectively from the 1, 3‐dipolar cycloaddition of peptidyl phosphoranes and azides …

The generation of bioactive molecules from inactive precursors is a crucial step in the
chemical evolution of life, however, mechanistic insights into this aspect of abiogenesis are …

The phosphorylation of tyrosine residues is an important posttranslational modification of
proteins and regulates the activity of numerous signal transduction pathways, for example, in …

SARS coronavirus main proteases (3CL proteases) have been validated as
pharmacological targets for the treatment of coronavirus infections. Current inhibitors of …