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 …

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 …

Multivalent peptide–oligosaccharide conjugates were prepared and used to investigate the
multivalency effect concerning the activity of Bid‐BH3 peptides in live cells. Dextran …

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

Are aliphatic alkynes truly bioorthogonal? In an attempt to prepare clickable ubiquitin
derivatives bearing a C‐terminal propargyl amide, two groups have now independently …

Protein tyrosine phosphatases (PTPs) are key regulators in living systems and thus are
attractive drug targets. The development of potent, selective PTP inhibitors has been a …

Proteintemplat‐gesteuerte Fragmentligationen sind ein neuartiges Konzept zur
Unterstützung der Wirkstofffindung und können dazu beitragen, die Wirksamkeit von …