Discovering new bioactive molecules is crucial for drug development. Finding a hit
compound for a new drug target usually requires screening of millions of molecules. Affinity …

Encoding small-molecule information in DNA has been leveraged to accelerate the
discovery of ligands for therapeutic targets such as proteins. However, oligonucleotide …

Bispecific antibody‒drug conjugates (BsADCs) represent an innovative therapeutic
category amalgamating the merits of antibody‒drug conjugates (ADCs) and bispecific …

We report the development of a new oxazole-based cleavable linker to release peptides
from attached cargo. Oxazoles are stable to most reaction conditions, yet they can be rapidly …

Hundreds of peptides can be synthesized by automated parallel synthesizers in a single run.
In contrast, the most widely used peptide purification method–high-pressure liquid …

The first drugs discovered using DNA-encoded chemical library (DEL) screens have entered
late-stage clinical development. However, DEL technology as a whole still suffers from poor …

Amino groups are abundant in both natural and synthetic molecules, offering highly
accessible sites for modifying native biorelevant molecules. Despite significant progress with …

Covalent chemical probes are important tools in chemical biology. They range from post-
translational modification (PTM)-derived metabolic probes, to activity-based probes and …

Peptide-mediated delivery of macromolecules in cells has significant potential therapeutic
benefits, but no therapy employing cell-penetrating peptides (CPPs) has reached the market …

Barbier-type reactions are a classic group of reactions for carbon–carbon bond formation;
however, their common use of stoichiometric metals restricts their widespread application …