Target-identification and mechanism-of-action studies have important roles in small-
molecule probe and drug discovery. Biological and technological advances have resulted in …

The design of synthetic, monovalent host–guest molecular recognition pairs is still
challenging and of particular interest to inquire into the limits of the affinity that can be …

Identification and confirmation of bioactive small‐molecule targets is a crucial, often decisive
step both in academic and pharmaceutical research. Through the development and …

The medical and pharmaceutical communities are facing a dire need for new druggable
targets, while, paradoxically, the targets of some drugs that are in clinical use or …

Interest in cleavable linkers is growing due to the rapid development and expansion of
chemical biology. The chemical constrains imposed by the biological conditions cause …

The azide− alkyne cycloaddition provides a powerful tool for bio-orthogonal labeling of
proteins, nucleic acids, glycans, and lipids. In some labeling experiments, eg, in proteomic …

Activity-based protein profiling (ABPP), the use of active site-directed chemical probes to
monitor enzyme function in complex biological systems, is emerging as a powerful post …

Traditional proteomics methodology allows global analysis of protein abundance but does
not provide information on the regulation of protein activity. Proteases, in particular, are …

Membrane proteomics, the large-scale global analysis of membrane proteins, is often
constrained by the efficiency of separating and extracting membrane proteins. Recent …

Arginine-rich cell-penetrating peptides (CPPs) such as Tat and oligoarginine peptides have
been widely used as carriers for intracellular delivery of bioactive molecules. Despite …