Technological advances and breakthrough developments in the pharmaceutical field are
knocking at the door of the “undruggable” fortress with increasing insistence. Notably, the …

The development of potent, specific, and pharmacologically viable chemical probes and
therapeutics is a central focus of chemical biology and therapeutic development. However, a …

Glycosyltransferases are a superfamily of enzymes that are notoriously difficult to inhibit.
Here we apply an mRNA display technology integrated with genetic code reprogramming …

mRNA display of macrocyclic peptides has proven itself to be a powerful technique to
discover high-affinity ligands for a protein target. However, only a limited number of …

Inhibitors of heterotrimeric G proteins are being developed as therapeutic agents.
Epitomizing this approach are YM-254890 (YM) and FR900359 (FR), which are efficacious …

Interactions between proteins and α-helical peptides have been the focus of drug discovery
campaigns. However, the large interfaces formed between multiple turns of an α-helix and a …

In this retrospective/perspective, I will share thoughts on developing and applying the activity‐
based protein profiling (ABPP) technology, an endeavor that has consumed much of our …

Caspases are a highly conserved family of cysteine-aspartyl proteases known for their
essential roles in regulating apoptosis, inflammation, cell differentiation, and proliferation …

G-protein–coupled receptors (GPCRs) compose the largest family of transmembrane
receptors and are targets of approximately one-third of Food and Drug Administration …

Many G protein-coupled receptors (GPCRs) initiate a second phase of stimulatory
heterotrimeric G protein (Gs)-coupled cAMP signaling after endocytosis. The prevailing …