Multicyclic peptides with stable 3D structures are a kind of novel and promising peptide
formats for drug design and discovery as they have the potential to combine the best …

Expanding the repertoire of electrophiles with unique reactivity features would facilitate the
development of covalent inhibitors with desirable reactivity profiles. We herein introduce …

The Golgi apparatus (GA) is the hub of intracellular trafficking, but selectively targeting GA
remains a challenge. We show an unconventional types of peptide thioesters, consisting of …

In recent years, a variety of cycloalkyl groups with quaternary carbons, in particular
cyclopropyl and cyclobutyl trifluoromethyl groups, have emerged as promising bioisosteres …

Recent developments in bond cleavage reactions have expanded the scope of
bioorthogonal chemistry beyond click ligation and enabled new strategies for probe …

Cells produce electrophilic products with the potential to modify and affect the function of
proteins. Chemoproteomic methods have provided a means to qualitatively inventory …

Here we report a new series of hydrolytically stable chemotype heteroaromatic azoline
thioethers (HATs) to achieve highly selective, rapid, and efficient covalent labeling of …

Peptide stapling emerged as a versatile strategy to recapitulate the bioactive helical
conformation of unstructured short peptides in water to improve their therapeutic properties …

Significant efforts have been invested to develop site-specific protein modification
methodologies in the past two decades. In most cases, a reactive moiety was installed onto …

The occurrence of sulfoximines and sulfonimidoyl groups in biologically active molecules
within pharmaceuticals and agrochemicals has notably increased in the past decade. This …