This Account provides an overview and examples of function-oriented synthesis (FOS) and
its increasingly important role in producing therapeutic leads that can be made in a step-…

The ability of a drug or probe to cross a biological barrier has historically been viewed to be
a function of its intrinsic physical properties. This view has largely restricted drug design and …

With over 20 antibody‐drug conjugates in clinical trials as well as a recently FDA‐approved
drug, it is clear that this is becoming an important and viable approach for selectively …

Staphylococcus aureus is considered to be an extracellular pathogen. However, survival of
S. aureus within host cells may provide a reservoir relatively protected from antibiotics, thus …

Recent single-cell studies of cancer in both mice and humans have identified the
emergence of a myofibroblast population specifically marked by the highly restricted leucine-rich-repeat…

Many cancer therapeutic agents elicit resistance that renders them ineffective and often
produces cross-resistance to other drugs. One of the most common mechanisms of resistance …

Heterobifunctional compounds that direct the ubiquitination of intracellular proteins in a
targeted manner via co-opted ubiquitin ligases have enormous potential to transform the field of …

The biological and medicinal impacts of proteolysis-targeting chimeras (PROTACs) and
related chimeric molecules that effect intracellular degradation of target proteins via ubiquitin …

The reversible attachment of a small-molecule drug to a carrier for targeted delivery can
improve pharmacokinetics and the therapeutic index. Previous studies have reported the …

The ability to selectively degrade proteins with bifunctional small molecules has the potential
to fundamentally alter therapy in a variety of diseases. However, the relatively large size of …