Screening of small-molecule libraries is a productive method for identifying both chemical
probes of disease-related targets and potential starting points for drug discovery. In this …

Eukaryotic and prokaryotic organisms possess huge numbers of uncharacterized enzymes.
Selective inhibitors offer powerful probes for assigning functions to enzymes in native …

Deubiquitinating enzymes (DUBs) are an emerging drug target class of~ 100 proteases that
cleave ubiquitin from protein substrates to regulate many cellular processes. A lack of …

Small-molecule probes can illuminate biological processes and aid in the assessment of
emerging therapeutic targets by perturbing biological systems in a manner distinct from …

Dysregulation of lipid metabolism underlies many chronic diseases such as obesity,
diabetes, cardiovascular disease, and cancer. Therefore, understanding enzymatic …

Abstract Protein phosphatase 2A (PP2A) is a highly complex heterotrimeric enzyme that
catalyzes the selective removal of phosphate groups from protein serine and threonine …

S-Palmitoylation is a reversible lipid post-translational modification that has been observed
on mitochondrial proteins, but both the regulation and functional consequences of …

Much of the experimental evidence in the literature has linked altered lipid metabolism to
severe diseases such as cancer, obesity, cardiovascular pathologies, diabetes, and …

Mitochondria play a central role in bioenergetics, and fulfill a plethora of functions in cell
signaling, programmed cell death, and biosynthesis of key protein cofactors. Mitochondria …

Target identification involves deconvoluting the protein target of a pharmacologically active,
small-molecule ligand, a process that is critical for early drug discovery yet technically …