Highlights•Self-contained overview of current high-throughput screening technologies.•
Expands on the current use of most recent tools, like high-throughput microscopy.•Learn …

Over the past decade, remarkable advances have been witnessed in the development of
small-molecule probes. These molecular tools have been widely applied for interrogating …

Despite advances in genetic and proteomic techniques, a complete portrait of the proteome
and its complement of dynamic interactions and modifications remains a lofty, and as of yet …

Cysteine can be specifically functionalized by a myriad of acid-base conjugation strategies
for applications ranging from probing protein function to antibody-drug conjugates and …

Sulfonyl fluoride electrophiles have found significant utility as reactive probes in chemical
biology and molecular pharmacology. As warheads they possess the right balance of …

Phenotype-based screening has emerged as an alternative route for discovering new
chemical entities toward first-in-class therapeutics. However, clarifying their mode of action …

Phospholipase A2 (PLA2) enzymes are considered the primary source of arachidonic acid
for cyclooxygenase (COX)–mediated biosynthesis of prostaglandins. Here, we show that a …

Genome sequencing projects have provided researchers with a complete inventory of the
predicted proteins produced by eukaryotic and prokaryotic organisms. Assignment of …

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

Endogenous ligands for cannabinoid receptors (" endocannabinoids") include the lipid
transmitters anandamide and 2-arachidonoylglycerol (2-AG). Endocannabinoids modulate a …