Protein levels within a cell are not fixed and invariant. Rather, they represent the net result of two continuous and dynamic operations – protein synthesis and protein degradation. These two processes jointly determine a protein’s turnover rate, or the rate […]

As the world of small-molecule therapeutics continues to expand, researchers are broadening their horizons to discover not only straightforward inhibitors of enzymatic activity but also compounds that modulate protein abundance and activity by targeting the upstream steps of RNA transcription, […]

MicroRNAs (miRNAs) are a class of short noncoding RNAs that modulate gene expression across a broad range of developmental and diseaseprocesses. Following their discovery in C. elegans in 1993, miRNAs were initially dismissed as a nematode-specific anomaly. Not until the […]

Since January 2024, 46 novel drugs have been approved by the U.S. Food and Drug Administration (FDA), with roughly half of these being small molecules. These innovations represent life-saving progress in the treatment of a wide range of human diseases, […]

Inductively coupled plasma mass spectrometry (ICP-MS) is a powerful technique for the trace and ultra-trace elemental analysis of a variety of sample types. As the name indicates, this technology makes use of a high-energy argon plasma to break down nebulized […]

Covalent drugs and degraders, defined by their ability to form covalent bonds with their targets, represent a powerful therapeutic modality for the potent and selective inhibition, modulation, or degradation of clinically relevant proteins. Thanks to technological innovations facilitating the screening […]

Traditional drug development depends upon the discovery of a small molecule that binds to the active site of a protein of interest (POI) and functionally blocks its activity. However, this type of ‘occupancy-driven’ pharmacology is only suitable for a narrow […]

DNA-encoded libraries – DELs, for short – have attracted the attention of the pharmaceutical industry in recent years, promising the ability to readily screen millions or billions of potential ligands in parallel by linking small-molecule test compounds to unique DNA […]

The ability to target RNA with small-molecule drugs presents a powerful opportunity for therapeutic intervention. In contrast to traditional drugs, which generally act against proteins, these drugs interact with RNA molecules. In most cases, they function by modulating splicing or […]

Recent publications highlight an “evolving toolbox” of techniques and technologies implemented in covalent inhibitor discovery and design. Though historically covalent compound discovery has been conducted via structure based drug design, direct covalent ligand screening of electrophilic compound libraries has been […]

Affinity Selection Mass Spectrometry (ASMS) is a high throughput screening (HTS) technique for identifying small molecule test compounds based on their binding affinity to a target. Unlike traditional biochemical assays that test a compound’s functional activity, ASMS is a biophysical […]