Proteins are the main targets of most drugs; however, system-wide methods to monitor
protein activity and function are still underused in drug discovery. Novel biochemical …

Targeted protein degradation (TPD) provides unprecedented opportunities for drug
discovery. While the proteolysis-targeting chimera (PROTAC) technology has already …

Receptor tyrosine kinases (RTKs) are transmembrane receptors of great clinical interest due
to their role in disease, notably cancer. Since their discovery, several mechanisms of RTK …

Background Monitoring target engagement at various stages of drug development is
essential for natural product (NP)-based drug discovery and development. The cellular …

Target identification is an essential part of the drug discovery and development process, and
its efficacy plays a crucial role in the success of any given therapy. Although protein target …

The solute carrier (SLC) superfamily represents the biggest family of transporters with
important roles in health and disease. Despite being attractive and druggable targets, the …

Only around 20% of the human proteome is considered to be druggable with small-molecule
antagonists. This leaves some of the most compelling therapeutic targets outside the reach …

Small molecule chemical probes are valuable tools for interrogating protein biological
functions and relevance as a therapeutic target. Rigorous validation of chemical probe …

Increasing attention has been focused on the study of protein–metabolite interactions (PMI),
which play a key role in regulating protein functions and directing an orchestra of cellular …

Highlights•In-vitro evolution and whole genome sequencing elucidates gene–drug
interactions.•Cellular thermal shift assay and mass spectrometry directly reveals small …