Target Fishing

DARTS is an innovative technique developed based on the principle that the binding of small-molecule drugs to theirtarget proteins reduces the target protein's susceptibility to proteolytic degradation. This technique does not requiredrug modification or depend on drug activity, making it widely applicable for drug screening and target identification.

In DARTS experiments, specific methods are reguired to assess the effects of proteolysis, Commonly used techniguesinclude SDS-PAGE and gel staining methods such as Coomassie Brilliant Blue staining. Additionally, protein two-dimensional electrophoresis (2D-PAGE), gel-based or gel-free mass spectrometry (LC-MS/MS), and other methods canalso be utilized for detection, By comparing the significant differences in proteolysis between the drug-treated andcontrol groups, potential drug targets can be identified forfurther experimental validation.

Kinases include protein kinases, phosphatases, and phosphodiesterases. Among the more than 500 kinases encoded in the human genome, protein kinases represent the largest class. They covalently transfer phosphate groups to other proteins, resulting in protein phosphorylation and altered activity, playing widespread and critical roles in cellular signaling and various complex biological processes.

Dysregulation of protein kinase expression or function can lead to cancer and other diseases. Among well-established drug targets, protein kinases have become a highly important class for drug discovery and screening. To date, approximately 280 kinase inhibitor drugs have been approved, with receptor tyrosine kinase (RTK) inhibitors being the most prominent.

TargetMol has extensive experience in kinase-targeted drug screening, discovery, and development.