| Talk title | Discovery of New Targets of Bioactive Small Molecules and Validation in vivo by Mass Spectrometry Imaging |
| Speaker | Prof. Ho Jeong KWON Professor Yonsei University, South Korea |
| Date & Time | 24 August 2018 (Friday) 11:00-12:00 |
| Venue | Room G004, E12 Building (University of Macau) |
| Abstract | Identifying protein targets of bioactive small molecules and deciphering the specific mechanisms-of-action at the molecular level are crucial steps in the development of drugs to treat human diseases. We have developed target protein identification methods including conventional affinity chromatography using labeled small molecules as well as recent target identification methods with label-free small molecules such as Drug Affinity Responsive Target Stability (DARTS), Cellular Thermal Shift Assay (CETSA), and Thermal Proteome Profiling (TPP) to identify the direct binding proteins of small molecules. This interaction information of small molecule and target protein facilitates structure based better drug development and functional annotation of target protein as well. Furthermore, integration of MALDI-MS imaging technology will enable to validate the interaction of label-free small molecule with target protein in tissue that harnesses the preclinical studies of small molecules with respect to absorption, distribution, metabolism and excretion (ADME). In this presentation, our recent studies on target identification of bioactive small molecules for exploring new mechanism studies and translational applications will present by introducing our case studies of “drug-target” identification and validation of bioactive small molecules from natural products and clinical drugs. |
