Small molecules play an important role in biological research and drug discovery. Demonstrating target engagement by a small molecule is essential to understand its mechanism of action. This course will give a solid practical and theoretical grounding in evaluating how a small molecule interacts with its biological target in cells or in vitro, and its role in drug discovery. This course will use proteins of the kinase family to exemplify the general principles and methodologies and their application.
This course is aimed at pre and post doctoral and established researchers developing/using small molecules in drug discovery or for the elucidation of biological questions.
Cellular Thermal Shift Assay (CETSA)
- PROTAC (targeted protein degradation) mode of action cascade (nanoBRET and luminescence assays)
- Overview on click-probe based approach for target engagement by imaging
- Overview on computational methods for target identification
- Overview on genetic methods for target identification (CRISPR-based)