Kinase Inhibitors: Types and Mechanisms

This lecture delves into the world of kinase inhibitors, focusing on the different types defined by their site of interaction and the mechanisms of action. The instructor discusses the critical roles of kinases in cellular signaling, the approval status of small-molecule kinase inhibitors by the US FDA, and the emergence of new targeted covalent drugs. Various concepts such as ATP-competitive and -non-competitive inhibitors, transition state analog drugs, and irreversible mechanism-based inactivators are explored. The session also covers the experimental evaluation of reversibility for drugs, the behavior of slow on/off inhibitors, and the importance of covalent drugs in modern pharmaceutical research.