Enzyme Inhibition Mechanisms

This lecture covers the modulation of enzyme activity and the mechanism of action of small-molecule-based drugs, focusing on reversible and irreversible inhibitors. Students are presented with chemical structures of drugs used in treating non-small cell lung cancer and are tasked with identifying the type of inhibition. The lecture delves into progress curves of enzyme activity inhibition, distinguishing between reversible and irreversible schemes. Additionally, crystal structures of enzymes bound by drugs are analyzed to determine competitive or non-competitive inhibition. Students are also challenged to draw mechanisms of covalent bond formation between drugs and enzyme residues. The lecture concludes with a discussion on synthesizing covalent drugs targeting enzyme sites, evaluating potential benefits and concerns.