PD U0126 PD (CI-1040) PD Structures of MEK Inhibitors
Model structure of MEK with bound inhibitor
Gap1: G1 phase Growth and preparation for DNA replication Synthesis: S phase Synthesis of DNA and centrioles Gap2: G2 phase Preparation for mitosis and cell division Mitosis: M phase Equal division of chromosomal content into two daughter cells The Cell Cycle
days Growth Curves: U0126 causes a reduc- tion in cell number. Cells accumulate in G1.
Enzyme catalysis: What are enzymes really doing?
Km: Michaelis constant k 1, k -1, k 2 : rate constants for the individual steps Enzyme kinetics (Michaelis Menten)
E E E E E E S S P P P P S S E E S S E E S S nI S S E E E E cI S S 1. Enzyme catalysis 2. Competitive inhibition 3. Noncompetitive inhibition
Enzyme inhibition: competitive vs noncompetitive