2. Conformational change The enzyme switches back and forth between the two forms. They are in equilibrium. Inactive form Active form Allosteric Regulation of Enzymes
4. When the enzyme is in its inactive form, the allosteric sites on the regulatory subunits can accept inhibitor. Allosteric regulation Inactive form Allosteric Regulation of Enzymes Catalytic subunit Regulatory subunit
5. Allosteric regulation Inactive form Allosteric Regulation of Enzymes Catalytic subunit Regulatory subunit Allosteric inhibitor
6. When the enzyme is in its active form, the active sites on the catalytic subunits can accept substrate. Allosteric regulation Active form Allosteric Regulation of Enzymes
7. Once a site is filled with a substrate or inhibitor, binding at a second site of the same type is favored. Cooperativity Allosteric Regulation of Enzymes Substrate
20. TRADITIONAL DRUG DESIGN Lead generation: Natural ligand / Screening Biological Testing Synthesis of New Compounds Drug Design Cycle If promising Pre-Clinical Studies
21.
22. Structure-based Drug Design (SBDD) Molecular Biology & Protein Chemistry 3D Structure Determination of Target and Target-Ligand Complex Modelling Structure Analysis and Compound Design Biological Testing Synthesis of New Compounds If promising Pre-Clinical Studies Drug Design Cycle Natural ligand / Screening