Medicinal Chemistry: Enzyme Inhibition & Drug Interactions - PDF

I Chapter 7 Discuss the importance of the fine balance in the strength of binding interactions between substrate binding to active sites of enzymes Binding hold interactions...

I Chapter 7 Discuss the importance of the fine balance in the strength of binding interactions between substrate binding to active sites of enzymes Binding hold interactions the substrate must be strong enough to long enough for the reaction to occur , but these interactions must also be allow weak enough to the product to leave. 2. Define enzyme inhibition and identify inhibitors as reversible or irreversible inhibition refers Enzyme to the process in which the activity of an enzyme is blocked due to an inhibitor. block ↑ inhibition used to Enzyme site is the active in order to have stronger interactions. binding Reversible inhibitors involve intermolecular bonds and the inhibitor undergoes notoreaction. Irreversible inhibitors bind the active site Substrate is blocked using covalent bonds. active site substrate the from Increasing concentration does not reverse inhibition n. Transition State involves noncovalent bonds , although it is considered a irreversible inhibitor. These drugs transition of are designed to mimic the state an enzyme-catalysed reaction. Transition-state inhibitors bind are likely substrate to more strongly than drugs mimicking the or product. Suicide substrates are agents which are converted irreversible inhibitors the enzyme-catalysed by to reaction. These often covalent bonds. form 3 Categorize reversible inhibitors as competitive, uncompetitive or noncompetitive. There 3 reversible inhibitors competitive are types of , and non-competitive uncompetitive , & - competitive: bind the active site reversibly and can be displaced if the substrate increases. - uncompetitive bind to the enzyme when the substrate will then not overcome the inhibition. Increasing the substrate will not displace the inhibition - - noncompetitives bind to an allosteric , active site inhibiting the enzyme without affecting the of it bind ability to the substrate. Increasing the the substrate inhibitor. will not (likely displace 6. Be able to interpret Lineweaver–Burk graphs or changes in Km and Vmax to determine type of inhibition