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14 Cards in this Set

  • Front
  • Back
What shape are Irrevesible Inhibitors in?
Inhibitor is likely to be similar in structure to the substrate
What are enzyme kinetics used to compare?
Enzyme kinetics are used to compare the activity of enzyme inhibitor. Compounds with high IC50 are less powerful inhibitors than those with low IC50.
What is the difference between uncompetative inhibitors and non-competative inhibitors?
Uncompetative Inhibitors are inhibitors that can only bind reversibly to an enzyme when the substrate is already bound to the active site.

Non-competative inhibitors are inhibitors that bind to allosteric binding sites and inhibit an enzyme-catalysed reaction without affecting the abitlity of the substrate to bind to the active site.
T/F
Enzymes lower the activation energy of a reaction, but deltaG remains the same.
True
What theory can explain why enzymes can catalyse reactions involving a wide range of substrate?
Induced Fit Theory
What are the most important INITIAL INTERACTIONS as a drug enters the binding site?
Ionic Bonds
What type of intermolercular bonding force is due to transient areas of high and low electron densities leading to temporary dipoles?
Van der Waals interactions
How do intercalating agents work on DNA?
They contain planar aromatic or heteroaromatic ring systems that slip between the base pairs and disrupt the shape of the helix. Intercalation prevents replication and transcription and can inhibit topoisomerases. They usually slide in at either the major or minor groove
How does the intercalating agent Dactomycin work?
It intercalates via the minor groove, preventing unwinding of DNA double helix and Blocks Transcription by blocking DNA-dependant RNA polymerase.
How do alkylating agents affect DNA?
Can cause interstrand and intrastrand cross-linking if two electrophilic groups are present.
They contain highly electrophilic groups that form covalent bonds to nucleophilic groups in DNA
How do Metalliating agents affect DNA?
Affect Intrastrand links rather than interstrand. binds to DNA in guanine rich regions causing localized unwinding of DNA double helix, thereby inhibiting transcription.
How do Micro-RNA affect mRNA?
Micro-RNA are short segments of dsRNA recognised by enzyme complex RISC to produce ssRNA (small interfering or small inhibitory RNA siRNA). It binds to the complementary region of mRNA and mRNA is cleaved by enzyme complex.
What is a drug that mimics the natural messenger?
Agonist
What is a drug that blocks the binding of natural messenger?
Antagonist