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EXAM 1 PHARMACOLOGY

Terms in this set (23)

Which of the following statements about protein tertiary structure is false?
A. Proteins fold up into a tertiary structure such as that most amino acids with hydrophilic residues are exposed to the aqueous surroundings
B. Proteins fold up into a tertiary structure such that most amino acids with hydrophobic residues are in the center and hidden from the aqueous surroundings
C. Proteins fold up into a tertiary structure such that most amino acids with hydrophobic residues are exposed to the aqueous surroundings
D. Interactions between amino acid residues are important in protein tertiary structure
C. Proteins fold up into a tertiary structure such that most amino acids with hydrophobic residues are exposed to the aqueous surroundings
Which of the following descriptions best describes a coenzyme
1. A non protein substance that is required by an enzyme if it is to catalyze a reaction
2. A non-protein organic molecule that is required by some enzymes in order to catalyze a reaction on a substrate
3. A non-protein organic molecule that is bound covalently to an active site of an enzyme, an which is required if the enzyme is to catalyze a reaction on a substrate
4. A compound which is bound to the active site and undergoes a reaction
1. A non protein substance that is required by an enzyme if it is to catalyze a reaction
Which of the following amino acids acts as an acid-base catalyst in enzyme reaction mechanisms
1. Serine
2. Phenylalanine
3. Histidine
4. Tryptophan
3. Histidine
Which of the following descriptions best describes a competitive enzyme inhibitor?
1. A drug that binds to an active site and undergoes a reaction
2. A drug that binds to an active site and inhibits the enzyme, but which is displaced by increasing the concentration of substrate
3. A drug that binds to an active site and inhibits the enzyme, but is not displaced by increasing the concentration of substrate
4. A drug that binds to a different binding site from the active site and affects the activity of the enzyme
2. A drug that binds to an active site and inhibits the enzyme, but which is displaced by increasing the concentration of substrate
Which statement best describes the relevance of an allosteric binding site to medicinal chemistry?
A. It is more hydrophobic than normal binding sites and accepts hydrophobic drugs in preference to hydrophilic drugs
B. A larger variety of drug structures will bind to the allosteric site than to the active site
C. Drugs can be designed based on the structure of the endogenous chemicals which bind to allosteric sites and control enzyme activity
D. Drugs can be designed based on the transition state of the enzyme-catalyzed reaction
C. Drugs can be designed based on the structure of the endogenous chemicals which bind to allosteric sites and control enzyme activity
Identify an amino acid in an active site whose residue could bind a drug, principally by hydrogen bonding.
A. Serine
B. Aspartic Acid
C. Valine
D. Glycine
A. Serine
What type of receptor is this?
Metabotropic receptor (GPCR)
Ligand-gated ion channel
Voltage-gated ion channel
Nuclear Receptor
B. Ligand-Gated Ion Channel
Select the incorrect pathway
G⍺S: + Adenylyl Cyclase → ↑ cAMP → + PKA → ↑ Ca2+
G⍺q: + PLC → ↑ diacylglycerol & IP3 → + PKC & ↑ Ca2+
G⍺i: - Adenylyl Cyclase → ↓ cAMP → - PKA → ↓ Ca2+ & ↑ K+
G⍺S: + Adenylyl Cyclase → ↓ cAMP → + PKA → ↑ Ca2+
D. G⍺S: + Adenylyl Cyclase → ↓ cAMP → + PKA → ↑ Ca2+
Which drug is most potent?
Drug A
Drug B
Drug D
Drug G
D. Drug G
Where does a drug bind a nuclear receptor?
On the cell membrane
In the cytosol
In the nucleus
In the blood
B. In the cytosol
Which of the following describes induction?
Activation of an enzyme
Inhibition of an enzyme
Increased production of an enzyme
Decreased production of an enzyme
C. Increased Production of an Enzyme
How many times does a GPCR pass through the cell membrane?
Three times
Five times
Seven times
Once
Seven times
Which of the following is true regarding ionic interactions?

A. Ionic bonds are the most important initial interaction as the drug enters the binding site
B. The strongest interactions happen in hydrophilic environments
C. The greater the distance between the groups the stronger the interaction
D. Takes place between groups sharing the same chargeA
A. Ionic bonds are the most important initial interaction as the drug enters the binding site
Which of the following orders describes bond strength from strongest to weakest?

A. Van der Waals > ion ion > ion dipole > dipole dipole
B. Ion ion > dipole dipole > ion dipole > Van der Waals
C. Ion ion > ion dipole > dipole dipole > Van der Waals
D. Van der Waals > ion dipole > dipole dipole > ion ion
C. Ion ion > ion dipole > dipole dipole > Van der Waals
Letter A represents a HBA or HBD?
HBA
Letter B represents what type of bonding?
Hydrophobic
Which of the following is false regarding protein structures?

A. The primary amino acid linkage is a result of peptide bonds
B. Hydrophobic interactions are the most important interaction in determining the tertiary structure
C. In the secondary structure the side chains are usually pointed above the B sheet or outward in the alpha helix
D. Hydrophilic amino acids fold inward to interact with other hydrophilic areas
D. Hydrophilic amino acids fold inward to interact with other hydrophilic areas
True or False
Cofactors and coenzymes are protein substances that are required for the reaction to occur
False: They are NON-PROTEINS
Place the enzymatic reaction steps in order... (1-5)
_ Enzyme recycled
_ Substrate approaches active site
_ Enzyme substrate complex forms
_ Products released
_ Substrate transformed into products
5, 1, 2, 4, 3
Which of the following best describes a allosteric site?
A. An allosteric site is found within the active site
B. The allosteric site can only result in inhibition of the enzyme
C. Allosteric binding can provide feedback on regulating the enzyme function
D. Allosteric binding is a result of only hydrogen bonds
C. Allosteric binding can provide feedback on regulating the enzyme function
Which of the following is NOT how reversible inhibitors bind to receptors?
A. Dipole interactions
B. Covalent bonds
C. Ion-dipole interactions
D. Van Der Waals
E. All of the above
B. Covalent Bonds
T or F:
Reversible inhibitors can be overcome by increasing the number of substrates
True
Rank these inhibitors from most potent to least potent
Inhibitor A: IC50 of 2.7
Inhibitor B: IC50 of 4.3
Inhibitor C: IC50 of 1.23
Inhibitor D: IC50 of 10
C: 1.23 > A: 2.7 > B: 4.3 > D: 10
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