Question 1

Thiopurine drugs,such as 6-thioguanine,are toxic to some individuals because they have a genetic variation of the enzyme _________________________.

Accepted Answer

thiopurine methyltransferase

Question 2

Briefly explain why a drug candidate that has a partition coefficient (log P)greater than 5 is not a good candidate for oral bioavailability.

Accepted Answer

A partition coefficient of 5 means that the compound is 100,000 times more soluble in
n-octanol than it is in water.This means that its solubility in water will be too low to deliver as an oral drug.

Question 3

Drug candidateIC50(nmol)Log (P)Cmax (µM)BioavailabilityA0.44.67<0.1B0.013.70<0.1C0.33.690.7D0.62.9211Consider the information concerning a related class of potential drugs in the table above.Which one is least soluble in water and most hydrophobic?

Accepted Answer

A)  A 
B)  B 
C)  C 
D)  D 
E)  They are all equally soluble in water. 
A)  A 
B)  B 
C)  C 
D)  D 
E)  They are all equally soluble in water. A

Question 4

)What type of bond is used to link a glucuronic acid group to a xenobiotic?

Accepted Answer

A)  eEster 
B)  gGlycosidic 
C)  aAmide 
D)  pPhosphoester 
E)  tThioether 
A)  eEster 
B)  gGlycosidic 
C)  aAmide 
D)  pPhosphoester 
E)  tThioether

Question 5

What compound is increased by the action of Sildenafil (Viagra)?

Accepted Answer

A)  GTP 
B)  ATP 
C)  AMP 
D)  cAMP 
E)  cGMP 
A)  GTP 
B)  ATP 
C)  AMP 
D)  cAMP 
E)  cGMP

Question 6

________________ is the science that deals with the discovery,chemistry,composition,identification,biological and physiological effects,uses,and manufacture of drugs.

Accepted Answer

The answer of ________________ is the science that deals with...

Question 7

Give three types of conjugation reactions that occur in the metabolism of xenobiotics.

Accepted Answer

1.Addition of glutat

Question 8

First attempts to develop cholesterol-lowering drugs targeted the later steps in cholesterol biosynthesis.Why did this strategy have to be abandoned?

Accepted Answer

A)  These reactions were so efficient that they could not be blocked. 
B)  The accumulation of an insoluble substrate caused cataracts and other deleterious side effects. 
C)  All of the drugs that were developed actually enhanced cholesterol synthesis. 
D)  None of the drugs that were developed could survive the acid conditions in the stomach. 
E)  These drugs caused untreatable gall stones. 
A)  These reactions were so efficient that they could not be blocked. 
B)  The accumulation of an insoluble substrate caused cataracts and other deleterious side effects. 
C)  All of the drugs that were developed actually enhanced cholesterol synthesis. 
D)  None of the drugs that were developed could survive the acid conditions in the stomach. 
E)  These drugs caused untreatable gall stones.

Question 9

Successful drugs have been discovered by which of the following methods?

Accepted Answer

A)  chance observation of a beneficial, though unplanned, physiological effect 
B)  screening natural products with interesting activities 
C)  combinatorial chemical synthesis of large collections of chemically related compounds for screening 
D)  if the structure of the target is known, computer-aided design of compounds that might bind to the target 
E)  All of the answers are correct. 
A)  chance observation of a beneficial, though unplanned, physiological effect 
B)  screening natural products with interesting activities 
C)  combinatorial chemical synthesis of large collections of chemically related compounds for screening 
D)  if the structure of the target is known, computer-aided design of compounds that might bind to the target 
E)  All of the answers are correct.

Question 10

Describe what factors will affect the apparent Kd of a drug under physiological conditions.

Accepted Answer

The K_d of a drug under physiological cond

Question 11

A compound that inhibits HMG-CoA reductase has potential use as a drug that

Accepted Answer

A)  reduces inflammation and can be used to treat arthritis. 
B)  reduces stomach acid production and can be used to treat ulcers. 
C)  reduces blood cholesterol and can be used to treat atherosclerosis. 
D)  increases the concentration of cGMP and can be used to treat erectile dysfunction. 
E)  increases dopamine and can be used to treat schizophrenia. 
A)  reduces inflammation and can be used to treat arthritis. 
B)  reduces stomach acid production and can be used to treat ulcers. 
C)  reduces blood cholesterol and can be used to treat atherosclerosis. 
D)  increases the concentration of cGMP and can be used to treat erectile dysfunction. 
E)  increases dopamine and can be used to treat schizophrenia.

Question 12

What type of reaction is typically catalyzed by liver cytochrome P450?

Accepted Answer

A)  reduction 
B)  hydration 
C)  hydroxylation 
D)  hydrolysis 
E)  esterification 
A)  reduction 
B)  hydration 
C)  hydroxylation 
D)  hydrolysis 
E)  esterification

Question 13

Which of the following is a powerful animal model used for drug development?

Accepted Answer

A)  fruit fly models with specific genes "knocked out" 
B)  bovine models with specific genes "knocked out" 
C)  E. coli models with specific plasmids added 
D)  mouse strains with specific genes "knocked out" 
E)  None of the answers is correct. 
A)  fruit fly models with specific genes "knocked out" 
B)  bovine models with specific genes "knocked out" 
C)  E. coli models with specific plasmids added 
D)  mouse strains with specific genes "knocked out" 
E)  None of the answers is correct.

Question 14

Kd corresponds to the concentration of ligand,at which ______________ (fraction?)of the receptors are bound to ligand.

Accepted Answer

Question 15

Some bacteria are resistant to penicillin because they contain __________________ enzymes.

Accepted Answer

The answer of Some bacteria are resistant to penicillin because...

Question 16

Which of the following class of drugs is a common treatment for hypertension?

Accepted Answer

A)  beta blocker 
B)  statins 
C)  protease inhibitors 
D)  phosphodiesterase inhibitors 
E)  None of the answers is correct. 
A)  beta blocker 
B)  statins 
C)  protease inhibitors 
D)  phosphodiesterase inhibitors 
E)  None of the answers is correct.

Question 17

How is genomic information used to develop new drugs?

Accepted Answer

Genes for related target proteins can be

Question 18

Elevated doses of acetaminophen are toxic because an oxidized metabolite reacts with and depletes which of the following compounds that normally protects the liver and other vital organs?

Accepted Answer

A)  glutathione 
B)  cGMP 
C)  plasma albumin 
D)  vyclooxygenase I 
E)  cytochrome P450 
A)  glutathione 
B)  cGMP 
C)  plasma albumin 
D)  vyclooxygenase I 
E)  cytochrome P450

Question 19

Which of the following enzymes is associated with the inflammatory response?

Accepted Answer

A)  phosphodiesterase 5 
B)  HMG-CoA reductase 
C)  $\beta$-lactamase 
D)  cyclooxygenase 2 
E)  None of the answers is correct. 
A)  phosphodiesterase 5 
B)  HMG-CoA reductase 
C)  $\beta$-lactamase 
D)  cyclooxygenase 2 
E)  None of the answers is correct.

Question 20

Thiopurines such as 6-thioguanine are used to treat immune disorders and leukemia.Some individuals who are treated show signs of toxicity at doses well tolerated by most patients.Explain the reason for this toxicity.

Accepted Answer

These differences are due to rare variat

Exam 36: Drug Development

Thiopurine drugs,such as 6-thioguanine,are toxic to some individuals because they have a genetic variation of the enzyme _________________________.

Briefly explain why a drug candidate that has a partition coefficient (log P)greater than 5 is not a good candidate for oral bioavailability.

Drug candidateIC50(nmol)Log (P)Cmax (µM)BioavailabilityA0.44.67<0.1B0.013.70<0.1C0.33.690.7D0.62.9211Consider the information concerning a related class of potential drugs in the table above.Which one is least soluble in water and most hydrophobic?

)What type of bond is used to link a glucuronic acid group to a xenobiotic?

What compound is increased by the action of Sildenafil (Viagra)?

________________ is the science that deals with the discovery,chemistry,composition,identification,biological and physiological effects,uses,and manufacture of drugs.

Give three types of conjugation reactions that occur in the metabolism of xenobiotics.

First attempts to develop cholesterol-lowering drugs targeted the later steps in cholesterol biosynthesis.Why did this strategy have to be abandoned?

Successful drugs have been discovered by which of the following methods?

Describe what factors will affect the apparent Kd of a drug under physiological conditions.

A compound that inhibits HMG-CoA reductase has potential use as a drug that

What type of reaction is typically catalyzed by liver cytochrome P450?

Which of the following is a powerful animal model used for drug development?

Kd corresponds to the concentration of ligand,at which ______________ (fraction?)of the receptors are bound to ligand.

Some bacteria are resistant to penicillin because they contain __________________ enzymes.

Which of the following class of drugs is a common treatment for hypertension?

How is genomic information used to develop new drugs?

Elevated doses of acetaminophen are toxic because an oxidized metabolite reacts with and depletes which of the following compounds that normally protects the liver and other vital organs?

Which of the following enzymes is associated with the inflammatory response?

Thiopurines such as 6-thioguanine are used to treat immune disorders and leukemia.Some individuals who are treated show signs of toxicity at doses well tolerated by most patients.Explain the reason for this toxicity.

Biochemistry: An Evolving Science

Protein Composition and Structure

Exploring Proteins and Proteomes

DNA, RNA, and the Flow of Genetic Information

Exploring Genes and Genomes

Exploring Evolution and Bioinformatics

Hemoglobin: a Portrait of a Protein in Action

Enzymes: Basic Concepts and Kinetics

Catalytic Strategies

Regulatory Strategies

Carbohydrates

Lipids and Cell Membranes

Membrane Channels and Pumps

Signal-Transduction Pathways

Metabolism: Basic Concepts and Design

Glycolysis and Gluconeogenesis

The Citric Acid Cycle

Oxidative Phosphorylation

The Light Reactions of Photosynthesis

The Calvin Cycle and the Pentose Phosphate Pathway

Glycogen Metabolism

Fatty Acid Metabolism

Protein Turnover and Amino Acid Catabolism

The Biosynthesis of Amino Acids

Nucleotide Biosynthesis

Biosynthesis of Membrane Lipids and Steroids

The Integration of Metabolism

DNA Replication, repair, and Recombination

RNA Synthesis and Processing

Protein Synthesis

The Control of Gene Expression in Prokaryotes

The Control of Gene Expression in Eukaryotes

Sensory Systems

The Immune System

Molecular Motors

Filters

Drug candidateIC₅₀(nmol)Log (P)C_max (µM)BioavailabilityA0.44.67<0.1B0.013.70<0.1C0.33.690.7D0.62.9211Consider the information concerning a related class of potential drugs in the table above.Which one is least soluble in water and most hydrophobic?

Describe what factors will affect the apparent K_d of a drug under physiological conditions.

K_d corresponds to the concentration of ligand,at which ______________ (fraction?)of the receptors are bound to ligand.