Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Drug Action > Exam 1 > Flashcards

Exam 1 Flashcards

1
Q

What is a drug

A

An exogenous substance which has a physiological effect when introduced into the body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is pharmacology

A

The branch of medicine concerned with the uses,

effects, and modes of action of drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is pharmacokinetics

A

The study of how drug concentration varies with time
after administration, and how long and where it persists
in the body over time.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Pharmacokinetic parameters are affected by what four processes

A

Absorption
Distribution
Metabolism
Excretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is pharmacodynamics

A

The study of the relationship between drug concentration
in the body and the response of the body to that
concentration of drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Fundamental unit of life

A

Cell

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is the most common type of drug target

A

Receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is the importance of a cellular response

A

Affects the physiology and health of the individual

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Four major types of receptors

A

Ligand gated ion channels
G protein receptors
Receptor tyrosine kinases
Nuclear receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What non-receptor macromolecules can also be drug targets

A 
Nucleic acids
Structural proteins
Enzymes
Ion channels
Cytokines
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Drugs are categorized into families based on what three things

A
  • Structural characteristics of ligand or target
  • Signaling pathways affected by ligand engagement
  • Level of organization targeted by the drug (ex. molecule, organelle, cell, tissue)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is a structure activity relationship (SAR)

A

the relationship
between the chemical or 3D structure of a molecule and
its biological activity.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

How would you change the “structure” of a drug to alter

its interaction with a target?

A

Modification of covalent bonds and atomic composition
of a drug can alter its ability to participate in non-covalent
interactions with its target.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What are the four important non-covalent interactions between drug and target

A

– Number of H-bond donors or acceptors
– Number and type of charge
– Hydrophobicity
– Polar bonds

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What are some different types of “activities” that are

affected by the chemical structure of a drug?

A

-Target potency
-Target selectivity
-Modifications to reduce toxicity
-Scaffold hopping to allow patentability
-Physical properties and formulation
-Modifications for bioavailability
Modifications to modulate metabolism
-Receptor drug interactions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Define principle

A

a fundamental truth or proposition that serves as
the foundation for a system of belief or behavior or for a chain
of reasoning

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What is the central dogma?

A

DNA –transcription–> RNA –translation–> Protein

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What are the three building blocks of DNA

A

Sugar: Deoxyribose
Phosphate
Bases (Adenine, Guanine, Thymine, Cytosine)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What is the structural difference between deoxyribose and ribose sugar

A

Deoxyribose: 2’ carbon has H
Ribose: 2’ carbon has OH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Which nucleotide bases are purines

A

Adenine and guanine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Which nucleotide bases are pyrimidines

A

Thymine and cytosine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What is a nucleobase

A

a nitrogenous heterocycle

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What is the importance of nucleobases

A

The endocyclic nitrogens
are basic and can function
as hydrogen bond
acceptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What is the difference between nucleosides and nucleotides

A

Nucleosides only contain sugar and base, they lack phosphate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Nucleotides exist in what state

A

In equilibrium between various phosphorylated forms

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

What enzymes add phosphate groups

A

Kinases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

What enzymes remove phosphate groups

A

Phosphatases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Why are di- and triphosphate analogs involved in energy, metabolism, and cell signaling?

A

Phosphoanhydride bonds are very high energy and cyclization makes them key second messengers

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

What is the name of the important bonds in single stranded DNA

A

phosphodiester bonds

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Single stranded DNA runs in which direction

A

5’–> 3’

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

What is a polymer of nucleotides

A

DNA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

What causes the antiparallel nature of each DNA strand?

A

Directionality of phosphodiester linkages

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

What forms between nucleotide base pairs

A

Dimers (H-bonding)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

What happens if drug binding disrupts H bonding in DNA structure

A

Alters replication and transcription

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

What phase of the cell cycle is characterized by pre-DNA synthesis?

A

G1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

What phases of the cell cycle are encompassed under “Interphase”

A

G1 + S + G2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

What part of the cell cycle does DNA synthesis occur?

A

S

38
Q

What part of the cell cycle does post-DNA synthesis occur?

A

G2

39
Q

List the cell cycle phases from longest lasting to shortest

A

G1>S>G2>M

40
Q

What is the importance of major and minor grooves in DNA

A

Allow for interactions with proteins such as transcription factors

41
Q

Describe the helix-turn-helix motif

A
  • Found in transcription factors
  • 1st helix stabilizes interaction with DNA
  • 2nd helix often called “recognition helix” because it interacts with base pairs in the major groove
42
Q

Describe the zinc finger motif

A
  • Found in transcription factors
  • Arg 46 and His 49 form sequence (specific contacts)
  • 3 nonspecific contacts between PO4 groups and side chains
43
Q

What are the three steps of transcription

A

Initiation
Elongation
Termination

44
Q

What is mRNA

A

single stranded messenger RNA that serves as the template for protein biosynthesis

45
Q

True or false: mRNA has secondary structure

A

True

46
Q

What is tRNA

A

Transfer RNA transfers amino acids during protein synthesis. Matches anticodon to codon on mRNA

47
Q

tRNA forms what type of bond with amino acids?

A

Ester bond

48
Q

What are ribosomes composed of

A

rRNA and protein

49
Q

What is the site of protein synthesis

A

Ribosome

50
Q

What are the two ribosomal subunits found in prokaryotes

A

30S/50S

51
Q

What are the two ribosomal subunits found in eukaryotes

A

40S/60S

52
Q

Do eukaryotes or prokaryotes have a larger ribosome

A

Eukaryotes

53
Q

What are two examples of cancer drugs that form a covalent bond with DNA

A 
nitrogen mustards (melphalan) 
Platinum complexes (cisplatin)
54
Q

Melphalan and Cisplatin are alkylating agents that typically attack what specific nitrogenous base (at what site too)

A

N7 of guanine that is exposed in the major groove

55
Q

Why is alkylation important in cancer drugs

A

Alkylation adds on alkyl adducts to DNA, which prevent replication and leads to cell cycle arrest or cell death. Interrupts normal functions of enzymes involved in DNA replication

56
Q

What non-covalent forces contribute to DNA-drug binding

A

Van der Waals
H bonding
Electrostatic/ionic
Hydration/dehydration of binding site

57
Q

Intercalators like doxorubicin use what non-covalent force to intercalate between base pairs?

A

Van der Waals

58
Q

Minor groove binders like distamycin use what non-covalent force to bind adenine and thymine rich regions?

A

H bonding and hydrophobic interactions

59
Q

What dual binding molecule intercalates and binds to minor groove to cleave one or both DNA strands?

A

Dynemicin A

60
Q

What are nucleic acid analogs

A

Substrates or inhibitors of various enzymes that metabolize normal nucleic acids

61
Q

What must be done to nucleoside analogs to affect DNA and RNA synthesis

A

Converted to active forms as triphosphates

62
Q

Chemical modifications can be made to functional groups at various parts of the nucleotide, what can be done to the base?

A

Halogenation

63
Q

Chemical modifications can be made to functional groups at various parts of the nucleotide, what can be done to the sugar?

A

Hydroxylation/dehydroxylation

64
Q

Chemical modifications can be made to functional groups at various parts of the nucleotide, what can be done to the phosphate?

A

Protection by polar groups

65
Q

Retroviruses need to replicate their RNA. What enzyme do they use?

A

Reverse transcriptase

66
Q

What does the enzyme reverse transcriptase do?

A

Makes DNA from an RNA template

67
Q

Can reverse transcriptase be found in normal human cells?

A

No

68
Q

Zidovudine is an antiviral that acts as a reverse transcriptase inhibitor. How does this medication work?

A

Its sugar has been dehydroxylated and in place of the OH group on 3’ end it has an azido group. The azido group prevents DNA chain elongation. HOWEVER it can be phosphorylated on 5’ end for bioactivation

69
Q

Adefovir is an antiviral that acts as a reverse transcriptase inhibitor. How does this medication work?

A

The sugar ring is opened/eliminated, preventing DNA elongation during replication. The phosphate has been replaced with a phosphonate,
increasing stability

70
Q

Remdesivir is an antiviral. What characteristics help it to prevent DNA replication?

A

It is a prodrug with a 1’ cyano group and altered base

71
Q

How do anticancer agents work and why?

A

Cancer cells divide rapidly which required DNA synthesis. by blocking DNA synthesis, S phase of cell cycle is stopped.

72
Q

At what phase of the cell cycle do organelles and cytosolic components duplicate and centrosomes begin to replicate?

A

G1

73
Q

At what phase of cell cycle is DNA replicated?

A

S

74
Q

At what phase of cell cycle is cell growth continuing, enzymes and proteins are synthesized and centrosome replication is completed?

A

G2

75
Q

Fluorouracil is an anticancer agent. What characteristics help it treat cancers?

A

It is a pyrimidine analog. It is basically uracil that has undergone halogenation (addition of a fluorine)

76
Q

Fluorouracil (5-FU) can be converted into FdUMP, FdUTP, and FUTP. What does having multiple mechanisms of action do for this molecule?

A

It allows it to inhibit thmidylate synthase, causes DNA damage, and causes RNA damage respectively.

77
Q

Cytarabine is an anticancer agent. What characteristics help it to treat cancers?

A

It is a dehydroxylated isomer of cytidine. It causes DNA damage

78
Q

Gemcitabine is an anticancer agent. What characteristics help it to treat cancers?

A

It is an analog of cytidine formed by halogenation. Causes DNA damage

79
Q

What is a catalyst

A

A substance that increases the rate of a
chemical reaction, without itself being changed during
the reaction

80
Q

What is an enzyme

A

a protein that acts as a biological catalyst

81
Q

Describe lock and key model

A

The enzyme and substrate

fit together

82
Q

Describe conformation selection model

A

The conformation of the
enzyme varies, one
conformation recognizes
the substrate (ligand)

83
Q

Describe induced fit model

A

Binding the substrate
induces a change in the
enzyme

84
Q

Role of oxidoreductases

A

Catalyze oxidation/reduction

reactions; transfer of H and O atoms or electrons from one substance to another

85
Q

Role of transferases

A

Transfer of a functional group from one substance to another

86
Q

Role of hydrolases

A

Formation of two products from a

substrate by hydrolysis

87
Q

Role of lyases

A

Non-hydrolytic addition or removal of

groups from substrates

88
Q

Role of isomerases

A

Intramolecule rearrangement ie. isomerization

89
Q

Role of ligases

A

Join together two molecules

90
Q

DNA polymerases requires what cofactor?

A

Magnesium ions

Drug Action (1 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions