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Pathophysiology > Drug Discovery > Flashcards

Drug Discovery Flashcards

1
Q

What is the bulk of drug discovery?

A

preclinical and clinical studies

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2
Q

process of traditional drug discovery

A

target identification
target validation
lead identification
candidate optimization
preclinical

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3
Q

target identification involves

A

drug receptors

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4
Q

drug receptor

A

usually a protein
macromolecule component of a cell which a drug interacts to produce a response

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5
Q

challenges of drug discovery

A

proteome
large dynamic range

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6
Q

proteome involves

A

over 1 million proteins due to splice variants and post translational modifications

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7
Q

large dynamic range challenges

A

low abundance proteins
no amplification system

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8
Q

pharmaceutical proteomics

A

proteome approach to the interaction of drugs with biological systems

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9
Q

proteomics

A

study of protein properties on a large scale to obtain a goal, integrated view of disease processes, cellular processes and networks at the protein level

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10
Q

proteomes are

A

dynamic

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11
Q

why is proteomics important?

A

parallel analysis of multiple proteins
discovery of disease specific proteins

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12
Q

expression proteomics

A

quantitative expression of 1000s of proteins
2D gel/ image analysis central

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13
Q

approach to identify low abundant proteins

A

reduce complexity (purification)
enrichment (concentration)

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14
Q

specific proteins may be resident in

A

specific organelles

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15
Q

the conventional approach to separate out organelles

A

differential centrifugation - labor intensive

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16
Q

batch vs continuous

A

batch - have to make new batches, tedious

continuous - produce large amounts, don’t need to make batches

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17
Q

continuous flow - ultra centrifugation

A

material continues to be circulated
used in vaccine production
collect specific fractions along the way

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18
Q

experimental validation

A

organelle enrichment
proteomic profiling
protein identification

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19
Q

western blot steps

A

SDS polyacrylamide gel electro
protein blot on nitrocellulose
label with specific antibody
detect antibody and protein present

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20
Q

enrichment

A

fractions present can be used as a marker for organelles
can be used to isolate proteins

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21
Q

2D gel electrophoresis

A

charge (isoelectric point) and size (molecular weight)

can see a lot more proteins this way

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22
Q

when there is enrichment compared to no enrichment,

A

there are a lot more signals of proteins since enrichment can resolve lower abundant proteins
there is less noise from more abundant proteins

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23
Q

protein identification

A

2D gels –> digest and bioinformatics to identify

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24
Q

Post translational modified low abundance proteins

A

same aa sequence but different modifications

can be separated due to this

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25
Q

steps of discovery

A
  1. continuous flow centrifugation
  2. reduce complexity
  3. 2D gel
  4. mass spec
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26
Q

proteins typically function as

A

complexes

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27
Q

multi-protein complexes involved in

A

DNA replication
energy metabolism
signal transduction

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28
Q

___________ of protein-protein interactions occur in a cell

A

thousands

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29
Q

protein-protein interactions are essential to

A

most processes that take place in a living cell

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30
Q

protein-protein interactions occur because the interior of cells is

A

crowded

31
Q

what is common upon binding in protein-protein interactions?

A

conformational changes

32
Q

yeast two hybrid

A

insert bait gene protein alongside DNA for half of an activator protein
other half of the activator is inserted alongside DNA for random prey protein
yeast grows and protein interacts

33
Q

what signals a match in yeast two hybrid?

A

the cell turns blue when the two halves of the activator proteins meet

34
Q

whole genome two hybrid screens

A

construction of bait and target libraries covering entire proteome
automated screening for positives

35
Q

most proteins are involved in

A

many interactions

36
Q

protein microarrays

A

analysis of thousands of proteins at one time

37
Q

types of protein microarrays

A

antibody arrayed
proteins arrayed
peptides

38
Q

protein microarray process

A

high throughput analysis of proteins
proteins immobilized on glass chip
various probes are used

39
Q

examples of protein substrates

A

polyacrylamide or agarose gels
glass
nanowels

40
Q

protein attachment examples

A

diffusion
adsorption/absorption
covalent attachment
affinity

41
Q

protein interactions examples

A

antigen-antibody
protein-protein
aptamers
enzyme-substrate
receptor-ligand

42
Q

different _________________ must be used to study different interactions

A

capture molecules

43
Q

probes interact with

A

target proteins

44
Q

taxane

A

anticancer drug
protein-protein disruptor

45
Q

candidate targets goes after

A

transmembrane
cytoskeleton
nuclear receptors

46
Q

what type of drugs attack candidate targets?

A

anti cancer
anti infectives

47
Q

microfluidics

A

combinatory chemistry
comes up with new chemicals

48
Q

where are compounds discovered?

A

microfluidics
natural products
bog

49
Q

due to therapeutics, life expectancy has

A

increased up 60%

50
Q

drugs account for ________ of the 60% of increased life expectancy

A

40%

51
Q

challenges for drug discovery today?

A

higher costs
longer timeframes
declining productivity
generics and biosimilars
increased competition

52
Q

are clinical trials involved in the discovery process?

A

NO

they are involved in clinical development

53
Q

how long does it take to get 1 drug approved?

A

10-20 years

54
Q

how many drugs are screened in the time one gets approved?

A

over 10,000

55
Q

pharmaceuticals and medicines account for _______ of Pharma investments in R&D

A

12%

56
Q

are drugs costly?

A

NO!

only 10 cents per health care dollar

57
Q

where is drug discovery performed?

A

big Pharma
biotech companies

58
Q

biotech companies are

A

entrepreneurial

59
Q

who can found a biotech company?

A

an individuals or a small group of scientists

60
Q

how many biotech companies in the US?

A

300 out of 600 total

61
Q

biotechnology is responsible for

A

hundred of diagnostic tests (HIV/pregnancy), DNA fingerprinting, etc

62
Q

Big Pharma challenges

A

R&D spending growing faster than sales growth
new product discoveries lagging
need licensing from outside
blockbuster drugs off patent

63
Q

pharmacogenomics

A

study of how people respond differently to medications due to their genetic inheritance

64
Q

pharmacogenomics correlates ______________ to ________________

A

heritable genetic variation

drug response

65
Q

85% of the differences in patient responses to a drug are due to

A

genetic polymorphism

66
Q

drug responses are affected by

A

pharmacokinetics
pharmacodynamics
pharmacogenomics

67
Q

pharmacogenoics reduces

A

the risk of adverse events

68
Q

pharmacogenomics transforms a _______________ approach into a _____________________ approach

A

one size fits all

patient sub population

69
Q

pharmacogenomics improves _____________ and makes for more efficient, cost effective ________________

A

patient outcomes

drug development process

70
Q

two types of genetic mutations

A

single base mutation (SNPs)

insertion/deletion of one or more nucleotide (Tandem repeat or Insertion/deletion polymorphism)

71
Q

poor metabolizer phenotype

A

usual dose cleared slower, leads to more drug in the blood
stronger therapeutic effect

72
Q

normal metabolizer phenotype

A

usual dose cleared at the expected rate, normal blood levels
expected therapeutic effect

73
Q

ultra-rapid metabolizer phenotype

A

usual dose cleared quicker, less drug in the blood
less therapeutic effect

74
Q

AI has been helpful in

A

pharmaceutical design and drug discovery

Pathophysiology (17 decks)

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