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Pathophysiology > Drug Discovery (Exam 3) > Flashcards

Drug Discovery (Exam 3) Flashcards

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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
steps of discovery
1. continuous flow centrifugation 2. reduce complexity 3. 2D gel 4. mass spec
26
proteins typically function as
complexes
27
multi-protein complexes involved in
DNA replication energy metabolism signal transduction
28
___________ of protein-protein interactions occur in a cell
thousands
29
protein-protein interactions are essential to
most processes that take place in a living cell
30
protein-protein interactions occur because the interior of cells is
crowded
31
what is common upon binding in protein-protein interactions?
conformational changes
32
yeast two hybrid
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
what signals a match in yeast two hybrid?
the cell turns blue when the two halves of the activator proteins meet
34
whole genome two hybrid screens
construction of bait and target libraries covering entire proteome automated screening for positives
35
most proteins are involved in
many interactions
36
protein microarrays
analysis of thousands of proteins at one time
37
types of protein microarrays
antibody arrayed proteins arrayed peptides
38
protein microarray process
high throughput analysis of proteins proteins immobilized on glass chip various probes are used
39
examples of protein substrates
polyacrylamide or agarose gels glass nanowels
40
protein attachment examples
diffusion adsorption/absorption covalent attachment affinity
41
protein interactions examples
antigen-antibody protein-protein aptamers enzyme-substrate receptor-ligand
42
different _________________ must be used to study different interactions
capture molecules
43
probes interact with
target proteins
44
taxane
anticancer drug protein-protein disruptor
45
candidate targets goes after
transmembrane cytoskeleton nuclear receptors
46
what type of drugs attack candidate targets?
anti cancer anti infectives
47
microfluidics
combinatory chemistry comes up with new chemicals
48
where are compounds discovered?
microfluidics natural products bog
49
due to therapeutics, life expectancy has
increased up 60%
50
drugs account for ________ of the 60% of increased life expectancy
40%
51
challenges for drug discovery today?
higher costs longer timeframes declining productivity generics and biosimilars increased competition
52
are clinical trials involved in the discovery process?
NO they are involved in clinical development
53
how long does it take to get 1 drug approved?
10-20 years
54
how many drugs are screened in the time one gets approved?
over 10,000
55
pharmaceuticals and medicines account for _______ of Pharma investments in R&D
12%
56
are drugs costly?
NO! only 10 cents per health care dollar
57
where is drug discovery performed?
big Pharma biotech companies
58
biotech companies are
entrepreneurial
59
who can found a biotech company?
an individuals or a small group of scientists
60
how many biotech companies in the US?
300 out of 600 total
61
biotechnology is responsible for
hundred of diagnostic tests (HIV/pregnancy), DNA fingerprinting, etc
62
Big Pharma challenges
R&D spending growing faster than sales growth new product discoveries lagging need licensing from outside blockbuster drugs off patent
63
pharmacogenomics
study of how people respond differently to medications due to their genetic inheritance
64
pharmacogenomics correlates ______________ to ________________
heritable genetic variation drug response
65
85% of the differences in patient responses to a drug are due to
genetic polymorphism
66
drug responses are affected by
pharmacokinetics pharmacodynamics pharmacogenomics
67
pharmacogenoics reduces
the risk of adverse events
68
pharmacogenomics transforms a _______________ approach into a _____________________ approach
one size fits all patient sub population
69
pharmacogenomics improves _____________ and makes for more efficient, cost effective ________________
patient outcomes drug development process
70
two types of genetic mutations
single base mutation (SNPs) insertion/deletion of one or more nucleotide (Tandem repeat or Insertion/deletion polymorphism)
71
poor metabolizer phenotype
usual dose cleared slower, leads to more drug in the blood stronger therapeutic effect
72
normal metabolizer phenotype
usual dose cleared at the expected rate, normal blood levels expected therapeutic effect
73
ultra-rapid metabolizer phenotype
usual dose cleared quicker, less drug in the blood less therapeutic effect
74
AI has been helpful in
pharmaceutical design and drug discovery

Pathophysiology (18 decks)

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