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Drug Discovery And Development Flashcards

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1
Q

What occured in the rinderpest cattle 1709

A

Major outbreak in Western Europe
Wiped out most of the cows at that time

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2
Q

What is rinderpest

A

Major viral disease
Causes fever, anorexia and eye discharge

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3
Q

What happened in the anthrax outbreak 1712

A

Killed cattle quickly
Fatal bacterial disease
Humans can et the disease

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4
Q

Is anthrax used as a biological warfare agent

A

Yes

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5
Q

What happpend in the 1715 foot and mouth disease outbreak

A

Contagious viral disease
Blisters, fever in cloven hoofed animals

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6
Q

What is the one health initiative

A

Recognises the inter-relationship between animal health, human heath and environment health

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7
Q

Wh was the one health initiative made

A

This because they all link together. If environment is affected it effects humans animals as we eat animals

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8
Q

Where did drugs originally come from

A

Herbs and potions

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9
Q

What did scientists do in the 19th century

A

Isolate and identify the biological activity components from herbs and plants

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10
Q

What is the 1st step to drug discovery

A

Identification of a disease where there is a need for a new drug

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11
Q

What are economical factors pharcuetical companies face when making a new drug

A

Developing a drug is complex - takes 10 to 15 years
Costs over 100 million pounds
Make sure there is good financial return for their investment

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12
Q

What is the problem in the western world when it comes to making new drugs

A

They aren’t as rich therefore drugs for new diseases do not get created unless the rich areas take notice and create the drug

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13
Q

What is the issue with drug making and the veterinary world

A

Not a lot of money in veterinary mediciene compared to human mediciene

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14
Q

What are the approaches o drug discovery

A

Bo-assay based
Target based

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15
Q

What is bio-assay based drug discovery?

A

Develop compounds to use against the disease to see if they’re active at killing the biological compound.

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16
Q

What is target based drug discovery

A

Identify the disease and then the target - receptor, enzyme etc
It synthesized agonists, antagonist or inhibitors against the except or/enzyme of the disease

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17
Q

What is the bioassay-based drug discovery method

A

Raw material - crude extract
Extract compounds using solvents
Test crude extract on bioassay to see if the crude extract shows potency and biological activity
Biologically evaluate the compounds showing biological activity using mass spectrometry
Medicinal chemiss then modify the compounds to make a more potent and selective drug
Clinical trials - if new drug gets through clinical trials it can then be licensed and marketed

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18
Q

What is the right bioassay for bioassay drug discovery?

A

Need to choose right bioassay - important to success to drug research programme
Needs to be quick and simple cant test compounds
Tests should be done on enzymes, tissues and isolated cells
Suitable biological assay - antimicrobial assay

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19
Q

What is artemisinin

A

Traditional Chinese medicene
Herbal plant

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20
Q

What is artemisinin effective against?

A

It was active against the strain of malaria that north Vietnam where facing in 1972

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21
Q

What is cephalosporins

A

Derived from a fungus found in sees in Sardinia
Looked at water and noticed that there was a clearing of turbid water
This then created the antibiotic cephalosporin

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22
Q

What created the drug hypertension

A

Venom from jaraca

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23
Q

What drug comes from teprotide venom

A

Captopril

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24
Q

What are chemical extractions

A

Extract compounds from material

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25
What do you do in chemical extractions
Take plant and grind it in the solvent and look at the components in the solution you can use more than one solved to measure polarities in the plant
26
What is semi-purification
Removal of sugars and amino acids
27
Why do you remove sugars and amino acids from plants
We need to know if something is working due to the components of the plant and not the sugars in the plant
28
What happens during screening for biological activity
Once biological activation occurs you purify that compound more and separate into fractions and look at each fraction to see which one shows biological actity
29
What is purification
Separation and purification of individual compounds from the extract, screening for biological activity and purify using chromatography
30
What chromatography do you use if compounds are non polar
Normal phase chromatography
31
What chromatography do you use if compounds are polar
C18 reverse phase chromatography
32
What is preclinical testing
Biological evaluation in vitro and in vivo - identification of mode of action Individual purified compounds can be tested in vitro assay and in vivo assays to identify the active components
33
What is high performance liquid chromatography
Giveees molecular weight and forums Compound can be broken into fragments that can build up to make the molecule Sensitive method - you can use nano-grams of the particle Doesn’t tell you the carbon/hydrogen frame work
34
What is nuclear magnetic resonance spectroscopy
Gives the carbon framework of molecular and environment of the hydrogens Gives information on the shape of the molecule Information on how the compound binds to its target Need 1 milligram for it to work
35
What is proto NMR
Tells us the environments of the hydrogens in the molecule Usually locate double bonded hydrogens
36
What is cosy NMR
Find out which hydrogens are held by 3 bonds
37
What is NOESY nmr
Look up at hydrogens close up in space to other hydrogens - gives shape of molecule
38
What is HSQC NMR -
tells us which hydrogen is bonded to which carbon
39
What is HMBC NMR
Tells u what hydrogen is connected to carbon through 2-3 bonds
40
What is SARS
Structure acitvity relationships
41
What does SARS do
Identify which parts of the molecule are important for activity
42
How do you identify which parts of the molecule are important for activity in SARS
Changing each functional group of the molecule and investigate how it affects the way the molecule acts.
43
What drug do we aim for
A drug with god selectivity and no side effects Or little to no side effects
44
What do they look at in clinical trials
Drug absorption Distribution Metabolism Excretion Efficacy Dosage Toxicity
45
What are the process of drugs in the body
Drug is administered Drug is absorbed Drug is now in systemic circulation Drug gets distributed to tissues or he site of action Drug is metabolised or excreted Drug site of action creates a pharmological effect which creates a clinical response which can be efficacy
46
What is pharmokinetics
Where drugs go and what happens to it
47
What are pharmacodynamics
What does the drug do we it reaches the site of action
48
What is an effective dose
Dose or amount of drug that produces a therapeutic response
49
What is efficacy
Ability of the drug to elicit a response when it binds to the receptor
50
What does veterinary medicenes need
A marketing authorisation
51
What animal medicines not need a MA
Medicenes for small animals used as pets Aquarium animals
52
What drugs need a MA
Antibiotics Psychotics
53
What medicines with a MA need
A MA number Should carry the symbol vm on packaging and printed material
54
What are the advantages of natural products
Novel structures - novel molecules
55
Disadvantages of using natural products
Impossible to synthesize certain materials Some atrial moprducts are available in small amounts Takes years to synthesize drugs
56
Example of drug that takes years to synthesize
Palitaxal - taken from bark of taxis brevoila - non renewable as tree got chopped down They now use needles of the tree but takes 10 years to synthesize
57
What is the top down method
Candidate drugs screened for effect on phenotype
58
What does the top down method screen
Whole animals, organs or cells
59
What are the advantages of top down
Directly reliant to the disease if we have a good animal/experiemntal model of the disease
60
What is top down screening based on?
Screening for phenotypic changes relevant to treatment of disease
61
Why is top down method called top down?
Your testing at the most complex level and dining out what the biochemical target is
62
Disadvantages of top down methods
Very low throughout and cant test many compounds
63
What is the bottom up method
Candidate drugs tested for effect on biomechanical target molecule
64
What targets do bottom up test on
Receptors, enzymes dna
65
What is bottom up based on
Screeening of libraries or structure based design
66
What is the early essential step of bottom up procedures
Identification and validation of biomechanical target - protein dna -
67
What are the advantages of bottom up
Know the target Get the structure of target If you have structure - structure based design can be done
68
Disadvantages of bottom up
Although you find a target you dont know if it is valid or not
69
What is target identification and validation - bottom -up
Coming up with a good target to identify Validation - making sure it is the right target
70
What is hit generation - bottom - up
When you evaluate hit compounds more and test various parameters
71
Bottom up process or target based drug discovery
Target identification and validation Hit generation Lead discovery and de novo synthesis Lead optimisation Preclinical tests Clinical trials Licensing and marketing
72
What is lead optimisation - bottom uo
Look at strucutre acitvity relationships and improve reactivity of the drug to make it more potent and selective
73
What does validation of target ensure
That if the drug binds to the target, the desired phenotypic change is achieved
74
What is the first step in drig discovery
Identify the target and validate it as its essential for target based bottom up drig discovery
75
What is a target in drug doscbery
A molecule in the body which is usually a protein which is associated to a particular disease pathway, or modified and could be addressed if we get the drug bound to the target to treat the disease
76
What happens if you try to inhibit an enzyme
If you inhibit a whole enzyme there are chances you can inhibit every pathway the enzyme is associated too which leads to on target toxicity
77
What is the method used before we test the design of a new drug
Identification Assessment Validation
78
What is identification
Understanding where the drug comes from and how it works Biochemical pathways Signalling pathways
79
What is assessment
Assess the target Need to assess certain things before making the drug Drug ability - success rate? Can we get a drg to bind to the target selectivity
80
What is validation
Making sure if we binge a drug to the target we actually get the outcome we want Proving that all the steps done before this process will give us the outcome needed
81
What is knock-down.knock-out/Sirna
Ways to validate drugs - reduce amount of target proteins in the cells
82
What is knock-in/over expression
Add more copies of the gene for the protien target, does the disease get worse
83
What is drugabilit
Will it be possible to design a drug to bind to a target Is structure available Is it crystal or NMR Where is the binding site
84
Why are broad fat eaturls - hydrophobic - sites not good
Drug cant bind to the compound
85
What do you have to think about when it comes to selectivity
Is binding site exclusive to this enzyme That al the kinases bind atp These two issues cause selectivity to be really hard
86
What is on-target selectivity
Toxicity resulting from the drug binding to the intended protein target Unintended consequence - down regulation of the target n the cell
87
What is off target toxicity
Toxicity resulting from the drug binding to other protein targets in the cell Can be addressed by design of drugs which are more selective for the target protein
88
Why do we need to sign dual set inhibitors and extend outside the active site
Use strucutre of biochemical to build inhibitor molecule to recognise the features of inside and outside section of the active site to create more potency and selectivity
89
What are the drug targets of bacterial cells
Enzymes DNA/rna Ribosomes Cell walls Polymyxins
90
Once we have a validated target what’s next
Identify hit compounds which bind to the target as inhibitors, agonists, or antagonist through target screening
91
Why do you need to design compounds using the strucutre of the target
Drug needs to fill up the space of the active site otherwise it will be ineffective You can do this with computer models and make 3D strucutres of the target protein and the drug

Veterinary Pharmacology (12 decks)

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