Dr. greigs slides Flashcards
1
Q
chance of success
A
- you have to defeat overwhelming odds to get to the 1 in 20 chance
2
Q
gartner’s hype cycle
A
- peak of inflated, trough of disillusionment, slope of enlightenment, plateau of productivity
3
Q
what does blocking or activating a receptor do
A
- salbutamol activated an adrenoceptor and treats asthma
- antihistamines like benadryl block histamine receptors and control hayffever symtoms
4
Q
what is a target
A
- can be an enzyme
- can be anything that is different about a disease state and a healthy state
5
Q
why does selectivity matter
A
- when developing or repurposing drugs against a specific disease target, while guaranteeing that the drug should not have strong off-target activities toward other proteins which may lead to unwanted side effects
6
Q
what we can(not) do in 2020
A
7
Q
why cant we do this
A
- because most drugs are too small
8
Q
some targets are easier than others
A
- drugs that make strong binding interactions with a target may affect only this target and thus not cause toxicity by hitting other targets
- drug makes only weak binding interactions with target. Probably won’t affect target, but likely to bind to other targets and cause toxicity
9
Q
what is druggability
A
- drug must disolve in stomach
- drug mush be abdorbed from gut
- drug must survive the liver and the body’s attempts to destroy it
- drug must not affect other parts of the body
enough of the drug must reach the brain and get through the protective barrier around the brain - drug must now bind to target
10
Q
why is drug discovery so difficult
A
- polar drugs dissolve in stomach/gut (solubility)
- lipophilic drugs better absorbed from the gut (permeability)
- polar drugs, less likely to be metabolized in the liver
- lipophilic drugs are able to pass the blood brain barrier
- polar drugs less likely to hit other drug
- lipophilic drugs are less likely to be cleared by the kidneys
11
Q
what does a druggable target need
A
- mixture of lipophilic and polar residues in order for us to develop a drug that will be able to reach it
12
Q
1900-200 drug discovery is primarily evolutionary
A
- develop new drugs from what we already have
- develop new drugs from what we already know
- get lucky
- talented people free from corporate interference
- many diseases with no treatments
13
Q
natural sources
A
- the importance of natural products can be argued either way
- nature is extremely good at suggesting starting points for a study and identifying lead compounds which may then be developed, if over a period of many years to give a highly potent new drug
14
Q
what is a target
A
- receptor (blocking or activating)
- enzyme
- anything that is different about a disease state and a healthy state
15
Q
why does selectivity matter
A
- would activate all
- ex adrenaline
