Modern and Future Drug Discovery Flashcards
What is Gartner’s Hype Cycle?
explains the extreme levels of hype associated with drug discover
- Peak of inflated expectations
- trough of disillusion
- slope of enlightenment
- plateau of productivity
What are chemputers?
modular desktop-sized robotic synthesizers
What is a receptor target?
it can either block or activate a receptor which may have a therapeutic effect
What does Salbutamol do?
activates an adrenoceptor and treats asthma
What do antihistamines do?
Benadryl blocks histamine receptors and controls hayfever symptoms
What is an enzyme target>
it can either block or activate an enzyme which may have a therapeutic effect
How do Asprin, statins, and penicillin work?
Asprin (headaches)
Statins (lower cholesterol)
Penicillin (infection)
by blocking enzymes
Why does selectivity matter with asthma medication?
selective activator of the beta 2 adrenoceptors helps regulate asthma
Non-selective activation of all adrenoceptors would result in fight or flight
What can and cannot be done with drug targets?
Can: block messengers from binding to its target
Cannot: block a protein from binding to another protein or proteins from being to DNA
Why can’t proteins be blocked from binding to other proteins or DNA?
can’t make something that looks like the surface of DNA or proteins
Why are some drugs declared “undruggable”?
the drug makes only weak binding interactions with the target. Probably won’t affect the target and is likely to bind to other targets and cause toxicity
What are the characteristics of a drug being drugable?
- Dissolve in the stomach
- absorbed by the gut
- survive the liver and the body’s attempts to destroy it
- must not affect other parts of the body
- enough to reach the brain and get through its protective barrier
- must bind to target
Where can polar drugs dissolve?
stomach/ gut
What kind of drugs are better absorbed from the gut?
lipophilic drugs
What kind of drug is less likely to be metabolized in the liver?
polar drugs
