The billion dollar pill Flashcards
What are agonist drugs?
Drugs that stimulate biological responses
What are antagonist drugs?
Drugs that inhibit biological responses.
What are the 3 tenets of pharmaceutical science?
- All drugs must bind to a biological target in order to achieve a desired biological effect.
- Magnitude of the response depends on the dose.
- Every drug is a potential poison.
What are the general biological targets of a drug?
- Targets that are overexpressed.
- Targets that are underexpressed.
- Targets that control a critical process that affects the biology that you are trying to manipulate.
What is the largest class of drug targets?
Enzymes.
What are exogenous molecules?
Molecules originating from outside the organism
What is pharmacokinetics and pharmacodynamics?
pharmacokinetics: study of how the body affects the drug
Pharmacodynamics: study of how the drug affects the body
Where are HER2 receptors overexpressed?
on the cell surface of breast tumours
Why are enzymes the largest class of drug targets?
because of the presence of the active site, which can be exploited as binding sites for pharmaceutical enzyme inhibitors
How does potency relate to EC50?
higher potency = lower EC50
Why is higher potency of a drug sometimes bad?
the chance of the drug binding to other targets is higher, causing side effects
What are the 2 ways in which a drug can become a poison?
- Too much action on the target
- Loss of selectivity, where the drug binds to other targets
What is the first step in the process of drug discovery?
Identification and validation of a target.
What are the criteria for a good target?
- The target’s 3D structure is accessible
- Effects of altering the target is measurable
- It is not evenly distributed throughout the body
What are the criteria during target validation?
- Is the effect of the target reproducible?
- Can the target be modulated?
After identifying a target, how is the drug chosen?
Start with a endogenous molecule that is known to bind to the target and go from there
What is an endogenous molecule?
A molecule originating from inside the organism
What is a pharmacological assay?
An investigative procedure to measure the presence, amount or functional activity of a drug