Drug Receptors (Chapter 2) Flashcards
What is a receptor made of?
Protein
Regulatory proteins, Enzymes, Transport proteins, Structural proteins
Orphan Receptor
Receptor without a native ligand. (we don’t know what it is)
Category of receptors by molecular structure: (there are 7)
Seven-transmembrane receptors (7TM) Ligand-gated channels Ion channels Catalytic receptors Nuclear receptors Transporters Enzymes
About 50% or more of the drugs we give interact with what kind of receptor?
Seven-transmembrane receptors (7TM)
Most common 7TM receptor?
GPCRs
Ligand-gated channels
A receptor that opens when a certain ligand binds to them, then close when the ligand leaves (example: acetylcholine receptors)
Ion channels
Open and close independent to a ligand binding to them. As membrane potential changes these will open and close.
Catalytic receptors
Receptors that produce and enzymatic response inside the cell
Nuclear receptors
Inside the nucleus. Drug may diffuse through membrane to receptor on nucleus or drug binds to receptor on surface and causes a downstream effect that will active the nuclear receptors
Transporters
Don’t necessarily elicit a response, more for transporting drugs across barriers
Enzymes
Receptors that can either be blocked by a drug or activity can be increased
Lag period
Due to transcription and translation
Can take 30min to several hours to days
Persistence
How long the drug effect will last.
Depends on how long the receptor takes to degrade.
Can remain for hours to days
In a phosphorylation cascade, if a protein acquires phosphate from ATP, it is called..
a Kinase.
How are kinase and phosphorylase different from phosphatase?
Kinase and phosphorylase give protein a phosphate.
Phosphatase strips protein of a phosphate.
