What is a receptor?
A macromolecular protein that recognises a ligand and transduces a signal into a cellular response
What two key properties must receptors have?
Recognition and transduction
What happens when a ligand binds a receptor?
It induces a conformational change that triggers signalling
Why are receptors saturable?
There are a finite number of receptors
What determines the strength of a receptor signal?
The proportion of receptors occupied by ligand
What is receptor up-regulation?
Increase in receptor number
What is receptor down-regulation?
Decrease in receptor number
What factors determine hormone-receptor complex formation?
Hormone concentration, receptor concentration, and affinity
What types of bonds are involved in ligand-receptor binding?
Non-covalent (hydrogen, electrostatic, hydrophobic, Van der Waals)
What is an agonist?
A drug that activates a receptor to produce a response
What is an antagonist?
A drug that blocks or reduces receptor activity
How do drugs affect signalling?
They can enhance, reduce, or block generation or transmission
Are most drug-receptor interactions reversible or irreversible?
Reversible
Why are irreversible interactions often undesirable?
They can cause toxicity, mutagenicity, or carcinogenicity
What are orthosteric drugs?
Drugs that bind to the same site as the natural ligand
What are allosteric drugs?
Drugs that bind to a different site and modify receptor activity