Lecture 4 Protien Signaling Flashcards
block sympathetic signalling to heart (mainly).
Beta-blockers compete with binding of noradrenaline and adrenaline to β1 adrenergic receptors:
antagonists
Beta-blockers are antagonists of the β1 adrenergic receptor
Adverse effects:
beta-blockers also have affinity for the β2 adrenergic receptor: can exacerbate asthma
Beta-blockers (-olol) are widely prescribed and may be used to treat:
angina
heart failure
fibrillation
heart attack
high blood pressure ‘
angina
chest pain caused by narrowing of the arteries supplying the heart
heart failure
failure of the heart to pump enough blood around the body
atrial fibrillation
irregular heartbeat
heart attack
an emergency where the blood supply to the heart is suddenly blocked
high blood pressure
– when other medicines have been tried, or in addition to other medicines
Adrenergic and muscarinic receptors:
Cell-surface receptors
Integral membrane proteins
Members of the largest group of receptors: G protein-coupled receptors (GPCRs)
Characteristic: seven trans-membrane -helices (7-TM)
Main targets of drugs
Enzymes
Ion channels
Transport proteins
Receptors:
Main targets of drugs
Enzymes
Ion channels
Transport proteins
Receptors:
Type of receptor
Ligand gated ion channels
E.g. nicotinic acetylcholine receptor
G protein-coupled receptors
Adrenergic and cholinergic receptors
Kinase-linked receptors
Nuclear receptors
What receptor do
A receptor recognises a specific signal leading to a response.
Adrenergic receptor: noradrenaline (adrenaline)
Cholinergic receptors: acetylcholine
Receptor
protein molecule that recognises a specific chemical signal from outside the cell.
e.g. β1 adrenergic receptor
