Biological Signalling and Receptors - Drug Target L1 Flashcards
(21 cards)
Two types of intracellular signalling
Signalling by secreted molecules or signalling by plasma membrane bound molecules
Types of signalling by secreted molecules
Paracrine, endocrine, autocrine and synaptic
Paracrine
Molecules released Assad’s Albert Barnes to nearby cell receptors
endocrine
Hormones or other products are secreted directly into the blood to act on a distant tissue or organ
Synaptic
Similar to paracrine signalling molecule released outside cell however released into space called synapes molecule is neurotransmitter
What kind of ligand of the cell surface receptor have
Hydrophilic
What can a ligand is an intracellular receptor have
Hydrophobic as can past the hydrophobic bilayer. Issue that needs a carrier protein to transport it before it can pass bilayer
Receptor
Molecule that recognises the ligand and in response to ligand binding brings about regulation of the solar process.
An unbound state a receptor is functionally silent
Ligand
Any molecule binds specifically to receptor
Antagonist
Opposes the action of the agonist. Structuring the mix agonist blocks binding site
Agonist
At its receptor
What is the measure of the receptor binding affinity
Kd Kd low affinty
Classification of receptors
Classified according to agonist
sub classification affinity binds to antagonist
Four major class of receptors
Membrane-bound receptors with integral iron channels - e.g nicotinic acetlycholin receptors
Membrane-bound receptors of integral enzyme activity - e.g tyrosine kinase receptors (insulin)
Membrane-bound receptors which couple to effector through transducer and proteins - e.g G-protein coupled receptors
Intracellular receptors - e.g oestrogen
Nicotinic acetylcholine receptor strcuture
Gated pore, two alpha subunits bind Ach, Open Allowing Na+
Example of the tyrosine kinase receptor
Growth factor receptors, insulin , link directly to tyrosine kinase
Structure of tyrosine kinase insulin receptor
Dimer One polypeptide has a alpha and beta Sabina. Insulin binds an alpha domain, there is a transmembrane domain, and C terminal is a tyrosine kinase domain which allows the auto phosphorylation
G-protein coupled receptors structure
Seven transmembrane spanning, N-terminal outside cell where binding domain occurs and G-protein coupled domains inside of the C-terminal
GS subunit activates what
Adele cyclase which causes ATP to become cyclic AMP
Intracellular receptors namely three domains
Hormone binding domain, DNA binding domain and transcription activating domain
Noradrenaline binds beta one adrenoceptors causes what to heart
Acetylcholine Binds to M2 muscarinic receptor causes what
increased heart rate
slowing of heart rate