Chapter 5/Cell Signaling in Physiology Flashcards
Chemical messengers bind to
receptor
Water-soluble messengers bind to receptors
located at the
plasma membrane
Lipid-soluble messengers bind to
intracellular
receptors
cells express different receptors
Specificity
strength of ligand-receptor binding
Affinity
Different cells can have different responses to same
ligand
Specificity: cells express different receptors.
High affinity will bind at lower concentrations of
messenger
Affinity: strength of ligand-receptor binding
the fraction of total binding sites
that are occupied
Saturation
presence of multiple ligands able
to bind the same binding site
Competition
blocks the action of a chemical
messenger
Antagonists
activates receptors and triggers the cell’s
response
Agonist
receptors are removed
(internalized) in response to intense exposure to chemical messengers.
Down-regulation
number of receptors is
increased in response to low concentrations of
chemical messengers
Up-regulation
Up-regulation & down-regulation
Receptor Regulation
Can diffuse through the plasma membrane.
– Have intracellular receptors.
– Signal-receptor complexes bind directly to DNA
and alter gene expression.
– Slower response, but sustained response
Lipid-soluble messengers
A broad range of receptors.
– Activate intracellular signaling cascades
– Can activate mediators that affect DNA
expression
– Faster response but less sustained.
– Involve first messengers and second messengers
Membrane-bound receptors
Lipid-soluble messengers,
Membrane-bound receptors
Signal Transduction Pathways
Activation of receptor results in open ion
channel.
* Opening of ligand gated ion channels increase
net diffusion of ions specific to channel.
* Often results in a change in the membrane
potential.
* Ex: Na+, K+, Ca2+
Ligand-Gated Ion Channels
Some receptors have intrinsic
enzyme activity
Most are protein kinases that phosphorylate
the amino acid tyrosine
Receptor tyrosine kinase
transferring a phosphate
group from ATP
Phosphorylation
Binding of messenger to
receptor activates
enzymatic portion of
receptor.
* This autophosphorylates
the receptor’s tyrosine
groups
* Docking proteins bind to
phosphorylated tyrosine
groups.
* Activate cell’s response
Events for receptors with tyrosine kinase activity
These receptors do not have intrinsic kinase activity
Cytoplasmic Kinases
Binding of ligand causes conformational
change in receptor that leads to activation of
JAK kinase