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