Exam 2 Flashcards
What are receptors?
Chemical messengers bind to specific target-cell proteins
Where do most chemical messengers that are water-soluble bind to?
receptors located at the plasma membrane
Where do other chemical messengers, like steroids, that are lipid-soluble bind to?
An intracellular receptor
What does the N-terminal domain participate in?
gene activation
What does the DNA-binding domain determine?
which segments of DNA are bound by different receptors
What is the hinge domain required for?
Nuclear receptors to localize in the cell nucleus
What does the ligand-binding domain determine?
Which messenger binds to a given receptor
Specificity
The ability of a receptor to bind only one type or a limited number of structurally related types of chemical messengers. Only cells that express the correct receptor can bind a particular messenger.
Saturation
The degree to which receptors are occupied by messengers. If all are occupied, the receptors are fully saturated; if half are occupied, the saturation is 50%, and so on.
Affinity
The strength with which a chemical messenger binds to its receptor.
Competition
The ability of different molecules to compete with a ligand for binding to its receptor. Competitors generally are similar in structure to the natural ligand.
Antagonist
A molecule that competes with a ligand for binding to its receptor but does not activate signaling normally associated with the natural ligand. Therefore, an antagonist prevents the actions of the natural ligand. Certain types of antihistamines are examples of antagonists.
Agonist
A chemical messenger that binds to a receptor and triggers the cell’s response; often refers to a drug that mimics a normal messenger’s action. Some decongestants are examples of agonists.
Down-regulation
A decrease in the total number of target-cell receptors for a given messenger; may occur in response to chronic high extracellular concentration of the messenger.
Up-regulation
An increase in the total number of target-cell receptors for a given messenger; may occur in response to a chronic low extracellular concentration of the messenger.
Increased sensitivity
The increased responsiveness of a target cell to a given messenger; may result from up-regulation of receptors.
Can lipid messengers diffuse through the plasma membrane?
yes
Where do the signal receptor complexes in lipid soluble messengers bind?
directly to recognized sequences in the DNA and alter gene transcription
What does activation of the receptor by a first messenger (ligand) result in?
a conformational change of the receptor so it forms an open channel through the plasma membrane.
What does the opening of ligand-gated ion channels in response to binding of a first messenger result in?
an increase in the net diffusion across the plasma membrane of one or more types of ions specific to that channel.
What is the sequence of protein kinases?
- messenger binds to the receptor
- changes the conformation of the receptor
- enzymatic portion on the cytoplasmic side of the plasma membrane becomes activated.
autophosphorylation of the receptor
the receptor phosphorylates some of its own tyrosine residues
what does the cytoplasmic portion of the receptor serve as?
docking sites for cytoplasmic proteins
What do docking proteins do?
bind and activate other proteins which in turn activates one or more signaling pathways within the cell.
What is the common denominator for enzyme pathways?
they all involve activation of cytoplasmic proteins by phosphorylation.
What does a guanylyl cyclase catalyze the formation of?
a molecule known as cyclic GMP (cGMP) in the cytoplasm
What does cyclic GMP (cGMP) function as
a second messenger to activate a protein kinase called cGMP-dependent protein kinase.
what does cGMP-dependent protein kinase do?
phosphorylates specific proteins that then mediate the cell’s response to the original messenger.
Where are Receptors that function both as ligand-binding molecules and as guanylyl cyclases abundantly expressed?
in the retina of the eye where they are important for processing visual inputs
what are janus kinases (JAKs) associated with?
the receptor
G proteins
Bound to the inactive receptor; located on the cytosolic surface of the plasma membrane
What are the the three subunits of g proteins?
alpha, beta, and gamma
What does the alpha subunit of g proteins bind?
GDP and GTP
What do the beta and gamma subunits of g proteins do?
help anchor the alpha subunit in the membrane
What does the binding of a first messenger to the receptor do?
changes the conformation of the receptor
What does the activated receptor do for GTP?
increases the affinity of the alpha subunit of the G protein for GTP
What happens to the alpha subunit of g proteins when it is bound to GTP?
it dissociates from the beta and gamma subunits of the trimeric G protein
What does the dissociation of the alpha subunit from the beta and gamma subunits allow?
the activated alpha subunit to link up with still another plasma membrane protein, either an ion channel or an enzyme.
What does a G protein serve as?
a switch to couple a G-protein-coupled receptor to an ion channel or to an enzyme in the plasma membrane
What two functions can G proteins have?
either stimulate (Gs) or inhibit (Gi) some aspect of cell function.
What does activation of the receptor by the binding of the first messenger allow?
the receptor to activate its associated G protein
What is the Gs effector protein?
adenylyn cyclase
What does activated adenylyl cyclase catalyze?
the conversion of cytosolic ATP molecules to cyclic AMP (cAMP)
What does cyclic AMP (cAMP) act as?
a second messenger
what does cAMP phosphodiesterase catalyze?
The action of cAMP eventually terminates when it is broken down to AMP
What does the activation of Gi cause?
the inhibition of adenylyl cyclase
What does the inhibition of adenylyl cyclase cause?
decrease the concentration of cAMP in the cell and thereby the phosphorylation of key proteins inside the cell
what does phospholipase C (PLC) catalyze?
the breakdown of a plasma membrane phospholipid
What does DAG activate?
protein kinase C, which then phosphorylate a large number of other proteins, leading to the cell’s response.
where does Cytosolic IP3 bind?
ligand-gated Ca^(2+) channel receptors on the endoplasmic reticulum that open when bound to IP3 resulting in increased cytosolic Ca^(2+) concentration
What is an action of Ca2+?
to help activate some forms of protein kinase C
What are the two ways Ca2+ can be used in the cytosol?
can be either increased or decreased in the cytosol to elicit a cellular response (change in membrane potential)
How is Ca2+ maintained at an extremely low level in the cytosol?
By means of active-transport systems in the plasma membrane and cell organelles
eicosanoids
present in plasma membrane phospholipids.
when does the synthesis of eicosanoids begin?
when an appropriate stimulus binds to its receptor and activates phospholipase 𝐀_𝟐 (PLA_2 )
Afferent neurons
- sensory
- Transmit information into the CNS from receptors at their peripheral endings
- Single process from the cell body splits into a long peripheral process (axon) that is in the PNS and a short central process (axon) the enters the CNS