Exam 2 Flashcards
(142 cards)
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.