Signaling Flashcards
___________________ is a 51 amino acid peptide that is released by pancreatic beta cells of the islets of Langerhans when the concentration of blood glucose is high.
Insulin
______________________ is a 29 amino acid peptide hormone that is released when the concentration of glucose in the blood drops below 5 mM.
Glucagon
Where are receptors for glucagon located in the body?
In the liver and fat cells; there are no glucagon receptors on muscle cells
_______________________ is a catecholamine hormone that signals fight or flight; it is produced in the adrenal glands.
Epinephrine
Both _____________ and ____________ act upon G-protein coupled receptors.
Glucagon
Epinephrine
____________ ________________ ____________ _____________ are a key component of a signaling pathway - a pathway that transduces a signal that converts information (i.e., a hormonal signal) into a chemical change. Signal transduction pathways are characterized by having highly specific interacts between ligands and receptors in the nM kd range and amplified signals.
G-protein coupled receptors
What are the three essential components of G-protein coupled receptors?
- Plasma membrane receptor with 7 transmembrane helical segments
- An effector enzyme in the pasma membrane that generates an intracellular second messenger
- A guanine nucleotide binding protein (“G-protein”)
What are the seven steps of the GPCR stimulatory pathway?
- Ligand binds to receptor
- Occupied receptor causes replacement of the GDP bound to Gs by GTP, activating Gs
- Gs (alpha subunit) moves to adenylyl cyclase and activates it
- Adenylyl cyclase catalyzes the formation of cAMP
- cAMP activates PKA
- PKA phosphorylates cellular proteins that causes response to ligand
- cAMP is degraded, reversing the activation of PKA
What are three ways to stop a signal?
- Degrade secondary messenger (cAMP)
- Replace GTP with GDP on G-protein (intrinsic GTPase activity)
- Receptor endocytosis
What degrades the secondary messenger cAMP?
Cyclic nucleotide phosphodiesterase
______ _____________ is a heterotrimeric protein that consists of three subunits (alpha, beta, gamma). Upon hormone binding to receptor, GDP is replaced by GTP, activating the alpha subunit and releasing it from the beta-gamma complex. The alpha subunit moves in the membrane to an effector protein and activates it. This protein contains intrinsic GTPase activity that limits its time in the active GTP bound state.
G-protein
_____________ _______________ is an integral membrane protein that is activated by association with Gsalpha-GTP and catalyzes the formation of the secondary messenger, cAMP.
Adenylyl cyclase
___________ is a common secondary messenger, an intracelullar mediator of an extracellular hormonal signal.
cAMP
Adenylyl cyclase catalyzes the conversion of ATP to _____________, a 3’ –> 5’ cyclic structure.
Cyclic AMP
___________________ phosphorylates multiple targets at specific sites containing serine or threonin residues; it is inactive when its regulatory and catalytic subunits are bound together and active when cAMP binds its regulatory subunits, freeing its catalytic subunits.
Protein kinase A