Intracellular Signalling at the Cell Membrane Flashcards
the intracellular events that transform the extracellular signal into an intracellular signal
transduction
examples of effectors
protein kinases or transcription factors
An extracellular signal activates a ________
membrane-bound receptor
receptor activation leads to an _______ cytosolic or membrane concentration of 2nd messenger
increased
Single activated receptor → many molecules of 2nd messenger =
amplification
signal termination is due to a number of processes (3)
- inactivation of receptor (no 1st messenger) or receptor-associated effectors
- degradation or removal of 2nd messenger
- negative feedback
name 3 types of cell membrane receptors
- ion channel-coupled receptors
- G-protein coupled receptors
- enzyme-coupled receptors
the largest family of cell membrane receptors are
G-protein-coupled receptors (GPCRs)
800 unique G-protein-coupled receptors (GPCRs). Almost half of ________ act on these receptors or their pathways
medications
GPCR: Receptor activation → activation of a protein that binds to a _____ nucleotide
guanine
The activated G-protein is on a “timer”. Has intrinsic GTP-ase activity. When GTP hydrolyzed → GDP then the G-protein is
______
inactive
Receptor = integral transmembrane protein. Spans the membrane _ times
7
3 protein subunits:
α, β, γ
α is bound to GDP, and βγ is bound to α
unstimulated
α subunit releases GDP, replacing it with GTP and the α subunit disengages from the βγ subunits
Stimulated
When the α unit hydrolyzes
GTP → GDP, it becomes
______ again
inactivated
- Ligand binds to receptor associated with a ___ G-protein
- G_ releases GDP and binds GTP at the alpha subunit - by detaches from G-protein
- G_ binds to and activates adenylyl cyclase
- membrane-bound enzyme that converts ATP to cAMP - cAMP binds to protein kinase (PK A)
- binds to inhibitors of PK A, which then detach, and allow the activate parts of PK A to work - PK A phosphorylates a multitude of effector proteins
Gs GPCR
what enzyme converts ATP to cAMP
adenylyl cyclase
what enzyme causes an inactivation of cAMP by converting it to 5’-AMP
cyclic AMP phosphodiesterase
- called the “turning off” process
Stimulates adenylyl cyclase → cAMP production. cAMP activates PK A → phosphorylation of effectors
Gs
biological impact of: Glycogenolysis,
thyroid hormone
synthesis
Gs
alpha subunit Inhibits adenylyl
cyclase → decreased cAMP production. Decreases PK A activation.
Gi
what pathway inhibits Gs pathways
Gi alpha
beta-gamma Activates K+ channels*. Creates More negative cell membrane potential.
Gi
Biological impact of reduction of
heart rate
Gi beta-gamma