Cell signaling II Flashcards
(58 cards)
What are G-protein-coupled receptors (GPCRs)?
The largest family of cell-surface receptors that mediate responses to external signals, hormones, neurotransmitters, and local mediators.
How many GPCRs are estimated to be present in humans?
More than 800 GPCRs.
What types of signal molecules can activate GPCRs?
Proteins, small peptides, derivatives of amino acids and fatty acids, photons of light, and molecules that can be smelled or tasted.
How many different GPCRs can a single signal molecule activate?
For example, epinephrine activates at least 9 distinct GPCRs.
What is the structural characteristic of GPCRs?
They consist of a single polypeptide chain that threads across the lipid bilayer seven times.
What is the role of G proteins in GPCR signaling?
They relay the signal into the cell interior.
What are the components of heterotrimeric G proteins?
Three subunits: α, β, and γ.
What happens to the α subunit of a G protein when a GPCR is activated?
It releases GDP and binds GTP.
What effect does GTP binding have on the Gα subunit?
It triggers a conformational change, allowing it to dissociate from the receptor and Gβγ pair.
What is the function of RGS proteins?
They act as GTPase-activating proteins (GAPs) that enhance GTP hydrolysis and shut off G-protein-mediated responses.
What does cyclic AMP (cAMP) act as in signaling pathways?
A second messenger.
What enzyme synthesizes cyclic AMP from ATP?
Adenylyl cyclase.
How is cyclic AMP degraded?
By cyclic AMP phosphodiesterases.
What does the activation of Gs G protein do to cAMP levels?
It increases cAMP concentrations.
What is the role of protein kinase A (PKA) in cAMP signaling?
It phosphorylates specific serines or threonines on target proteins, regulating their activity.
What happens to PKA upon cAMP binding?
The regulatory subunits dissociate, activating the catalytic subunits.
What are A-kinase anchoring proteins (AKAPs)?
Proteins that bind to the regulatory subunits of PKA and to components of the cytoskeleton or organelle membranes, localizing the kinase inside the cell.
What is the role of cyclic AMP in activating PKA?
Binding of cAMP to regulatory subunits induces a conformational change, activating the catalytic subunits.
What does the cyclic AMP response element (CRE) do?
It is a short cis-regulatory sequence that is recognized by the CRE-binding (CREB) protein, activating gene transcription.
What is the function of CREB in response to cAMP?
CREB is phosphorylated by PKA, which then recruits CBP to stimulate transcription of target genes.
What are the two products generated from the hydrolysis of PI(4,5)P2 by phospholipase C-β?
- Inositol 1,4,5-trisphosphate (IP3)
- Diacylglycerol.
What effect does IP3 have in the cell?
It binds to IP3 receptors in the ER membrane, triggering the release of Ca2+ into the cytosol.
What is the role of diacylglycerol (DAG) in cell signaling?
It activates protein kinase C (PKC) and remains embedded in the plasma membrane.
What is the function of protein kinase C (PKC)?
PKC phosphorylates target proteins, influencing various cellular responses.