Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
32 Cards in this Set
- Front
- Back
Activation of PTK-associated receptors is thought to be a result of what?
|
Receptor dimerization
|
|
Autophosphorylation both increases the activity of _________________ and creates ______________ for specific binding of proteins with so-called SRC homology-2 (SH2) domains.
|
Tyrosine kinase; phosphotyrosine
|
|
What 2 pathways involving phosphoinositides are activated by receptor PTKs ?
|
Phosphatidylinositol 3-kinase (PI3K); phospholipase C-γ (PLC-γ) and phosphoinositide turnover pathway
|
|
After an insulin receptor binds insulin, it undergoes autophosporylation on what?
|
The carboxyl-terminal Tyrosine residues
|
|
What binds to pyrophosphate of IRS-1?
|
The SH2 domain of Grb2
|
|
What causes GDP release and GTP binding to Ras?
|
Sos binding to Grb2
|
|
What happens once Ras is activated?
|
Activated Ras binds and activates Raf-1
|
|
What does Raf-1 do?
|
phosphorylates MEK on 2 Serine residues (activating it)
|
|
MEK phosphorylates ERK on a ________ and a ________ residue, activating it.
|
threonine; tyrosine
|
|
Ras is inactivated by _________.
|
GTP
|
|
IRS-1, phosphorylated by the insulin receptor, activates what by binding to its SH2 domain?
|
PI-3K
|
|
PI-3K converts PIP2 to ______.
|
PIP3
|
|
What is the target on PIP2 for phosphorylation by PI3-K?
|
the hydroxyl group at C-3
|
|
PIP3 interacts with proteins via their PH domains causing what?
|
the activation of protein kinase B (PKB - a protein Ser/Thr kinase)
|
|
What degrades PIP3 back to PIP2?
|
a lipid phosphatase called PTEN
|
|
PDK1 phosphorylates __________ bound to __________.
|
PKB; PIP3
|
|
When activated, PKB phosphorylates GSK3 on a ______ residue, (inactivating or activating) it.
|
Ser; inactivating
|
|
What happens if GSK3 becomes phosphorylated?
|
it cannot convert glycogen synthase (GS) to its inactive form (so GS remains active) and synthesis of glycogen from glucose is accelerated
|
|
When GS is inactive PKB stimulates movement of what from which transporter?
|
Glucose uptake is increased through the glucose transporter GLUT4
|
|
In the liver, insulin promotes what?
|
glycogen synthesis by enhancing dephosphorylation of both phosphorylase and glycogen synthase
|
|
In adipose tissue, insulin promotes ___________ and inhibits ____________.
|
Lipogenesis; lipid breakdown (lipolysis)
|
|
In muscle and fat cells, insulin promotes what?
|
Glucose transport by stimulating fusion of vesicles containing GLUT-4 glucose transporters with the plasma membrane
|
|
Once ERK is phosphorylated, it moves into the __________ and phosphorylates ________________ such as EIK1
|
Nucleus; nuclear transcription factors
|
|
What kinase cascade is important of cellular division?
|
MAP Kinase Cascade
|
|
_______ is a monoclonal antibody against a minor form of human epidermal growth factor receptor (Her2) for treatment of breast cancer.
|
Herceptin
|
|
What is a monoclonal antibody against epidermal growth factor receptor?
|
Erbitux
|
|
What is a monoclonal antibody against vascular endothelial growth factor for treatment of advanced colorectal cancer?
|
Avastin
|
|
_________ is a chemical inhibitor of protein tyrosine kinases, c-Abl and c-Kit for treatment of chronic myeloid leukemia and gastrointestinal stromal tumors
|
Gleevac
|
|
The receptors for EPO, prolactin, and growth hormone are atypical cytokine receptors. So their ligand-binding component binds what?
|
JAK
|
|
JAKs are activated by ______________.
|
trans autophosphorylation
|
|
Activated JAKs stimulate tyrosine phosphorylation of cytoplasmic components of _______ factors.
|
STAT
|
|
After activated JAKs phosphorylate STAT, what 3 things happen?
|
1.) STAT dimerizes through interactions of tyrosine phosphates with SH2 domains
2) translocates to the nucleus 3) regulates specific gene activities |