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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