Enzyme-linked cell surface receptors Flashcards
Receptor Classes - 6
What are they and what are their receptors?
Receptor guanylyl cyclases - ANP receptor; Receptor tyrosine kinases - growth factor receptors, insulin receptor, RAS; Tyrosin kinase associated receptors - erythropoietin receptor; Receptor Tyrosine phosphatases - CD45; Receptor serine/threonine kinases - Mullerian inhibiting substance; bone morphogenic protein
What is the ANP receptor?
a single membrane spanning protein with an extracellular receptor binding domain, a transmembrane domain and an intracellular guanylyl cyclase domains.
When is the guanylyl cyclase inactive?
As an unbound monomer
Guanylyl cyclase catalyzes what reaction?
The generation of cGMP from GTP and cGMP activates protein kinase G
s;o GTP > cGMP > protein kinase G > targeted proteins phosphorylated
What does Protein kinase G phosphorylate?
Target proteins
What do phosphorylated proteins mediate?
hormone function
BP Regulation - Why is ANP released from secretory vesicles in atria?
In response to an increase in stretch.
BP regulation - Where are NP-A/B receptors present?
adrenal glands, kidneys, and in vascular smooth muscle.
BP Regulation - what is caused by activation of NP-A/B?
results in cGMP generation and PKG activation.
BP Regulation - NP - A/B activation in the kidney increases? Reduces? Inhibits?
Increases glomerular filtration, reduces renin secretion, and inhibits Na+ and water retention.
BP Regulation - NP-A/B activation in adrenal gland inhibits? What does inhabitation lead to?
Inhibits aldosterone secretion, which leads to reduction of Na+ in water retention
BP Regulation - NP-A/B in blood vessels causes?
vasodilation via a relaxation of smooth muscle.
BP Regulation - Reduction in blood volume and vasodilation lead to what?
Reduction in BP
Insulin receptors consist of two what? What do they contain?
The receptor consists of two extracellular subunits which contains hormone binding domains and two membrane spanning subunits which contain cystolic tyrosine kinase domains.
What does binding of insulin cause?
activation of the receptor through auto-phosphorylation of cytosolic tyrosine kinase
Activated insulin receptor pathways - 1 - IRS1 pathway
where?
activated receptor associated with what? What does that cause?
In skeletal muscle and adipose tissues.
Activated receptor associates with IRS-1 on adapter protein, and causes activation of PI3K.
What does PI3K mediate?
mediates fusion to the cell membrane of vesicles that include GLUT4 in the vesicle membrane
What does GLUT4 mediate?
facilitated diffusion of glucose into the cell.
Insulin receptor signaling - MAPK pathways: The activated receptor activates what?
Activated receptor activates the adapter protein SOS
SOS activates what? and by promoting what? In the insulin pathways.
RAS by promoting the GTP bound form