Cell Receptors

*Insulin vs Glucagon Receptors

  • insulin = tyrosine kinase receptor
    --> PI3K pathway
    --> increases GLUT 4 transporters to the surface
    for glucose uptake into cell
  • glucagon = Gs receptor
    --> increase AC and cAMP levels

Receptor Type Mneumonics

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Intracellular Receptors:

  • "stay IN, watch TV, PET a CAT"

"stay IN, watch TV, PET a CAT"


stay IN = intracellular receptors


T = T3/T4
V = Vitamin D


P = progesterone
E = estrogen
T = Testosterone


C = cortisol
A = Aldosterone
T = T3/T4
intracellular = intracellular


intracellular = intracellular



*Types of Rectors

  • Ionotropic receptors = ions go through immediately when ligand/voltage stimulate
  • metaboltropic receptors = 2nd messenger system
    --> cAMP, cGMP, IP3/DAG/PKC

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*Metabotropic Receptors

  • G proteins
    2nd messenger system
    --> cAMP, cGMP, IP3/DAG/PKC

*IonotropicReceptors

  • Ionotropic receptors = ions go through immediately when ligand/voltage stimulate
  • IONOTROPIC = NICANOTROPIC = Nicotonic Musc receptors allow ions into the cell
    --> they are nonspecific
    --> allow Na+ and Ca+ in
    --> allow K+ leakage out

*G protein Receptors

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*Gq Protein receptors
(q = contracting / Ca++)

  • "PIP DAGs for PKC... IP3 = INdoPLasmic reticulum"
    --> PIP2 = phospholipid from the cell membrane
    --> PIP2 makes DAG and release PIP2 also
    --> DAG anchors the PKC to the cell membrane and gets it ready for Ca++ binding
    --> IP3 = INdoPLasmic reticulum"" = IP3 goes to the INdoPLastic reticulum to release Ca++ to bind to PKC and activate it
  • 5HT serotonin
  • histamine H1
  • angiotensin receptor 1

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  • NE binds to alpha 1 NE receptors
  • GDP bound to alpha subunit of (α,β,γ) G protein --> phosphorylated to GTP
  • the GTP-Alpha subunit leaves the Gq protein complex and activates the phospholipase C protein
  • phospholipase C converts PIP2 from the plasma membrane into both
    --> DAG = dyacylglycerol
    --> IP3
  • DAG prepares PKC = protein kinase C to be activated by anchoring it to the plasma membrane
  • IP3 then travels to the sarcloplasmic reticulum to release Ca++
  • Ca++ then travels to the PKC and DAG to activate PKC
  • together these lead to muscle contraction

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*Gi Protein receptors
(i = inhibitory)

  • alpha 2 receptors

*Gs Protein receptors
(s = stimulating)

  • beta receptors
  • glucagon

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Glycogen and Insulin and Glucagon
(Glucose Hormone Control)

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Notes:

  • glycogen is released from stores by the enzyme glycogen phosphorylase
  • note that below, no matter the receptor, the activation of glycogen phosphorylase is in the name
    --> activated by phosphorylation
    --> cAMP + PKA (glucagon + Epi.)
    --> inhibited by Tyr. Kinase (insulin)
  • the opposite is true for glycogen synthase
    --> activated by DEphosphorylation (Tyr. Kinase --> protein phosphatase)

*Insulin Receptors

  • insulin = tyrosine kinase receptor
    --> PI3K pathway
    --> increases GLUT 4 transporters to the surface
    for glucose uptake into cell

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*Glucagon Receptors

  • glucagon = Gs receptor
    --> increase AC and cAMP levels

Glucagon receptors

Glucagon Example

Notes:
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Glucagon receptors for Beta blocker overdose case

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Notes:

  • note that

Clinical Case

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