Receptor Classes, Structures, Signaling Mechanisms, and Drug Examples Flashcards

1
Q

Ligand-gated ion channel receptors

A
  • Nicotinic acetylcholine receptor
  • plasma membrane
  • 5 subunits
  • 4 transmembrane domains each
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2
Q

Ligand-gated ion channel receptors

A

Agonist binding to extracellular domain opens transmembrane ion pore allowing Na+ ions to enter cell

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3
Q

G protein-coupled receptors

A
  • B2-adrenergic receptor for epinephrine, norepinephrine
  • in plasma membrane
  • 7 transmembrane domains
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4
Q

G protein-coupled receptors

A

agonists binding inside the transmembrane domains activates associated GTP-binding proteins that in turn regulate effector enzymes that generate intracellular second messenger molecules

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5
Q

G protein-coupled receptors

A

Targets for OVER HALF OF ALL PRESCRIPTIONS

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6
Q

Receptors with intrinsic enzyme activity

A
  • insulin receptor
  • cell surface
    2 single-transmembrane proteins
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7
Q

Receptors with intrinsic enzyme activity

A

agonist binding to extracellular domain activates enzymatic activity of intracellular domain

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8
Q

Receptors with intrinsic enzyme activity

A
  • most commonly tyrosine kinase activity
  • phosphorylated substrates then medicate effects
  • “tyrosine kinase receptors”
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9
Q

Receptors with intrinsic enzyme activity

A

regulate gene expression, cell growth, cancer, differentiation

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10
Q

Nuclear transcription factor receptors

A
  • estrogen receptor

- steroid hormone receptors

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11
Q

Nuclear transcription factor receptors

A

agonist binds to ligand binding domain, allows DNA binding domain to bind specific DNA sequences, activation domain then increases/decreases transcription of associated genes

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12
Q

Nuclear transcription factor receptors

A

regulate gene expression, cell growth, cancer, development

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