Pharmacodynamics II: Membrane Receptors Flashcards

1
Q

What are the FOUR main classes of receptors in cell signalling?

A
  1. Ligand-Gated Ion Channels - ionotropic
  2. G-Protein-Coupled Receptors - metabotropic
  3. Kinase-Linked Receptors
  4. Nuclear Receptors - intracellular
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2
Q

How many subunits do Ion Channels have?

A

4-5

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3
Q

Do Ion Channels have fast or slow communication?

A

Very fast (μs - ms)

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4
Q

What are SIX examples of receptors that use Ion Channels?

A
  1. Nicotinic Acetylcholine Receptor (nAChR)
  2. GABAa Receptor
  3. Glycine Receptor
  4. Glutamate Receptor
  5. 5-HT3 Receptor
  6. P2x Purine Receptor
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5
Q

How do G-Protein-Coupled Receptors work?

A
  • Receptors linked to EFFECTORS
  • Change intracellular level of second messenger via GTP-binding proteins (G-Proteins)
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6
Q

What are SIX examples of receptors that use G-Protein-Coupled Receptors?

A
  1. Muscarinic Acetylcholine Receptor (mAchR)
  2. GABAb Receptor
  3. Adrenoceptors
  4. Dopamine Receptors
  5. 5-HT2 (Serotonin) Receptor
  6. Histamine H2 Receptor
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7
Q

How many times does the G-Protein-Coupled Receptor span the membrane?

A

7 times

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8
Q

Which intracellular loop couples to G-Protein and determines selectivity?

A

Third

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9
Q

Where do SMALLER ligands bind on the G-Protein-Coupled Receptor?

A

Within helix structure

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10
Q

Where do LARGER ligands bind on the G-Protein-Coupled Receptor?

A

Extracellular surface

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11
Q

How does the Thrombin Receptor work?

A
  • Receptor activated by protease cleavage of N-terminus domain
  • Reveals a ‘tethered agonsit’
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12
Q

Which TWO subtypes of GPCR ACTIVATE specific receptors?

A

Gs and Gq

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13
Q

Which TWO subtypes of GPCR INHIBIT specific receptors?

A

Gi and Go

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14
Q

How long do GCPRs take to signal?

A

Seconds to minutes

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15
Q

What enzymes do secondary messengers on GCPRs activate?

A

Protein Kinases
* phosphorylate target proteins

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16
Q

Which enzymes synthesise and breakdown cAMP?

A
  • Synthesised by from ATP by ADENYLATE CYCLASE
  • Broken down by PHOSPHODIESTERASES
17
Q

Which enzyme synthesises cGMP?

A

Synthesised from GTP by GUANYLATE CYCLASE

18
Q

What are the TWO main functions of Kinase-Linked Receptors?

A
  1. Proliferation
  2. Differentiation
19
Q

Are Kinase-Linked Receptors monomers or polymers?

A

Monomers

20
Q

What THREE components make up a Kinase-Linked Receptor?

A
  1. Extracellular domain containing the ligand-binding site
  2. Single α-helix crossing the membrane
  3. Intracellular domain with catalytic activity
21
Q

What THREE amino acids do Kinase-Linked Receptors phosphorylate?

A
  1. Tyrosine
  2. Serine
  3. Threonine
22
Q

What are the TWO main types of Cytokines?

A
  1. Interferons α, β, γ
  2. Interleukins 2-7, 9-12, 15