Molecular target 3 Flashcards

1
Q

Difference between primary and secondary active transport

A
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2
Q

What are the different transporters

A
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3
Q

Pumps (transporters) can be divided into what four categories

A
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4
Q

Metabolite transporters

A
  • 31 families
  • Important drug target e.g. chloroquine
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5
Q

How do neurotransmitter transporters work

A

They transport vesicles containing neurotransmitters
- Vesicular inhibitory AA transporter
- Vesicular excitatory AA transporter
- Vesicular amine transporter
They are mainly used for scientific research

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6
Q

Neurotransmitter transporters name examples and where are they found

A
  • They can be found in plasma membrane (presynaptic, postsynaptic and glial localisation)
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7
Q

How does citalopram work

A
  • Its a seratonin/5-HT transporter
  • Type of neurotransmitter transport (5-HT)
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8
Q

How does riluzole work

A
  • EAAT; excitatory amino acid transport
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9
Q

Transporters as drugs

A
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10
Q

What an enzyme-coupled receptor

A
  • Type of transmembrane receptor when bound by a ligand (growth factor or hormone) it functions as an enzyme
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11
Q

Classifications of ECRs

A

Receptor tyrosine kinases (main one)
Tyrosine kinase-associated receptors
Receptor serine/threonine kinases
Histidine-kinase-associated receptors
Receptor guanylyl cyclases
Receptor-like tyrosine phosphatases

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12
Q

Receptor tyrosine kinases

A
  • Phosphorylate tyrosine residue on a specific set of substrates
  • Usually activated by secrete growth factors and hormones
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13
Q

How are signals transduced across the plasma membrane? - ECR

A
  1. For GPCRs, ligands induce a conformational change
  2. Most ECRs are single a-helicase
  3. Receptor subunits create dimers or oligomers
  4. Oligomerisation of ECRs cause reorienation
  5. Reorientation - signalling- autophosphorylation
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14
Q

How does autophosphorylation cause biological effects?

A
  • When a kinase enzyme adds a phosphate to itself
  • This alters the enzymes structure and function
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15
Q

Why do we need to understand
molecular signalling pathway?

A

Identification of molecules involved in signalling may unearth new targets for drugs

EGF promotes cellular proliferation

Mutations in the EGF receptor have been identified in cancer

EGF and EGF-activated pathways are targets for anti-cancer therapies
Anti-EGF receptor antibodies
Tyrosine kinase inhibitors

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16
Q

Signalling through the insulin receptor

A
17
Q

How does insulin promote glycogen synthesis?

A