PHAR232 - receptors and targets Flashcards

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1
Q

What are receptor tyrosine kinases (RTKs)?

A

A kinase putting a phosphate on tyrosine

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2
Q

What’s another name for receptor tyrosine kinases (RTKs)?

A

Kinase linked receptors

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3
Q

How many estimated genes have been associated with RTKs?

A

59 genes

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4
Q

Quick review

A
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5
Q
A
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6
Q

What does a kinase do?

A

Puts a phosphate on
(phosphorylation = activation)

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7
Q

What does a phosphatase do?

A

Takes phosphates off
(dephosphorylation = deactivation)

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8
Q

What is dimerisation?

A

two molecules come together to form a dimer, a complex consisting of two subunits.

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9
Q

What is growth factor receptor signalling especially goal orientated towards?

A

Gene transcription

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10
Q
A
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11
Q

What is the primary goal of the nuclear receptors?

A

Alter gene transcription

  • bind directly to DNA to trigger transcription of designated genes
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12
Q

What is another name for DNA binding domain?

A

Zinc fingers

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13
Q
A
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14
Q

Activation of gene tranription occurs in what 2 phases?

A
  • Primary response (within 30 mins)
  • Secondary response (utilises primary genes and takes longer)
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15
Q

What are 2 non ligand-gated ion channels?

A
  • Voltage-gated
  • Small cation channels
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16
Q
A
17
Q
A
18
Q

What do false-substrates do?

A

Try to out-compete normal substrates

19
Q

What are pro-drugs?

A

they become a blocker once acted upon by enzyme to be blocked

20
Q

What type of enzyme inhibitor is aspirin?

A

Irreversible inhibitor
- protein target must be destroyed in order to remove the drug
(like irreversible receptor antagonist)

21
Q

What is a competitive enzyme inhibitor?

A

Binds to the same site as normal substrate but CANNOT be catalysed
e.g. ACE inhibitors e.g. captopril

22
Q
A
23
Q
A
24
Q

Define receptor desensitisation

A

Loss of sensitivity of receptor continually stimulated by agonist e.g. insulin resistance

25
Q
A
26
Q

How do receptors predominantly undergo desensitisation?

A
  • ## PHOSPHORYLATION OF RECEPTORS
27
Q

What is the protein that removes a receptor from the membrane for cellular desensitization?

A

Arrestin

28
Q

What protein does homologous pathway of desensitization utilise?

A

Arrestin (it’s ARRESTING the molecule = no longer working)

29
Q

What does is the end result of heterologous receptor desensitation?

A

Reduced G-protein coupling

30
Q

LEARN - DESENSITIZATION & RECEPTOR TRAFFICKING - draw it out

A
31
Q
A
32
Q

Is caffeine an antagonist or agonist of adenosine receptors?

A

antagonist

33
Q
A