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Pharmacology > Nuclear Hormone Receptor Signalling Pathways > Flashcards

Nuclear Hormone Receptor Signalling Pathways Flashcards

1
Q

What are the main classes of receptors?

A

Ligand-gated ion channels
G-protein coupled receptors
Enzyme-linked receptors
Nuclear receptors

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2
Q

Where can receptors be found?

A

Cell surface

Intracellular

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3
Q

What roles does hormones play in signal transduction?

A

1st messenger

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4
Q

How are hormones classified?

A

Steroids or nonsteroidal

Bases on structure + mechanism of action

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5
Q

Describe steroid hormones

A

Lipid soluble = pass through membrane
Derived from cholesterol
Slower acting that nonsteroidal

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6
Q

What is the process of steroid hormones?

A

Enter target cell
Bind to intracellular receptor
Activate genes
= proteins

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7
Q

Describe nonsteroidal hormones

A

H2O soluble
Derived from amino acids
Faster than steroid hormones

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8
Q

What is the process for nonsteroidal hormones?

A

Bind to cell surface receptor
Activates signal transduction pathway
Produce 2nd messenger

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9
Q

What mechanism does nonsteroidal follow?

A

Intermediate
Activate existing enzymes
= small amount of hormone produce significant change

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10
Q

What are examples of steroid hormones?

A

Androgens, oestrogens + progesterone
Corticosteroids
Mineralocorticoids
Glucocorticoids

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11
Q

Where are androgens, oestrogens + progesterone found?

A

Cytoplasm

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12
Q

What are androgens, oestrogens + progesterone produced by?

A

Gonads

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13
Q

What are corticosteroids, mineralocorticoids, glucocorticoids produced by?

A

Adrenal gland

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14
Q

What does glucocorticoids do?

A

Stimulate glucose production

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15
Q

What does mineralocorticoids do?

A

Act on kidney to regulate salt + H2O balance

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16
Q

Where are mineralocorticoids + glucocorticoids found?

A

Cytoplasm

17
Q

What is thyroid hormone produce by?

A

Thyroid gland

18
Q

Where is thyroid hormone found?

A

Bound to DNA in nucleus

19
Q

What does thyroid hormone do?

A

Development + regulation of metabolism

20
Q

What does vitamin D3 do?

A

Regulate Ca2+ metabolism = bone growth

21
Q

What does retinoic acid do?

A

Vertebrate development

22
Q

Where is retinoic acid found?

A

Bound to DNA in nucleus

23
Q

What is retinoic acid synthesised from?

A

Vitamin A

24
Q

What do receptors for steroid hormones form?

A

Homodimers

25
Q

What are homodimers?

A

Two identical molecules that come together

26
Q

What do other nuclear receptors form?

A

Heterodimers

27
Q

What are heterodimers?

A

Two different molecules

28
Q

Describe structure of nuclear receptors

A 
Transactivation domain (A/B + E)
DNA-binding/dimerization domain (C)
Nuclear localisation domain (D)
29
Q

What is transactivation domain (A/B + E)?

A

Allows change in response to ligand

= change in DNA, initiating transcription

30
Q

What is DNA-binding/dimerization domain (C)?

A

Allows dimerization of receptors + binding to DNA

31
Q

What is nuclear localisation domain (D)?

A

Allows receptors to enter nucleus

OR maintain nuclear localisation

32
Q

Describe mechanism for cytoplasmic receptor activation

A

Ligand enters cell + causes receptor activation
Binding dislodges repressor protein
Ligand-receptor complex enters nucleus
Binds to specific DNA sequence
In promotor region
Specific sequence = hormone response element
Gene transcribed + translated = protein

33
Q

What is the alternative to gene transcribed in mechanism for cytoplasmic receptor activation?

A

Gene expression inhibited
Latent period
= production of mRNA + protein

34
Q

Describe transcriptional activation by glucocorticoid hormone

A

Hormone binds to hormone receptor
Repressor dislodged
Complex receptor free to go into nucleus
Binds to glucocorticoid response element = transcription

35
Q

Describe transcriptional activation by thyroid hormone

A

Thyroid diffuses into cytoplasm
Bind to nuclear receptor
OR bind to receptor already bound to DNA
Transcription

36
Q

What is an example of steroid signalling?

A

Aldosterone

37
Q

Describe steroid signalling - aldosterone

A

Stimulate renal Na+ stimulation
Na+ reabsorption depends upon epithelial Na+ channel
In cortical collecting duct
CDC cells express protein Nedd4-2
It binds to ENaC = channels internalised
Limits rate of Na recovery = Na+ lost in urine

38
Q

What does aldosterone do?

A 
Induces expression of protein kinase (serum)
SGK1 phosphorylates Nedd4-2
Prevents protein binding to ENaC
= ENaC remains in membrane
= increased Na+ retention

Pharmacology (40 decks)

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