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Mechanisms of Drug Action > Cell Biology and Drug Targets > Flashcards

Cell Biology and Drug Targets Flashcards

1
Q

Which type of transcription factors are involved in cell differentiation?

A

Yamanaka factors

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2
Q

Give 4 examples of post-translational modification of proteins

A
  • Glycosylation
  • Phosphorylation
  • Lipidation
  • Acetylation
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3
Q

Which organelle generates new ribsomes?

A

Nucleolus

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4
Q

What are the 4 major drug targets?

A
  • Receptors
  • Enzymes
  • Transporters
  • Ion Channels
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5
Q

Give 4 effects of phosphorylation on proteins

A
  • in enzymes generate binding sites
  • increase/decrease acitivity
  • mark proteins out for degradation
  • binding of proteins together
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6
Q

Give an example of an intracellular receptor

A

Steroid receptors in cytoplasm

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7
Q

What are the 4 types of signalling?

A
  • Intercellular signalling
  • Paracrine signalling
  • Endocrine signalling
  • Synaptic signalling
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8
Q

How many transmembrane domains do GPCR contain?

A

7

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9
Q

Give 3 examples of drugs which act on GPCRs

A
  • Propanolol
  • Salbutamol
  • Atropine
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10
Q

Give an example of an enzyme coupled receptor

A

Receptor tyrosine kinase

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11
Q

How is an enzyme coupled receptor activated when something binds?

A

Binding causes cross-linking (which activates the enzyme)

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12
Q

What do nuclear receptors generally regulate?

A

Gene transcription

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13
Q

How do steroid hormones cause a change in protein synthesis?

A
  • Hormones bind and cause hydrophobic molecules to diffuse into the cytosol
  • These molecules bind to cytoplasmic binding protein which allows the molecule to enter the nucleus
  • This alters gene expression
  • Which alters protein synthesis
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14
Q

What is a full agonist?

A

A drug which induces a maximum tissure response

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15
Q

How are enzyme coupled receptors acitvated?

A

The binding of a ligand causes cross linking

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16
Q

What are receptor tyrosine kinases often receptors for?

A

Growth factors

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17
Q

What is the link between receptor tyrosine kinases and cancer?

A

RTK pathways are often mutated in cancer cells. Because RTKs are involved in gene regulation and cell growth

18
Q

Why are enzymes important drug targets?

A
  • They are an important part of signalling cascades
  • Some drugs are not active so require an enzyme to convert the drug into an active form
19
Q

Give an example of a drug which acts on an enzyme

A

Aspirin acts on COX -1 and COX-2 enzymes

20
Q

What is the structure of a channel mediated transporter?

A

A protein with a pore down the centre

21
Q

What is the structure of a transporter-mediated protein?

A

Contain abinding pocket for a molecule, once bound the transporter can flip 180º to allow the molecule through the membrane

22
Q

Are transporter-mediated proteins faster or slower than pore/channel proteins?

A

Slower

23
Q

What are the 3 types of transporters?

A
  • Uniport
  • Symport
  • Antiport
24
Q

What is a uniport transporter?

A

A transporter which only transports one product in one direction

25
Q

What is a symport transporter?

A

A transporter which transports two things in the same direction at the same time

26
Q

What is an antiport transporter?

A

A transporter which transports two substances in opposite directions at the same time

27
Q

Give an example of a passive transporter

A

The glucose transporter

28
Q

Give an example of an active transporter

A

Na+/K+ ATPase

29
Q

What class of enzyme do active transporters require?

A

ATPase

30
Q

Give a mechanism for how some transporters work

A
  • Transporter has a binding site on one side
  • binding of a ligand causes conformational shape change
  • this causes the transporter to close on one side and open on the other side
31
Q

What is the ratio of transport for Na+/K+ ATPase?

A

3 Na+ in for every 2K+ out

32
Q

Give an example of a drug which acts on the Na+/K+ ATPase

A

Digoxin

33
Q

What effect does digoxin have on:

a) Na+/K+ APTase
b) Heart rate?

A

a) Blocks it
b) Increases strength of contraction and increases heart rate due to greater depolarisation in muscle cells

34
Q

Are all ion channels passive?

A

yes

35
Q

What is the specificity of an ion channel determined by?

A

Size and charge of the molecule

36
Q

In which direction does movement of ions through an ion channel occur?

A

Down a concentration gradient

37
Q

What is the function of Gs (α) subunit?

A

Activates adenylyl cyclase

38
Q

What is the function of Gi (α) subunit?

A

Inhibition of adenylyl cyclase

39
Q

What is the function of Gq(α)?

A

Activation of phospholipase c

40
Q

What is the function of Gi (βγ)?

A

Opening K+ ion channels

41
Q

Which ligand-gated ion channel is involved in insulin secretion from β-cells?

A

ATP sensitive K+ channels

42
Q

Outline how glucose stimulates insulin secretion from β cells in the pancreas

A
  • Intracellular glucose levels rise and cause a rise in [ATP] as respiration rate increases
  • ATP binds to K+ channel and prevents movement of K+, causing depolarisation
  • This causes the opening of voltage gated Ca2+ channels and increased [Ca2+] causes storage granules to release insulin

Mechanisms of Drug Action (8 decks)

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