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Introductory Biochemistry > Messengers in Drugs & Aspirin > Flashcards

Messengers in Drugs & Aspirin Flashcards

1
Q

What is protein kinase C (PKC)?

A

It forms a family of key enzymes that are involved in signalling pathways that specifically phosphorylated substrates at serine/threonine residues

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2
Q

What organelle has a very dense store of calcium ions?

A

A specialised area of the Endoplasmic Reticulum (ER)

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3
Q

How many molecules of InsP3 are required to open calcium-ion channels?

A

Four

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4
Q

What two things does PKC need for activity?

A

Calcium and PPS

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5
Q

What is InsP3?

A

A short-lived messenger that is metabolised and recycled

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6
Q

What is InsP3 dephosphorylated into?

A

Inositol

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7
Q

Calmodulin is a 17kDa calcium-responsive protein. How many calcium binding sites does it have, and how many calciums does it need to bind to for activation?

A

It has four calcium binding sites, and needs to bind to 3-4 calciums

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8
Q

The continual release of calcium can have detrimental effects, such as?

A
  1. Neural diseases
  2. Diabetes
  3. Duchenne muscular dystrophy
  4. Cardiac diseases
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9
Q

Diacylglycerol (DAG) works by increasing membrane-bound PKC’s affinity for what ions?

A

Calcium ions

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10
Q

Once PKC is activated, it is translated to the membrane by what proteins?

A

RACK proteins

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11
Q

What effect does PKC have on appetite?

A

It suppresses appetite

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12
Q

Eicosanoids are derived from 20C unsaturated fatty acids. What are they called?

A

Arachidonic acids

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13
Q

Where are arachidonic acids stored?

A

In membranes

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14
Q

What three types of eicosanoid lipid mediators can be derived from phospholipase-released arachidonic acid?

A
  1. Prostaglandins
  2. Thromboxane
  3. Leukotrienes
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15
Q

What function do prostaglandins have?

A

Has many roles including inducing fever, pain, and inflammation

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16
Q

What function does thromboxanes have?

A

They are involved in blood coagulation

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17
Q

What function does leukotrienes have?

A

They are released in response to an allergic reaction

18
Q

What effect does prostacyclin have on thromboxane?

A

It is anti-thromboxane

19
Q

What does PGH synthase convert arachidonic acid into?

A

Prostaglandins

20
Q

How does aspirin work against the symptoms of prostaglandins?

A

Aspirin works by inhibiting PGH synthase synthesis

21
Q

What are the benefits of aspirin?

A
  1. Analgesic - relieves pain
  2. Antipyretic - lowers fever
  3. Antiinflammatory
  4. Antiplatelet
22
Q

What are the serious side-effects of aspirin?

A
  1. Gastric bleeding
  2. Reyes syndrome (hepatic and cerebral damage in children)
23
Q

What component of PGH synthase is irreversibly inhibited by aspirin?

A

The COX component

24
Q

Is the inhibition of PGH synthase by aspirin competitive or non-competitive?

A

Non-competitive

25
Q

What are the two isoforms of PGH synthase?

A

PGH1 and PGH2

26
Q

What properties does PGH1 have?

A

It has housekeeping activities in cells

27
Q

What properties does PGH2 have?

A

It induces fever, inflammation and pain

28
Q

What isoform of PGH does aspirin effect?

A

PGH1 and PGH2 (both forms)

29
Q

What isoform of PGH is ibuprofen more specific for?

A

PGH2 (the COX2 component)

30
Q

How do leukotrienes differ from prostaglandins?

A

Leukotrienes are released more slowly, act more slowly, but last longer

31
Q

What are the effects of leukotrienes?

A
  1. They promote smooth muscle contraction
  2. Cause constriction of pulmonary arteries
  3. Increases permeability of blood capillary endothelium
  4. Increases mucus secretion
32
Q

The generation of leukotrienes is triggered in cells of the immune system due to what event?

A

An initial allergic reaction event

33
Q

What hormone decreases inflammation in the lungs?

A

Corticosteroid hormones

34
Q

Prostacyclin is produced by what type of cells to induce vasodilation and inhibition of platelet aggregation?

A

Endothelial cells

35
Q

What does viagra inhibit to increase cGMP levels?

A

A phosphodiesterase

36
Q

How many inositol triphosphate (InsP3) molecules are required to open a calcium channel in the calciosome?

A

Four

37
Q

What do the C1 domains of protein kinase C bind to?

A

Diacylglycerol

38
Q

What are the properties of PGH synthase?

A
  1. It is a bifunctional enzyme
  2. It has peroxidase activity
  3. It has 2 isoforms
  4. It is cytosolic rather than membrane bound
39
Q

How does aspirin inhibit prostaglandin production?

A

By acetylating a serine in the cyclo-oxygenase functional unit of the PGH synthase enzyme

40
Q

Does the drug Salbutamol act as an agonist or antagonist of a receptor?

A

An agonist

41
Q

What receptor is the drug Salbutamol associated with?

A

An adrenergic receptor

42
Q

Iloprost acts as a mimic of what secondary messenger?

A

Prostacyclin

Introductory Biochemistry (16 decks)

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