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Pharmacology and Toxicology > Enzymes as drug targets > Flashcards

Enzymes as drug targets Flashcards

1
Q

What is Vmax?

A

The maximum rate at which an enzyme

can carry out a reaction

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2
Q

What is Km?

A

Substrate concentration at which the

enzyme will work at ½ Vmax

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3
Q

What is 1/Vmax?

A

Where lineweaver burk plot crosses the y axis

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4
Q

What is -1/Km?

A

Where lineweaver burk plot crosses x axis

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5
Q

What are DD transpeptides?

A

Also known as penicillin binding protein (PBP)

Carries out crosslinking of peptidoglycan wall subunits for bacteria

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6
Q

How do beta lactams effect DD transpeptides?

A

Beta lactam antibiotics bind to and irreversibly inhibit DD Transpeptidase

preventing building of new cell walls

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7
Q

How are Beta lactamases responsible for some forms of antibiotic resistance

A

Bacteria counter the impact of beta lactam drugs by

producing an enzymatic defence system

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8
Q

What do HIV proteases do?

A

Activity central to HIV replication

Processes (cleaves) viral virion proteins
required for formation of active virus

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9
Q

What is atazanir?

A

a HIV protease

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10
Q

What are NSAIDs?

A

Cyclo-oxygenase inhibitors (one of the more selective coxibs)

NSAIDs are among the most widely used of all medicines. There are now more than 50 different examples on the global market.

  • Provide symptomatic relief from fever, pain and swelling in chronic joint disease, as well as in more acute inflammatory conditions
  • Inhibits the fatty acid cyclo-oxygenase (COX) enzyme
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11
Q

What is cyclo-oxygenase?

A
  • Responsible for the synthesis of prostaglandins
  • These are involved in inflammatory response
  • COX inhibitors reduce the synthesis of prostaglandins by inhibiting COX enzymes
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12
Q

What is COX-1?

A

Constitutive enzyme
Expressed in most tissue
‘housekeeping’ role
production of prostaglandins

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13
Q

What is COX-2?

A

Inducible enzyme

Production of mediators of inflammation

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14
Q

What COX does asparin inhibit?

A

COX 1 and 2

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15
Q

What COX does ibuprofen inhibit?

A

COX1 and 2

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16
Q

What COX does Celecoxib inhibit?

A

selectively inhibits COX 2

17
Q

What effects do cylco-pxygenase inhibitors have?

A

Anti-inflammatory, antipyretic and analgesic effects

18
Q

What does inhibiting COX enzymes result in?

A

inhibit the production of prostaglandin

19
Q

How do COX 2 selective drugs compare to regular cyclo-oxygenase inhibitors?

A

Lower GI toxicity

20
Q

What does Angiotensin converting enzyme do?

A

• Angiotensin converting enzyme (ACE) is involved
in regulating the function of the kidney

• Acts as a protease, cleaving angiotensin I and
converting it into angiotensin II, the active form of
the peptide

• This has a number of downstream consequences,
one of which is to increase water retention

21
Q

Difference between Angiotensin I and II?

A
  • Angiotensin I is inactive, but is converted by ACE to Angiotensin II
  • Angiotensin II is a potent vasoconstrictor
22
Q

Is the order of molecules between Angiotensinogen and the inactive degradation products of Angiotensin III?

A

Angiotensinogen

Angiotensin I

Angiotenisin II

Angiotensin III

Inactive degradation products

23
Q

What enzyme cleaves angiotensinogen to Angiotensin I?

A

Renin

24
Q

What enzyme cleaves angiotensin I to angiotensin II?

A

Angiotensin Converting Enzyme

25
Q

What enzyme cleaves angiotensin II to angiotensin III?

A

Aminopeptidase

26
Q

What enzyme converts angiotensin III to the inactive degradation products?

A

Angiotensinases

27
Q

How many amino acids constitutes angiotensinogen?

A

400+

28
Q

What does angiotensin II do?

A

potent vasoconstrictor

29
Q

How does ramipril lower blood pressure?

A

By inhibiting the proteolytic activity of ACE,
Ramipril decreases the production of
Angiotensin II, decreasing fluid retention
and thereby resulting in lowered blood
pressure

30
Q

What do protein kinases do?

A
  • Kinases are enzymes that form an integral part of signaling cascades within the cell
  • They hydrolyse ATP, transferring the gamma phosphate onto other molecules (often, but not always, other proteins)

• Covalent modification with phosphate groups modifies
protein function

31
Q

What is the function of reverse transcriptase in retroviruses?

A

It uses viral RNA as a template for DNA synthesis

32
Q

Drugs developed to treat AIDS are known as reverse transcriptase inhibitors. They worked because they ___.

A

bonded to the viral reverse transcriptase enzyme, thus preventing the virus from making a DNA copy of its RNA genome.

33
Q

Fill in the blanks: Angiotensin II causes ___________ of the vessels and triggers the release of ____________.

A

vasoconstriction; aldosterone

34
Q

What does a protein kinase do?

A

it transfers phosphates from ATP to proteins

Pharmacology and Toxicology (7 decks)

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