W7 - Enzymes as Drug Targets Flashcards

1
Q

What are enzymes

A

Enzymes are biological catalysts that speed up the pace of chemical reactions, which are central to all aspects of cellular function in both prokaryotic and eukaryotic cells

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2
Q

What is the active site

A

Enzymes have specialized binding sites that are specific for certain substrates, once bound (via non covalent bonding) the substrate is then modified and released

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3
Q

What is the effect of an enzyme of the kinetics of a reaction

A

The enzyme lowers the activation energy for a reaction to take place. So less energy is required for the reaction to take place so it is more likely to occur

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4
Q

What is activation energy

A

Minimum amount of energy needed for a reaction take place

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5
Q

What is Vmax

A

the maximum rate at which an enzyme can carry out a reaction

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6
Q

What is Km

A

Substrate concentration at which the enzyme will work at 1/2 v max

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7
Q

Where do you see vmax and Km

A

Rate concentration graph

Lineweaver burke plot

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8
Q

what is a Lineweaver burke plot

A

it is a linier plot using data to calculate both Km and Vmax

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9
Q

What are the two types of inhibitio

A

reversible

irreversible

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10
Q

what are the two categories of inhibition

A

competitive

Non competitive

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11
Q

How does competitive inhibition work

A

The inhibitor binds to the active site, meaning that the substrate cannot form an enzyme substrate complexes so less reactions taking place

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12
Q

What is the result of competitive inhibition on the Km

A

Km value gets larger

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13
Q

What is the result of competive inhibition on the Vmax

A

does not change

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14
Q

Describe non competitive inhibition

A

Inhibitor binds to an enzyme at its allosteric site (away from the active site) changing the shape of the active site meaning that enzyme substrate complexes cannot form

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15
Q

What is the result of non competitive inhibition on the Km

A

Does not change

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16
Q

What is the result of non competitive inhibition on the Vmax

A

Increases

17
Q

What is the result of enzymes being turned off in bacteria and viruses

A

If the enzymes produced by infectious agents can be switched off this can be fatal for the bacteria or virus in question.

18
Q

What do the best bactericidal drugs target

A

DD transpeptidases

19
Q

Why are DD transpeptidases good to target

A

It carries out crosslinking of peptidoglycan wall subunits so when it is inhibited it prevents the building of new bacterial cell walls.

20
Q

What happens as a result of beta lactam drugs

A

Produces an enzymatic defense system and it is part of the reason there are some forms of antibiotic resistance

21
Q

What does altering regulatory enzyme function do to the body

A

Alters the physiological function downstream of that enzyme

22
Q

What can targeting enzyme function be used for

A

Can be used to modulate human physiology

23
Q

What is a common cause of disease

A

Mutations, changes in the protein sequence leads to a variety of human diseases due to altered enzymatic function