Enzyme inhibitors Flashcards

1
Q

How does allopurinol bind

A

Non covalently
Binds to serine on xanthine oxidase which mimics hypoxanthine

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2
Q

What does allopurinol prevent

A

Production of uric acid

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3
Q

Aspirin

A

irreversible, covalent inhibitor
Binds covalently to serine of COX and inhibits production of prostaglandins which cause pain and swelling

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4
Q

How do organophosphates bind

A

Covalently

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5
Q

What does organophosphates do

A

Irreversible covalent inhibitor
Binds to sarin nerve gas and pesticides
Binds to serinde residue on acetylcholinesterase
-can’t break down Ach and causes paralysis

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6
Q

What kind of inhibitor is allopurinol

A

Suicide

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7
Q

What kind of enzyme is penicillin

A

Suicide, transition state analog

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8
Q

What does penicillin inhibit

A

glycopeptide aminotransferase

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9
Q

What does penicillin do

A

Suicide inhibitor
Pretends to be glycopeptide transpeptidase which cleaves bacterial cell wall
Active site serine attacks it and gets stuck

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10
Q

How many carbons does stearic acid have

A

18 (s)

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11
Q

How many carbons in palmitic acid

A

16 (p)

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12
Q

Saturated fats are _____ at room temperature

A

Solid

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13
Q

Which glycerophospholipids is predominantly found on the outer leaflet of the plasma membrane

A

Phosphatidylcholine

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14
Q

General acid/base catalysts

A

Glu, His, Asp
Conditional: Lys, Ser, Tyr, Cys, Arg

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15
Q

Covalent catalysts

A

His, Lys, Ser, Cys

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16
Q

What type of inhibitor is statin

A

Competitive inhibitor
Treats hypercholesterolemia

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17
Q

V0 is limited by

A

K3

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18
Q

Km equation

A

K2+k3/K1

19
Q

What is “on”

A

K1

20
Q

What is “off”

A

K2+K3

21
Q

how to find Km based on michaelis menton graph

A

Take 1/2 of vmax

22
Q

[s] <km

A

vmax/km

23
Q

[S]»km

A

vmax

24
Q

Hexokinase I

A

Present in RBC
works at vmax so that RBC always has energy

25
Q

Glucokinase

A

Present in hepatocytes
Rate depends on serum glucose

26
Q

What happens to glucokinase in fed state

A

Increases

27
Q

What happens to glucokinase in fasted state

A

decreases

28
Q

X intercept of LWB

A

-1/km

29
Q

Slope of LWB

A

Km/vmax

30
Q

Y intercept of LWB

A

1/vmax

31
Q

What does an x-intercept close to 0 mean on LWB

A

Higher Km

32
Q

What does a high y-intercept on LWB mean

A

Lower vmax

33
Q

LWB equation

A

1/v0=km/vmax(1/[S]) + 1/vmax

34
Q

Irreversible inhibitors

A

Bind extremely tightly to enzyme or form covalent bond

35
Q

Competitive inhibition can be reversed by

A

Increasing substrate concentration

36
Q

What is the only thing that can increase vmax

A

Adding enzyme

37
Q

Why does Km decrease in uncompetitive inhibibition

A

Equilibrium shifts right to get rid of ES

38
Q

In vitro

A

in parts
IC50

39
Q

In vivo

A

whole tissue
EC50

40
Q

Low IC50 or EC50 means

A

more potent, less of the drug is required to be effective

41
Q

What are the covalent inhibitors

A

Aspirin, Organophosphates

42
Q

What are the suicide inhibitors

A

Penicillin, Allopurinol

43
Q
A
44
Q
A