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

19
Q

What is “on”

20
Q

What is “off”

21
Q

how to find Km based on michaelis menton graph

A

Take 1/2 of vmax

22
Q

[s] <km

23
Q

[S]»km

24
Q

Hexokinase I

A

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

25
Glucokinase
Present in hepatocytes Rate depends on serum glucose
26
What happens to glucokinase in fed state
Increases
27
What happens to glucokinase in fasted state
decreases
28
X intercept of LWB
-1/km
29
Slope of LWB
Km/vmax
30
Y intercept of LWB
1/vmax
31
What does an x-intercept close to 0 mean on LWB
Higher Km
32
What does a high y-intercept on LWB mean
Lower vmax
33
LWB equation
1/v0=km/vmax(1/[S]) + 1/vmax
34
Irreversible inhibitors
Bind extremely tightly to enzyme or form covalent bond
35
Competitive inhibition can be reversed by
Increasing substrate concentration
36
What is the only thing that can increase vmax
Adding enzyme
37
Why does Km decrease in uncompetitive inhibibition
Equilibrium shifts right to get rid of ES
38
In vitro
in parts IC50
39
In vivo
whole tissue EC50
40
Low IC50 or EC50 means
more potent, less of the drug is required to be effective
41
What are the covalent inhibitors
Aspirin, Organophosphates
42
What are the suicide inhibitors
Penicillin, Allopurinol
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