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M2M Unit III > Androgen Receptor > Flashcards

Androgen Receptor Flashcards

1
Q

5-10% of testosterone is produced in the _____.

A

adrenal glands

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1
Q

Upon _____, inhibitory chaperones are _____ and AR moves to the nucleus.

A

ligand binding; dissociated

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2
Q

Name 3 places testosterone is produced.

A

1) testes 2) adrenal glands 3) intracrine

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2
Q

What does leuprolide do?

A

it’s used for medical castration

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2
Q

How does enzalutamide work?

A

it inhibits nuclear translocation, co-activator recruitment, and DNA binding of AR

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3
Q

______ is an anti-androgen that blocks the receptor.

A

bicalutamide

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4
Q

The AR gene has ___ exons with protein length of ___ amino acids.

A

8; 919

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5
Q

Upon ligand binding, inhibitory chaperones are dissociated and ___ moves to the _____.

A

AR; nucleus

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6
Q

Abiraterone acetate, along with hormonal therapy, can reduce systemic testosterone levels to ____.

A

near 0

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7
Q

____ of abiraterone users report hypertension.

A

10%

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8
Q

The microsomal enzyme _____ plays a key role in androgen production.

A

cytochrome P 17 (CYP 17)

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8
Q

17% of abiraterone users had _______ (side effect).

A

hypokalemia

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8
Q

Mineralcortacoid excess leads to main side effects of _____.

A

abiraterone

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9
Q

What is bicalutamide for?

A

it’s an anti-androgen that blocks the receptor

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10
Q

90-95% of testosterone is produced in the _____.

A

testes

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10
Q

1% of testosterone is produced _____.

A

intracrinally

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11
Q

Approximately _____ men die each year from prostate cancer.

A

30,000

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12
Q

When not associated with an androgen, the ____ resides in the cytoplasm.

A

AR

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13
Q

______ is a CYP17 inhibitor.

A

Abiraterone acetate

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14
Q

Abiraterone acetate is a ______.

A

CYP17 inhibitor

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16
Q

______ is an antiandrogen with high binding affinity.

A

Enzalutamide

18
Q

______ is a new generation androgen receptor antagonist.

A

Enzalutamide

20
Q

What is the main treatment for prostate cancer?

A

hormone therapy that targets the androgen receptor (AR)

21
Q

_____, along with hormonal therapy, can reduce systemic testosterone levels to near 0.

A

Abiraterone acetate

21
Q

Lowering ____ produces clinical benefits in prostate cancer.

A

testosterone

23
Q

_______ aim for specific receptors or enzymes critical to cancer growth and survival.

A

Next generation targeted agents

23
Q

What does Abiraterone do?

A

inhibits CYP 17

24
Q

Name 3 methods of hormonal therapy in PC.

A

1) surgical orchiectomy 2) GNRH agonists and antagonists 3) anti-androgens

25
Q

The microsomal enzyme cytochrome P 17 (CYP17) plays a key role in ______.

A

androgen production

26
Q

The ____ gene has 8 ____with protein length of 919 amino acids.

A

AR; exons

27
Q

When not associated with an androgen, the AR resides in the ______.

A

cytoplasm

28
Q

____ undergoes homo‐dimerization and binds to the androgen‐responsive elements of the DNA

A

AR

29
Q

Name 3 side effects of abiraterone.

A

1) Hypokalemia 2) edema 3) hypertension

30
Q

____ of abiraterone users had hypokalemia.

A

17%

32
Q

After DNA binding, AR recruits co‐activators and _____.

A

gene expression occurs

32
Q

What does enzalutamide do?

A

antiandrogen with high binding affinity

34
Q

orchiectomy

A

castration

35
Q

31% of users of abiraterone had _____ (side effect).

A

edema

36
Q

_____ of users of abiraterone had edema.

A

31%

36
Q

______ excess leads to main side effects of abiraterone.

A

Mineralcortacoid

37
Q

After DNA binding, AR recruits _____ and gene expression occurs.

A

co‐activators

38
Q

What is the most common androgen?

A

testosterone

39
Q

Next generation targeted agents aim for _____ critical to cancer growth and survival.

A

specific receptors or enzymes

41
Q

_____ is the most common cancer in men.

A

Prostate cancer

43
Q

_____ is used for medical castration.

A

leuprolide

45
Q

What is Ketoconazole?

A

an antifungal whose side effect is to shut down the adrenal gland

46
Q

Name the 4 parts of the AR protein.

A

1) N-terminus activation domain 2) DNA binding domain 3) hinge region 4) C-terminus ligand binding domain

47
Q

What drug inhibits CYP 17 to prevent testosterone production from all 3 sources?

A

Abiraterone

48
Q

AR undergoes _____ and binds to the androgen‐responsive elements of the ____.

A

homo‐dimerization; DNA

50
Q

Name 4 mechanisms of hormone resistance in PC.

A

1) AR activation by non-gonadal testosterone 2) overexpression of AR 3) AR mutations 4) truncated AR with constitutive binding activation

51
Q

10% of abiraterone users report _____.

A

hypertension

52
Q

Enzalutamide is a new generation androgen receptor _____.

A

antagonist

M2M Unit III (30 decks)

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