Androgen Receptor

Question 1

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

Answer 1

adrenal glands

Question 1

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

Answer 1

ligand binding; dissociated

Question 2

Name 3 places testosterone is produced.

Answer 2

1) testes 2) adrenal glands 3) intracrine

Question 2

What does leuprolide do?

Answer 2

it’s used for medical castration

Question 2

How does enzalutamide work?

Answer 2

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

Question 3

______ is an anti-androgen that blocks the receptor.

Answer 3

bicalutamide

Question 4

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

Answer 4

8; 919

Question 5

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

Answer 5

AR; nucleus

Question 6

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

Answer 6

near 0

Question 7

____ of abiraterone users report hypertension.

Answer 7

10%

Question 8

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

Answer 8

cytochrome P 17 (CYP 17)

Question 8

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

Answer 8

hypokalemia

Question 8

Mineralcortacoid excess leads to main side effects of _____.

Answer 8

abiraterone

Question 9

What is bicalutamide for?

Answer 9

it’s an anti-androgen that blocks the receptor

Question 10

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

Answer 10

testes

Question 10

1% of testosterone is produced _____.

Answer 10

intracrinally

Question 11

Approximately _____ men die each year from prostate cancer.

Answer 11

30,000

Question 12

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

Answer 12

AR

Question 13

______ is a CYP17 inhibitor.

Answer 13

Abiraterone acetate

Question 14

Abiraterone acetate is a ______.

Answer 14

CYP17 inhibitor

Question 16

______ is an antiandrogen with high binding affinity.

Answer 16

Enzalutamide

Question 18

______ is a new generation androgen receptor antagonist.

Answer 18

Enzalutamide

Question 20

What is the main treatment for prostate cancer?

Answer 20

hormone therapy that targets the androgen receptor (AR)

Question 21

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

Answer 21

Abiraterone acetate

Question 21

Lowering ____ produces clinical benefits in prostate cancer.

Answer 21

testosterone

Question 23

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

Answer 23

Next generation targeted agents

Question 23

What does Abiraterone do?

Answer 23

inhibits CYP 17

Question 24

Name 3 methods of hormonal therapy in PC.

Answer 24

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

Question 25

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

Answer 25

androgen production

Question 26

The ____ gene has 8 \_\_\_\_with protein length of 919 amino acids.

Answer 26

AR; exons

Question 27

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

Answer 27

cytoplasm

Question 28

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

Answer 28

AR

Question 29

Name 3 side effects of abiraterone.

Answer 29

1) Hypokalemia 2) edema 3) hypertension

Question 30

\_\_\_\_ of abiraterone users had hypokalemia.

Answer 30

17%

Question 32

After DNA binding, AR recruits co‐activators and \_\_\_\_\_.

Answer 32

gene expression occurs

Question 32

What does enzalutamide do?

Answer 32

antiandrogen with high binding affinity

Question 34

orchiectomy

Answer 34

castration

Question 35

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

Answer 35

edema

Question 36

\_\_\_\_\_ of users of abiraterone had edema.

Answer 36

31%

Question 36

\_\_\_\_\_\_ excess leads to main side effects of abiraterone.

Answer 36

Mineralcortacoid

Question 37

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

Answer 37

co‐activators

Question 38

What is the most common androgen?

Answer 38

testosterone

Question 39

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

Answer 39

specific receptors or enzymes

Question 41

\_\_\_\_\_ is the most common cancer in men.

Answer 41

Prostate cancer

Question 43

\_\_\_\_\_ is used for medical castration.

Answer 43

leuprolide

Question 45

What is Ketoconazole?

Answer 45

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

Question 46

Name the 4 parts of the AR protein.

Answer 46

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

Question 47

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

Answer 47

Abiraterone

Question 48

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

Answer 48

homo‐dimerization; DNA

Question 50

Name 4 mechanisms of hormone resistance in PC.

Answer 50

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

Question 51

10% of abiraterone users report \_\_\_\_\_.

Answer 51

hypertension

Question 52

Enzalutamide is a new generation androgen receptor \_\_\_\_\_.

Answer 52

antagonist