Androgen Receptor Flashcards
5-10% of testosterone is produced in the _____.
adrenal glands
Upon _____, inhibitory chaperones are _____ and AR moves to the nucleus.
ligand binding; dissociated
Name 3 places testosterone is produced.
1) testes 2) adrenal glands 3) intracrine
What does leuprolide do?
it’s used for medical castration
How does enzalutamide work?
it inhibits nuclear translocation, co-activator recruitment, and DNA binding of AR
______ is an anti-androgen that blocks the receptor.
bicalutamide
The AR gene has ___ exons with protein length of ___ amino acids.
8; 919
Upon ligand binding, inhibitory chaperones are dissociated and ___ moves to the _____.
AR; nucleus
Abiraterone acetate, along with hormonal therapy, can reduce systemic testosterone levels to ____.
near 0
____ of abiraterone users report hypertension.
10%
The microsomal enzyme _____ plays a key role in androgen production.
cytochrome P 17 (CYP 17)
17% of abiraterone users had _______ (side effect).
hypokalemia
Mineralcortacoid excess leads to main side effects of _____.
abiraterone
What is bicalutamide for?
it’s an anti-androgen that blocks the receptor
90-95% of testosterone is produced in the _____.
testes
1% of testosterone is produced _____.
intracrinally
Approximately _____ men die each year from prostate cancer.
30,000
When not associated with an androgen, the ____ resides in the cytoplasm.
AR
______ is a CYP17 inhibitor.
Abiraterone acetate
Abiraterone acetate is a ______.
CYP17 inhibitor
______ is an antiandrogen with high binding affinity.
Enzalutamide
______ is a new generation androgen receptor antagonist.
Enzalutamide
What is the main treatment for prostate cancer?
hormone therapy that targets the androgen receptor (AR)
_____, along with hormonal therapy, can reduce systemic testosterone levels to near 0.
Abiraterone acetate
Lowering ____ produces clinical benefits in prostate cancer.
testosterone
_______ aim for specific receptors or enzymes critical to cancer growth and survival.
Next generation targeted agents
What does Abiraterone do?
inhibits CYP 17
Name 3 methods of hormonal therapy in PC.
1) surgical orchiectomy 2) GNRH agonists and antagonists 3) anti-androgens
The microsomal enzyme cytochrome P 17 (CYP17) plays a key role in ______.
androgen production
The ____ gene has 8 ____with protein length of 919 amino acids.
AR; exons
When not associated with an androgen, the AR resides in the ______.
cytoplasm
____ undergoes homo‐dimerization and binds to the androgen‐responsive elements of the DNA
AR
Name 3 side effects of abiraterone.
1) Hypokalemia 2) edema 3) hypertension
____ of abiraterone users had hypokalemia.
17%
After DNA binding, AR recruits co‐activators and _____.
gene expression occurs
What does enzalutamide do?
antiandrogen with high binding affinity
orchiectomy
castration
31% of users of abiraterone had _____ (side effect).
edema
_____ of users of abiraterone had edema.
31%
______ excess leads to main side effects of abiraterone.
Mineralcortacoid
After DNA binding, AR recruits _____ and gene expression occurs.
co‐activators
What is the most common androgen?
testosterone
Next generation targeted agents aim for _____ critical to cancer growth and survival.
specific receptors or enzymes
_____ is the most common cancer in men.
Prostate cancer
_____ is used for medical castration.
leuprolide
What is Ketoconazole?
an antifungal whose side effect is to shut down the adrenal gland
Name the 4 parts of the AR protein.
1) N-terminus activation domain 2) DNA binding domain 3) hinge region 4) C-terminus ligand binding domain
What drug inhibits CYP 17 to prevent testosterone production from all 3 sources?
Abiraterone
AR undergoes _____ and binds to the androgen‐responsive elements of the ____.
homo‐dimerization; DNA
Name 4 mechanisms of hormone resistance in PC.
1) AR activation by non-gonadal testosterone 2) overexpression of AR 3) AR mutations 4) truncated AR with constitutive binding activation
10% of abiraterone users report _____.
hypertension
Enzalutamide is a new generation androgen receptor _____.
antagonist
