Androgen Receptors

Question 1

Most of prostate cancer is treated with ______.

Answer 1

non-specific cytotoxic chemotherapy

Question 2

______ is an anti-fungal medication that suppresses ________.

Answer 2

Ketoconazole; adrenal production

Question 3

What are the three methods of hormonal therapy for prostate cancer?

Answer 3

Bilateral orchiectomy; GNRH agonists and antagonists; anti-androgen

Question 4

The androgen receptor resides in the ________ when not bound to an androgen.

Answer 4

cytoplasm

Question 5

Upon binding to an androgen, _______ dissociate from the androgen receptor, allowing it to enter the nucleus.

Answer 5

chaperone proteins

Question 6

Where is testosterone produced, and in what proportions?

Answer 6

Testis = 90%

Adrenal glands = 10% (hence ketoconazole)

Question 7

_____ and ______ are androgen receptor antagonists.

Answer 7

Flutamide; bicalutamide

Question 8

_______ is a CYP17 inhibitor that blocks production of androgens (both testosterone and estradiol).

Answer 8

Abiraterone

Question 9

List three side effects of abiraterone.

Answer 9

Hypokalemia, edema, and hypertension.

Question 10

The newest AR antagonist is _____; it has a binding affinity 5-8 fold greater than bicalutamide.

Answer 10

enzalutamide

Question 11

The androgen receptor is made up of four parts: _____, ______, _____, and _____.

Answer 11

N-terminus transactivation domain (NTD);

DNA-binding domain; hinge region; C-terminus ligand-binding domain (CTD)