Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Cancer PD > Hormonal treatments of cancer > Flashcards

Hormonal treatments of cancer Flashcards

1
Q

Describe the drug palbociclib

A

It is a selective CDK4 and CDK6 inhibitor approved for treating hormone receptor-positive HER2-negative breast cancer COMBINED with endocrine therapy

(It targets the cell cycle)
palbociclib inhibits cell growth and suppresses DNA replication

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Give examples of Topoisomerase I inhibitors

A

Camptothecins
topotecan
Irinotecan

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Give examples of Topoisomerase II inhibitors

A

Anthracyclines

Epipodophyllotoxins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Where are steroid hormones synthesised from?

A

Cholesterol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Where is the aromatase enzyme stored?

A

Adipose and hepatic tissue

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

How do postmenopausal women receive oestrogen (endogenous)?

A

Through the conversion of androgens by the aromatase enzyme

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Aromatase inhibitor mechanism of action

A

Inhibits the aromatase enzyme which reduces the production of oestrogen

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Explain the 2 types of aromatase inhibitors

A

Type 1 inhibitors (androgen analogues) they bind irreversible to aromatase

Type 2 inhibitors contain a functional group that binds to the heme iron of the cytochrome p450 which interferes with the hydroxylation reactions.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Give examples for the 2 types of aromatase inhibitors

A

Type 1 inhibitors exemestane

Type 2 inhibitors anastrozole

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

State a type 1 aromatase inhibitor

A

Exemestane

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

State a type 2 aromatase inhibitor

A

Anastrozole

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Selective oestrogen receptor modulators (SERMs) examples

A

Tamoxifen

Raloxifen

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Tamoxifen moa

A

Tamoxifen binds to the ER at the ligand binding site.
(partial agonist)

Competitevely binds to the ER and adopts a different conformation that is dimerised and translocated to the cells nucleus
It binds to the DNA forming a new complex that has partial functions.

AF1 is active (AF2 domain doesn’t function)
Partial coactivators recruited

= partially inactivated transcription

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

How does tamoxifen have mixed activity?

A

It activates ER in the liver and uterus

It acts as an antagonist in breast tissue

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Give an example of a selective receptor down-regulator

A

Fulvestrant

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Fulvestrant moa

A

Binds to the ER monomers
inhibiting receptor dimerisation = blocking nuclear localisation of the receptor

Fulvestrant- ER complex that enters the nucleus is ‘transcriptionally inactive’ as AF1 and AF2 are disabled

= Fulvestrant - ER complex its unstable = accelerated degradation of the ER protein

17
Q

What is an apocrine gland?

A

A specialised exocrine gland in which a part of the cells cytoplasm breaks off releasing the contents

18
Q

Explain the differences between endocrine and exocrine glands

A

Exocrine glands secrete substances out onto a surface of a cavity through a ductal structure
Whereas
Endocrine glands secrete substances directly into the blood stream

19
Q

Oestrogen function in the normal breast

A

(oestrogen is involved in cellular proliferation and differentiation)
Oestrogen allows the maintenance of mammary gland tissue
It primes tissue for the effects of progesterone during pregnancy for milk production

20
Q

What is breast cancer?

A

Breast cancer occurs when abnormal cells in the breast begin to grow and divide uncontrollably leading to tumour formation

21
Q

Where does breast cancer usually start?

A

In the breast tissue (commonly in cells that line the milk ducts of the breast)

majority of breast cancers arise from the luminal cells (that express ER)

22
Q

Ductal breast carcinoma in situ (DCIS) vs lobular breast carcinoma in situ (LCIS)

A

DCIS - When cancer develops in ducts (that carry milk to the nipple) but remain within ducts ‘in situ’
Cancer cells have not yet spread outside the ducts into surrounding tissue

LCIS - abnormal cells form in the lobules (milk-producing glands) of the breast
*isn’t cancer but indicates an increased risk of developing breast cancer

23
Q

Main function of the prostate gland

A

It produces prostatic fluid that creates semen when mixed with sperm produced by the testicles

24
Q

AR (androgen receptor) function in the normal prostate

A

Androgens regulate prostate cell division and development

25
Q

Which grading system is used to evaluate the prognosis of men using prostate biopsy samples?

A

Gleason grading system

Sample is examined by histology

26
Q

Give an example of an androgen biosynthesis inhibitor

A

Abiraterone

It inhibits the production of androgenic pre-cursors

27
Q

Abiraterone MOA:

A

It inhibits adrenal androgen production (disruption in adrenal synthesis) = decreased levels of serum testosterone

28
Q

Testosterone synthesis inhibitors

& moa

A

Goserelin -> Super agonist
Abarelix -> Antagonist

They depress testosterone production

29
Q

Abarelix moa

A

Abarelix = Antagonist

It blocks the GnRH in the pituitary gland = decreased LH = sustained suppression of testosterone release

30
Q

What mechanism drives prostate growth and function?

A

Testosterone is converted in the prostate cells to a more potent form = dihydrotestosterone (DHT)
DHT binds to the androgen receptor = receptor dimerisation = translocation into the nucleus = binds to DNA = coactivation of machinery stimulation gene transcription = cell growth

31
Q

5 alpha reductase inhibitors moa

A

5 alpha reductase converts testosterone into DHT

Inhibits the conversion of testosterone into dihydrotestosterone (= inhibits tumour growth)

32
Q

Examples of 5 alpha reductase inhibitors

A

Finasteride
Dutasteride

(asteride)

33
Q

When are 5 alpha reductase inhibitors mainly used?

A

They are commonly used for benign prostate hyperplasia

34
Q

Examples of androgen antagonists

A

Bicatutamide
Flutamide
(-amide)

35
Q

Androgen antagonists moa

A

It inhibits androgens (DHT) from binding to the receptor (AR) at the ligand binding site.
= inactivation of the receptor

Cancer PD (4 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions