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IHO Week 3 > Signal Transduction I > Flashcards

Signal Transduction I Flashcards

1
Q

Huggins

A

1966, hormone deprivation as a treatment for hormone driven cancer.

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2
Q

3 ways to lower hormone concentration

A

decrease synthesis
Increase catabolism
neutralizing Ab to soak up hormone

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3
Q

2 ways to decrease hormone synthesis

A

turn down synthesis stimulation

drug directed-based interaction

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4
Q

LHRH Superagonist Mech

A

binds very strongly to LHRH receptor

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5
Q

LHRH Analog names

A

leuprolide

goserlin

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6
Q

What happens when LHRH superagonist binds?

A

Immediate increase in LH and testosterone
Then a fall to castrate levels
(things don’t like to be ovedriven)

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7
Q

LHRH side effects

A

medications, none

hypogonal, miserable

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8
Q

LHRH long term

A

iatrogenic osteoporosis

insulin resistence

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9
Q

Dagarelix (firmagone)

A

LHRH antagonist

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10
Q

Starting point for all sex hormones

A

cholesterol

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11
Q

17-lyase inhibition consequence

A

decrease in androgen like hormones

diminished cortisol

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12
Q

Lyase inhibitor

A

Abiraterone

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13
Q

What is given with abiraterone

A

adrenocorticoids (need physiological replacement)

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14
Q

Block testosterone by…

A

Conversion to T to DHT

Block androgen receptor

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15
Q

Anti-androgen (2)

A

Bicalutamide

Enzalutamide

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16
Q

Estrogen lowering drugs

A 
Leuprolide
Lysase inhibitors (not FDA approved)
17
Q

Best target for estrogen synthesis inhibition?

A

Aromatase (minimal tweaking of other hormones)

18
Q

Aromatase inhibitors

A

Anastrozole

Exemestane

19
Q

Anastrozole side effects

A

arthralgia and myalgia

20
Q

Exemestane

A

Suicide substrate

arthralgia and myalgia

21
Q

Tamoxifen

A

Selective Estrogen receptor modulator (SERM)

22
Q

How is Tamoxifen selective

A

Partial antagonist to certain isoforms
blocks breast form well
agonist in bone and uterus

23
Q

Tamoxifen problem

A

Endometrial cancer (agonist in uterus)

24
Q

Fulvestrant

A

pure ER antagonist

outperforms Tamoxifen

IHO Week 3 (4 decks)

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