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PHRM 864 > Dykheizen Kinases > Flashcards

Dykheizen Kinases Flashcards

1
Q

what molecule is the source of a kinase?

A

ATP

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2
Q

which amino acids can be phosphorylated by kinases?

A

serine, threonine, tyrosine

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3
Q

what does a type I inhibitor do

A

binds active confirmation

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4
Q

what does a type II inhibitor do

A

binds inactive confirmation

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5
Q

what does a type III inhibitor do?

A

binds allosteric pocket outside of ATP binding pocket

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6
Q

how do competitive inhibitors bind

A

reversibly, compete with ATP

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7
Q

how do covalent inhibitors bind?

A

irreversibly

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8
Q

gefitinib target

A

EGFR

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9
Q

gefitinib class

A

kinase inhibitor
type 1 reversible
1st gen

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10
Q

what does EGFR do

A

induces cell proliferation
functions through tyrosine kinase activity

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11
Q

gefitinib approved for what

A

NSCLC with EGFR exon 19 or exon 21 mutations

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12
Q

afatinib target

A

EGFR

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13
Q

afatinib class and type

A

tyorsine kinase inhibitor
covalent inhibitor
2nd gen

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14
Q

what does rash mean with afatinib and gefitinib

A

drug working better

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15
Q

what type of resistance mutation forms with gefitinib and afatinib?

A

T790M

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16
Q

which drug is for NSCLC with T790M mutation?

A

osimertinib

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17
Q

osimertinib target

A

EGFR inhibitor

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18
Q

osimertinib class and type

A

covalent kinase inhibitor
3rd gen

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19
Q

lapatinib target

A

HER2 and EGFR

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20
Q

lapatinib type (rev or irev)

A

reversible inhibitor

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21
Q

lapatinib treats what

A

HER2+ breast cancer

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22
Q

lapatinib side effect

A

cardiac function decrease - CHF

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23
Q

tucatinib target

A

HER2

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24
Q

tucatinib side effect profile

A

decreased compared to lapatinib

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25
Q

tucatinib use

A

HER2+ breast cancer, second line

26
Q

FLT3 mutation found in what disease

A

30% of acute myeloid leukemias (AML)

27
Q

types of FTL3 mutations

A

internal tandem duplication (ITD) or activation mutation in tyrosine kinase domain

28
Q

what does a FTL3 mutation do?

A

increased proliferation
decreased apoptosis

29
Q

FTL3 inhibitors and types

A

midostaurin (I)
crenolanib (I)
quizartinib (II)

30
Q

midostaurin target and type

A

FTL3
broad inhibitor
type 1
1st gen

31
Q

crenolanib target and type

A

FTL3
specific
Type 1 Inhibitor
2nd gen

32
Q

quizartinib target and type

A

FTL3
ITD mutations
type II inhibitor

33
Q

what is Bcr-Abl

A

fusion protein from Philadelphia chromosome with tyrosine kinase activity

34
Q

what disease state has Bcr-Abl mutation

A

CML - chronic myeloid leukemia (95%)

35
Q

Abl inhibitors

A

imatinib
ponatinib

36
Q

imatinib target and class/type

A

Abl inhibitor
type 2 tyrosine kinase inhibitor

37
Q

imatinib adverse effects

A

N/V
edema
neutropenia

38
Q

T/F resistance is common in imatinib

A

T, they on this drug for life so resistance common

39
Q

ponatinib target

A

Abl inhibitor

40
Q

ponatinib resistance target

A

gatekeeper mutation
T315I

41
Q

what is EML4-ALK

A

translocation mutation in lung cancer
active in cytoplasm

42
Q

what is ALK

A

a transmembrane receptor like EGFR

43
Q

ALK inhibitor

A

alectinib

44
Q

alectinib target

A

ALK

45
Q

alectinib indication and test

A

ALK+ NSCLC
need companion diagnostic test

46
Q

BRAF inhibitor

A

dabrafinib

47
Q

dabrafinib target

A

BRAF- V600 inhibitor

48
Q

dabrafinib used in combo with what

A

trametinib

49
Q

trametinib target

A

MEK1 and MEK2

50
Q

what type is Trametinib

A

Type III inhibitor

51
Q

adverse effects trametinib

A

rash

52
Q

trametinib limitation? when can we not use

A

prior BRAF inhibitor therapy

53
Q

what is BTK

A

important for B cell activity and growth

54
Q

BTK inhibitor

A

acalabrutinib

55
Q

acalabrutinib target and type (rev or irrev)

A

BTK
covalent inhibitor

56
Q

aclabrutinib disease state target

A

B cell lymphoma
MCL and CLL

57
Q

sirolimus target

A

mTOR1
also IL-2

58
Q

what is mTOR

A

serine - threonine kinase

59
Q

mTOR inhibitor drug

A

sirolimus

60
Q

how do mutations prevent efficacy of drugs?

A

prevent inhibitors from binding

PHRM 864 (7 decks)

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