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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
tucatinib use
HER2+ breast cancer, second line
26
FLT3 mutation found in what disease
30% of acute myeloid leukemias (AML)
27
types of FTL3 mutations
internal tandem duplication (ITD) or activation mutation in tyrosine kinase domain
28
what does a FTL3 mutation do?
increased proliferation decreased apoptosis
29
FTL3 inhibitors and types
midostaurin (I) crenolanib (I) quizartinib (II)
30
midostaurin target and type
FTL3 broad inhibitor type 1 1st gen
31
crenolanib target and type
FTL3 specific Type 1 Inhibitor 2nd gen
32
quizartinib target and type
FTL3 ITD mutations type II inhibitor
33
what is Bcr-Abl
fusion protein from Philadelphia chromosome with tyrosine kinase activity
34
what disease state has Bcr-Abl mutation
CML - chronic myeloid leukemia (95%)
35
Abl inhibitors
imatinib ponatinib
36
imatinib target and class/type
Abl inhibitor type 2 tyrosine kinase inhibitor
37
imatinib adverse effects
N/V edema neutropenia
38
T/F resistance is common in imatinib
T, they on this drug for life so resistance common
39
ponatinib target
Abl inhibitor
40
ponatinib resistance target
gatekeeper mutation T315I
41
what is EML4-ALK
translocation mutation in lung cancer active in cytoplasm
42
what is ALK
a transmembrane receptor like EGFR
43
ALK inhibitor
alectinib
44
alectinib target
ALK
45
alectinib indication and test
ALK+ NSCLC need companion diagnostic test
46
BRAF inhibitor
dabrafinib
47
dabrafinib target
BRAF- V600 inhibitor
48
dabrafinib used in combo with what
trametinib
49
trametinib target
MEK1 and MEK2
50
what type is Trametinib
Type III inhibitor
51
adverse effects trametinib
rash
52
trametinib limitation? when can we not use
prior BRAF inhibitor therapy
53
what is BTK
important for B cell activity and growth
54
BTK inhibitor
acalabrutinib
55
acalabrutinib target and type (rev or irrev)
BTK covalent inhibitor
56
aclabrutinib disease state target
B cell lymphoma MCL and CLL
57
sirolimus target
mTOR1 also IL-2
58
what is mTOR
serine - threonine kinase
59
mTOR inhibitor drug
sirolimus
60
how do mutations prevent efficacy of drugs?
prevent inhibitors from binding

PHRM 864 (28 decks)

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