E1 association practice Flashcards
P16 or P53
tumor suppressor
CDK4/6 cell cycle phase
g1
CYP19
aromatase
steroidal/non-steriodal
androgens to estrogens
lymphoid lineage
glucocorticoids
antag and agonist effects
tamoxifen
adipocytes
source of estrogen in post meno women
6.5
prostate cancer
flare
GnRH analogs (leuprolide, goselerin)
feminization
17-a-hydrolase and CYP17
Abiraterone
-lutamide
Androgen receptor antagonists
inactive confirmation
type II kinase inhibitor
t790M
resistance to gefitinib
use osimertinib to treat
covalent
Afatinib
Osimertinib
Acalabrutinib
mesenchymal
sarcoma
both EGFR and HER2
lapatinib
sxs of CHF
lapatinib, trast/pert
GOAL
EGFR inhibitors
FLT3
myeloid leukemia
midostaurin
crenolanib
quizartinib
ITD mutations
quizartinib
Philadelphia
Bcr-Abl
CML
Imatinib
Ponatinib
T315, gatekeeper
Ponatinib
EML4-ALK
wild type
alectinib
BRAF-V600
dabrafenib
Dabrafenib
BRAF-V600
wild type
combo with trametinib
trametinib
MEK1 and MEK2
rash
allosteric (type III)
combo with dabraf
BTK
B cells
Ibrutinib
Acalabrutinib
Cys481
Acalabrutinib
mTOR
rapamycin analogs
-limus drugs
serine-threonine kinase
interfere with pyrimidine nucleotide synthesis
5-FU
capecitabine
Inhibit DNA polymerase alpha
Cytarabine and Gemcitabine
thymidylate synthase
5-FU
DPD
5-FU
Thymidine
5-FU rescue
5-FU synergy
leucovorate
Capecitabine
prodrug of 5-FU
Cytidine deaminase
Cytarabine
DNA polymerase alpha
Ara-CTP Cytarabine shit
tetrahydrouridine
cytidine deaminase inhibitor
cytarabine combo for effiacy
block purine synthesis
6-MP
TPMT
6-MP genetic shit
allopurinol
6-MP
xanthine oxidase
6-TG
allopurinol does NOT block breakdown
DHFR
folic acid/folates
TMP synthesis
methotrexate
methotrexate rescue
leucovorin
reverse toxic effects of DHFR inhibition
intrastrand and interstrand
dna alkylation
second malignancies
alkylators
all alkylators SE
myelosuppression
aryl group
chlorambucil
decrease nucleophilicity
hydroxylation by CP450
cyclophosphamide
aldehyde dehydrogenase
cyclophosphamide
acrolein
acrolein
cyclophosphamide
aldehyde dehydrogenase
hemorrhagic cystitis
acrolein
cyclophosphamide
mesna
cyclophosphamide
bladder
urine
bifunctional adducts
mitomycin C (alkylator)
prodrug (4)
tamoxifen
capecitabine
irinotecan (SN38)
cyclophosphamide
crosslinkers
platinum drugs
cisplatin
alkylators
cisplatin
intrastrand
aquo form shit
nephrotoxicity
ototoxicity
cisplatin
increased expression resistance class glutathione-S-transferase (GST)
alkylating agents
flu-like sxs with CHF risk
trastuzumab
inhibit dimerization drug
pertuzumab
CLEOPATRA
trast and pertuz
HER2+
EGF and TGF-alpha
Cetuximab
CYP2d6
tamoxifen
severe infusion reaction
xi drugs
VEGF
angiogenesis
bevacizumab
CD20
b cells (non-hodgkins)
rituximab
Ofatumumab
CD38
daratumumab
HER2/Neu
trastuzumab emtansine
CD3 and CD19
blinatumomab
Target T cells
also think CD3 apparently
CD3 and CD20
Mosunetuzumab
CTLA-4 and PD1 purpose
reactivate T cells
bind to CTLA-4
Ipilimumab
PD-1 location
on T cells
bind PD-1
pembrolizumab
Binds PDL-1
Atezolizumab
expressed on macrophages on tumor cells
PDL-1
PAP-GM-CSF
sipulcel-T
stimulate immune system to attack cancer
isolates T cells
CAR-T
CD19
target for CAR-T
topo I cleavage
S phase
Glutathione-s-transferase overexpression
resistance in topo I inhibitors
UGT1A1
Irinotecan polymorphism increases toxicity
SN-38
Irinotecan active metabolite
Topo I phase
S
anthracycline
topo II
doxorubicin
cardiotoxicity
doxorubicin
free radicals
dextra drug
G2/M block cell cycle
etoposide
vincristine
bleomycin
kinectochore
spindle assembly
microtubule inhibitors
peripheral neuropathy
vinca alkaloids
neurotoxicity and severe local inflammation
vincristine
vinca
taxane bind
tubulin
block depolymerization
Poor PGP substrate
epothilones (ixabepilone)
Proteasome activity
Bortezomib
ubiquitin
bortezomib
proteasome
potent teratogen
thalidomide
cereblon
pomalidomide
PROTACs
BCL-2
venetoclax
intercalators
irinotecan
bleomycin
doxorubicin
23% lung cancers
EGFR mutations
drug enhances t cell activation
ipilimumab
no requirement of chemical or enzymatic change drug
doxorubicin
5-azacytidine
DNA methyltransferase
BCR
CD20 works in combo with
L85R mutation
afatinib
allosteric
trametinib