Term
|
Definition
BRCA1/BRCA2: repair ssDNA breaks by
recombination
PARP: repairs ssDNA breaks.
Cancers with loss of BRCA1+2 repair are
sensitive to PARP inhibitors |
|
|
Term
G1 -> S phase inhibitors
(therapeutics that damage DNA) |
|
Definition
Platinum coordination compounds: form
complexes between guanine.
Alkylating Agents: Abnormal base
pairing with thymine -> strand breakage
Kill cells by initiating DNA damage pathways.(P53) |
|
|
Term
S Phase inhibitors
Antimetabolites: Lack nucleotides for synthesis |
|
Definition
Interfere with production of nucleic acids
Purine: mercaptopurine
Pyrimidine: 5-fluorouracil binds to
thymidylate synthase
Folic Acid: Methotrexate
All block DNA synthesis |
|
|
Term
| Agents that inhibit G2 -> M |
|
Definition
Lack of G2 -> M checkpoint control _>
mitotic catastrophe(p53 independent
apoptosis)
Low dose of doxorubicin -> mitotic
catastrophe
Doxurubicin inhibits topoisomerase II |
|
|
Term
Agents that inhibit M phase
Mitotic spindle inhibitors |
|
Definition
Paclitaxel(Taxol):
Stabilizes Microtubles, No dissassembly
Vinblastine, Vincristine:
Binds tubulin sub units, prevents
polymerization |
|
|
Term
|
Definition
Adenoviral p53 gene therapy
Bortezomib(Velcade) blocks proteasome activity
-> buildup of BAX
Inhibit Bcl-2, Bcl-xL.(BCl inhibits
pore formation) |
|
|
Term
|
Definition
VEGF: Bevacizumab(Avastin)
EGFR: Cetuximab(Erbitux)
HER2: Tratuzumab(herceptin) |
|
|
Term
| Drugs targeting kinases(RTKs) |
|
Definition
Tarceva and Iressa = EGFR TKI
Imatinib/Glevac inhibit Bcr-ABL fusion
(philadelphia chromosome, CML) |
|
|
Term
| Inhibition of Angiogenesis |
|
Definition
VEGF: Bevacizumab(avastin)
Monoclonal VEGF antibody
ECM derived: Thrombospondin, Endostatin
Block response to VEGF |
|
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Term
|
Definition
Mutation in RB LOF(normally binds EGF)
Leukocoria(white eye)
Germline mutation: 1 yr old. Bilateral.
Normally presents 0-2 years old
AD inheritance patern |
|
|
Term
|
Definition
Mutation in BRCA1/2 LOF
BRCA2 increases risk in males
Inheritance pattern AD
Increased risk of prostate or ovarian
cancer |
|
|
Term
|
Definition
t(9;22)
Palpable Spleen. Elevated WBC
Gleevac treats.
NO inheritance risk. Acquired transloation |
|
|
Term
| FAP(familial adenomatous polyposis) |
|
Definition
APC mutated -> Increase in B-catenin
AD inheritance patern. Test childern
Need additional mutations to progress
from adenoma to carcinoma
Many POLYPs |
|
|
Term
|
Definition
NF1(Ras GAP) mutation LOF
Have prolonged activation of Ras
(Ras gap inactivates Ras)
Inheritence AD 100% penetrance.
Lisch nodules, Cafe-au-lait spots
Bilateral freckling |
|
|
Term
| Xeroderma Pigmentosum(XP) |
|
Definition
Severe sun sensititvy, hyperpigmentation
Mutation in Nucleotide Excision repair
genes
Autosomal recessive Inheritance pattern
Pyrimidine dimers cant be repaired |
|
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