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Antineoplastics
N/A
22
Biology
Graduate
01/17/2010

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Term
Methotrexate
Definition
Antimetabolite: inhibits DHFR reduction of folic acid to THF, prevents synthesis of thymine from uracil
Term
5-fluorouracil
Definition
Antimetabolite: is phosphorylated to either 5-fluorouracil triphosphate (and is incorporated into mRNA) or 5-flourodeoxyuracil diphosphate (5F-dUMP), which inhibits thymidylate synthetase
Term
Vincristine and vinblastine
Definition
Vinca alcaloids: bind to and aggregate tubulin dimers to prevent polymerization of MT's
Term
Paclitaxel and Docetaxel
Definition
Taxanes: stabilize microtubules and inhibit spindle apparatus
Term
Etoposide and Teneposide
Definition
Epipodophyllotoxins: stabilize the cleavable form of the TOPO II-DNA to induce DNA fragmentation
Term
Topotecan and Irinotecan
Definition
Camptothecins: binds to the TOPO I-DNA complex to prevent ligation of cleaved DNA strands to induce fragmentation of DNA
Term
Bleomycins
Definition
Antibiotic: induce fragmentation of DNA
Term
Anthracyclins
Definition
Antibiotic: intercalates with DNA to prevent replication and RNA synthesis; targets P450 to release ROS's; targets cell membrane
Term
Mechloroethamine (nitrogen mustard)
Definition
Alkylating agent: electrophilic aziridine ring invites nucleophilic attack by guanine and alkylation of DNA; induces cross-linking of DNA, nucleotide excision, and incorrect base pairing between guanine and thymine
Term
Nitrosoureas
Definition
Alkylating agent: alkylates guanines in DNA and carbamoylates lysines in proteins, inhibiting them
Term
Cisplatin
Definition
Platinum coordinating complex: cross-links DNA, leading to strand breakage and miscoding
Term
Tamoxifen
Definition
Selective estrogen receptor modulator: Antagonizes estrogen receptors in breast tissue (estrogen can stimulate breast tissue growth)
Term
Bicalutamide
Definition
Selective androgen receptor modulator: targets androgen receptors in prostate tissue
Term
Imatinib
Definition
Targets the bcr/abl, c-kit (CD117), PDGFRB, and PDGFRA tyrosine kinases to trigger apoptosis (cells die because of oncogenic addiction)
Term
Dasatinib and Nilotinib
Definition
Target the bcr/abl tyrosine kinase if cells become resistant to imatinib
Term
Sunitinib and sorafinib
Definition
Target the VEGF receptor kinase to prevent angiogenesis
Term
Vorinostat
Definition
Targets HDAC to prevent deacetylation of histones and enable transciption of tumor repressor genes
Term
Decitabine and azacytidine
Definition
DNA methyltransferase inhibitor; prevents methylation of tumor-supressor genes
Term
Bevacizumab
Definition
Monoclonal antibody that targets VEGF; prevents angiogenesis
Term
Trastuzumab
Definition
Targets the HER2/NEU (EGFR-2) receptor in breast tissue to prevent cell proliferation
Term
Rituxumab
Definition
Targets the CD20 receptor on B-cells (treats non-hodgekin's lymphoma)
Term
Cetuximab
Definition
Targets the EGFR-1 receptor
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