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Ibuprofen (NSAID)
inhibits COX-1 and COX-2 and therefore prostaglandin synthesis? only S-isomer is biologically active
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Cisplatin
DNA crosslinking agent, chemotherapeutic agents
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Etoposide
topoisomerase inhibitor, induces ds DNA breaks
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Methotrexate
Anti-metabolite that inhibits enzymes involved in nucleoside production
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AZT
targets activity of DNA pols (inhibits elongation), AZT commonly used in HIV therapy
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Cytoxan
Alkylating agents
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Rifampin
binds prok RNA pol, for TB
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Actinomycin D/Dactinomycin D
binds DNA template and interferes is RNA pol progression (also used in tumor therapy), antibiotic
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5-aza-2�-deoxycytidine (decitabine)
(Rett treatment)nucleoside analog that inhibits DNMTs by trapping them in a covalent complex on DNA by preventing the beta-elimination step of catalysis�resulting in the enzymes� degradation�to be active, must be incorporated into genome of cell�also toxin to bone marrow
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Tetracycline
bacterial ribosome A site
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Streptomycin
Bacterial 30S sub-unit (blocks initiation)
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Erythromycin
Bacterial 50S subunit (blocks translocation)
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Chloramphenicol
bacterial peptidyl transferase
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Puromycin
Premature termination
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Cyclohexamide
Euk 80S ribosome
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Aspirin-(ASA)
Irreversibly acetylates and inactivates COX-1 at serine residue
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Tysabri (natalizumab)
Monoclonal antibody designed to block integrin function and prevent leukocytes from crossing the blood brain barrier
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Ceredase and Cerenzyme
expensive enzyme replacement therapy for Gaucher�s
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Etanercept
a fusion protein for treatment of RA, fuse to IgG1 to allow for secretion-perturbs TNFalpha pathway, involved in inflammation
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D-tubocurarine
a nonpolarizing blocker of Ach
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Taxol (Paclitaxel)
for treatment of lung, ovarian, breast, head and neck cancer. Hyperstabilizes MT by binding to B-tubulin and preventing dynamic instability
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Vinca alkaloids (vinblastine and vincristine)
used in treatment of leukemia and lymphoma, binds to tubulin dimers to inhibit their assembly
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Colchicine
used for treatment of gout, studied for anti-cancer drug, however extremely toxin. High affinity for tubulin and prevents polymerization
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Mebendazole (MT drug)
Worms
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Griseofulvin Antifungal
(binds to fungal MTs)
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Farnesyl transferase inhibitors (ftis)
originally studied for cancer, but now used as treatment for Progeria (premature aging caused by defect in nuclear lamin, type 5 intermediate filament, causes nuclear wrinkling)
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Imatinib/Gleevec
inhibits ATP binding and therefore cascade inhibited and you don�t get BCR-ABL protein, not as specific, will work against GIST (c-KIT tyrosine kinase receptor)�can develop resistance (possibly because of P loop mutation)
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Nilotinib(Tasigna)
more specific than Imatnib and well tolerated by patients, now treatment for Ph+ CML or if pt is resistant to Imatinib
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Trastuzamab (Herceptin)
used for pts with advanced breast cancer. Targets HER2 extracellular domain. Can work by blocking dimerization, or targeting the immune system to inhibit/kill overexpressing HER2 cells, or by allosterically blocking the ligand binding site
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Lapatinib
binds to intracellular domain of HER2, helps with inflammatory breast cancer
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