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22 Cards in this Set
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- 3rd side (hint)
Mycophenolic acid
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--IMPDH inhibitor
- recall we needed this to convert IMP to XMP -> GMP - B/T Lymphocytes require GTP for proliferation - thus we can use this drug as an Immunosupressant drug - binds to Active site of IMPDH to make stacking interaction with IMP - blocks hydrolysis of the thioimdiate ester |
IMPDH Inhibitor
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Sulfa drug
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inhibit bacterial synthesis of dihydrofolate (DHF)
- mimic p-aminobenzoic acid - block THF synthesis - can kill bacteria without affecting mammals |
Inhibits dihydrofolate synthesis
DHF |
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Methotrexate
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-- DHFR inhibitor
- childhood leukemia - anticancer |
DHFR inhibitor
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Allopurinol
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Xanthine Oxidase Inhibitor
- Treats: Gout and Lesch-Nyhan (maybe) - lowers uric acid production |
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5-Flourouracil
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thymidylate synthase inhibitor
- recall we needed the synthase to make dUMP -> dTMP - F similar size to H but electronegative - rxn stops after Ternary complex - SUICIDE inhibition (irreversible/mechanism inhibition) |
Thymidylate synthase inhibitor
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Capecitabine
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Thymidylate synthase inhibitor, prodrug of 5-FU
(antimetabolite) - aka Xeloda - treats colon/breast cancer - good substrate for Thymidine phosphorylase |
Thymidylate synthase inhibitor
prodrug of 5-FU Antimetabolite |
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Gemcitabine
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inhibitor of ribonucleotide reductase
Antimetabolite - aka Gemzar - Inhibit DNA elongation - leads to depletion of dNTP - long intracellular half life - treats: solid tumors (pancreatic/lung cancers) |
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Decitabine
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DNA methyltransferase inhibitor
Antimetabolite - aka Dacogen - suicide inhibitor - first epigenetic chemotherapy - activate silenced genes p15/16 - treats: myelodysplastic syndromes |
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AZT
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HIV reverse transriptase inhibitor
replaces 3’-OH with N3 blocks DNA elongation Antimetabolite? |
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Topotecan:
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“posion” of topoisomerase
Antimetabolite? stabalizes the cleavage complex of topo. - prevents religation - intercalates b/w -1/+1 Base |
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Novobiocin
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Catalytic inhibitor of topoisomerase
Antimetabolite stabalizes the cleavage complex of topo. - prevents religation - intercalates b/w -1/+1 Base |
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(Nitrogen) Mustard
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bisalkylating agent, DNA crosslinker
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Cisplatin
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bisalkylating agent
DNA crosslinker - chemotherapeutic - trans form is inactive - treat: ovarian carcinoma, lung/neck cancer - inhibits DNA replication Psoralen |
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Psoralen
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photoactivated DNA crosslinker
treats: psoriasis - intercalates (slips between) - TT Dimers when hit UV-A |
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Mytomycin C
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bifunctional DNA crosslinker
requires reductive activation kill bacteria - bind to 5'CG sequence - disrupts DNA and RNA synthesis |
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Aromatic amine
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metabolically activated alkylator
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Benzopyrene
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metabolically activated alkylator
one of most potent carcinogens known - scrotal cancer among chimney sweeps - olefin expoxidation and epoxide hyrolysis |
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Aflatoxin B1
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metabolically activated alkylator
potent liver carcinogen - contaminated peanuts - N7 adduct on Guanine -> abasic site |
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Acrylamide
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metabolically activated alkylator
-neurotoxic carcinogen in fries - temp 120+ -> glucose and aspargine react to form -> acrylamide -> metabolized by P-450 -> glycidamide (DNA Alkylator) |
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Temozolomide
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O6-MeG
methylating agent monoalkylating agent - O6-MeG (DNA Damaging Drug) - first gen. anticancer drug - treats brain tumors - success from diff in pH |
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Anthramycin;
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monoalkylating agent
(DNA Damaging drug) - antitumor antibiotic - belong to pyrrol[1,4] benzodiazepine - binds minor groove DNA -> forms adduct with N2 of Guanine |
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Calicheamycin
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induces DNA strand break via diradical mechanism
not alkylator (DNA Damaging Drug) - aka Mylotarg - potent antitumor antibiotic - Bergman cyclization - minor groove selective (TCCT) |
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