Term
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Definition
| covalently bind to the enzymatic site fo penicillin-binding proteins to produce an irreversible inhibition of PG transpeptidase and thus prevent PG cell wall synthesis |
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Term
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Definition
| covalently bind to the enzymatic site fo penicillin-binding proteins to produce an irreversible inhibition of PG transpeptidase and thus prevent PG cell wall synthesis |
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Term
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Definition
| covalently bind to the enzymatic site fo penicillin-binding proteins to produce an irreversible inhibition of PG transpeptidase and thus prevent PG cell wall synthesis |
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Term
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Definition
| covalently bind to the enzymatic site fo penicillin-binding proteins to produce an irreversible inhibition of PG transpeptidase and thus prevent PG cell wall synthesis |
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Term
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Definition
| covalently binds the D-ala-D-ala terminus of the peptide side chain: this binding prevents the binding of the Dala-D-ala terminus to the enzymatic site of PG transpeptidase. Cell wall synthesis is hinibited |
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Term
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Definition
binding to the A site o the 30S subunit of the bacterial ribosome prevents the binding of the aminoacyl tRNA
protein synth is inhibitied |
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Term
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Definition
binding to the 50S subunit of the bacterial ribosome inhibits translocation of the most recently added amino acid from the A site to the P site:
protein synth is inh |
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Term
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Definition
| the same as macrolides, bind 50S subunit preventin A to P translocation |
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Term
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Definition
inhib of Topo II (DNA gyrase) and
topo IV prevents the relaxation of positively supercoiled DNA needed for replication and separation of the replicated chromosomal DNA required for cell division, respectively |
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Term
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Definition
| bind to the 30S subunit to block formation of the initiation complex, cause misreading of mRNA and break polysomes into non-funtional monosomes |
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Term
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Definition
binding to the
23S ribosomal RNA of the
50S subunit blocking the assemply of the 70s complex |
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Term
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Definition
| binding to the bacterial membranes causes depolarization, loss of membrane potential and cell death |
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Term
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Definition
sulfamethoxazole inhibits dihydropteroate synthetase blocking the synthesis of dihydrofolate(DHF), and trimethoprim inhibits dihydrofolate reductase(DHFR) blocking the synthesis of tetrahydrofolate(THF) is blocked
NB1: methotrexate also inhibits dihydrofolate reductase(DHFR), but can be overcome in non-tumor cells with leucovorin rescue.
NB2: No leucovorin rescue for 5-FU thymidylate synthetase inhibition. |
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Term
| pyrimethamine-sulfadiazine |
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Definition
sulfadiazine inhibits DHopteroate synthetase blocking the synthesis of dihydrofolate(DHF) and pyrimethamine blocks DHfolate reductase blocking the synthesis of tetrahydrofolate(THF)
NB: This is the same pathway inhibition as Trim-Sulfa, just with different drugs. |
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Term
| pyrimethamine-sulfadiazine |
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Definition
| sulfadiazine inhibits DHopteroate synthetase and pyrimethamine blocks DHfolate reductase: the synth of THF is blocked |
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Term
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Definition
| bacterial enzymes reduce nitrofurantoin to a highly reactive intermediate which damages bacterial DNA to cause cell death |
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Term
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Definition
after bioactivation by mycobacterial catalase-peroxidase, the active metabolite covalently binds to the acyl carrier protein and the B-ketoacyl carrier protein synthetase to:
"prevent the synthesis of mycolic acid" which is the major component of TB cell membranes
NB: this is the 'i' in S.H.I.P. drugs, which are more slowly inactivated/acetylated in certain races/people, leading to hepatotoxicity with this drug |
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Term
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Definition
| binding to the B-subunit(beta) of bacterial DNA-dependent RNA polymerase prevents RNA synthesis |
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Term
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Definition
| interferes with the synthesis of mycolic acid by affecting the gene for fatty acid synthase I |
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Term
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Definition
| inhibits arabinosyl transferase to prevent the polymerization of arabinoglycan, an essential component of the mycobacterial cell wall |
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Term
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Definition
| binds to the 30S subunit to block formation of the initiation complex, cause misreading of mRNA and break polysomes into non-functional monosomes |
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Term
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Definition
| binding to ergosterol in fungal cell membranes creates pores which increases the permeability of the cell wall: the loss of intracellular macromolecules and ions causes cell death |
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Term
| -azoles. e.g. fluconazole |
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Definition
| inhibition of CYP450 lanosterol 14alpha-demethylase blocks the synthesis of ergosterol |
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Term
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Definition
| inhibit cell wall synthesis by blocking the enzyme 1,3-beta-D-glucan synthetase: called penicillins for fungi |
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Term
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Definition
5-FC -> to 5-FU by fungi; 5-FU -> to RdUMP which blocks fungal thymidylate synthetase; lack of thymidine prevents DNA synthesis
NB: non-tumor cells cannot be saved with leucovorin like in methotrexate treatment |
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Term
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Definition
| fungistatic: binds to microtubules to prevent fungal mitosis |
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Term
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Definition
| fungicidal: block squalene-2,3-epoxidase to block ergosterol synthesis |
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Term
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Definition
| blocks the release fo new viral particles from infected cells via the inhibition of viral neuraminidase |
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Term
| acyclovir ganciclovir penciclovir |
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Definition
| all are converted to monophosphates by HSV and CMV kinases followed by conversion to triphosphates by host cell kinases: triphosphates inhibit viral DNA polymerase and result in "chain termination" |
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Term
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Definition
| an antisense oligonucleotide which binds viral mRNA and prevents its translation |
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Term
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Definition
converted to trifluridine triphosphate by host-cell kinases: the active metabolite inhibits viral DNA polymerases
chain terminator just like acyclovir, first phosphorylation step for these compounds occurs at higher rates in virus infected cells. |
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Term
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Definition
directly inhibits viral DNA polymerase
NB: used to treat CMV retinitis in AIDS patients, otherwise usually used topically for Herpes outbreaks |
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Term
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Definition
| concerted to trifluridine triphosphate by host cell kinases: the active metabolite inhibitis viral DNA polymerase |
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Term
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Definition
| blocks the fusion of the viral and T-cell membranes, so HIV cannot enter the CD4+ T cell |
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Term
zidovudine lamivudine abacavir tenofovir
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Definition
after conversion to "false" nucleotides (triphosphates) by intracellular kinaeses, these false nucleotides competitively inhibit HIV reverse transcriptase and their incorporation in to the DNA chain causes chain termination
NB: these are the NRTI's nucleoside analog reverse transcriptase inhibitors, all RTIs are chain terminators, when they are incorporated they block elongation of the growing DNA or RNA molecule |
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Term
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Definition
directly inhibit reverse transcriptase: they block RNA and DNA dependent polymerase
NB: these are the NNRTI's non-nucleoside reverse transcriptase inhibitors, all RTIs are chain terminators, when they are incorporated they block elongation of the growing DNA or RNA molecule |
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Term
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Definition
| blockade of the viral integrase prevents the insertion of viral DNA into human DNA |
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Term
saquinavir
ritonavir
lopinavir |
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Definition
| blockade of viral protease prevents the cleavage of viral polyproteins into the functional subunits needed to assemble new functional, infectious viral particles |
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Term
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Definition
| protozoal and bacterial ferredoxins reduce the nitro group to produce a highly-reactive radical which attacks DNA and destroys its helical structure; also causes DNA mutations |
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Term
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Definition
| interferes with pyruvate: ferrodoxin oxidoreductase-dependent electron transfer reaction |
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Term
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Definition
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