- Nucleoside analogue
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Nucleoside analogues are a range of antiviral products used to prevent viral replication in infected cells. The most commonly used is Acyclovir, although its inclusion in this category is uncertain, as it contains only a partial nucleoside structure, as the sugar ring is replaced by an open-chain structure.
Contents
Function
These agents can be used against hepatitis B virus, hepatitis C virus, herpes simplex, and HIV. Once they are phosphorylated, they work as antimetabolites by being similar enough to nucleotides to be incorporated into growing DNA strands; but they act as chain terminators and stop viral DNA Polymerase. They are not specific to viral DNA and also affect mitochondrial DNA. Because of this they have side effects such as bone marrow suppression.
There is a large family of nucleoside analogue reverse transcriptase inhibitors, because DNA production by reverse transcriptase is very different from normal human DNA replication, so it is possible to design nucleoside analogues that are preferentially incorporated by the former. Some nucleoside analogues, however, can function both as NRTIs and polymerase inhibitors for other viruses (e.g., hepatitis B). Less selective nucleoside analogues are used as chemotherapy agents to treat cancer.
Resistance
Resistance can develop quickly with as little as one mutation.[citation needed] Mutations occur in the enzymes that phosphorylate the drug to activate it.
Examples
Nucleoside analogue drugs include:
- deoxyadenosine analogues
- Didanosine (ddI)(HIV)
- Vidarabine (chemotherapy)
- deoxycytidine analogues
- Cytarabine (chemotherapy)
- Emtricitabine (FTC)(HIV)
- Lamivudine (3TC)(HIV, hepatitis B)
- Zalcitabine (ddC)(HIV)
- deoxyguanosine analogues
- (deoxy-)thymidine analogues
- Stavudine (d4T)
- Telbivudine (hepatitis B)
- Zidovudine (azidothymidine, or AZT)(HIV)
- deoxyuridine analogues
Related drugs are nucleobase analogues such as Aciclovir and nucleotide analogues.
See also
- For nucleoside analogues in biology, see Nucleic acid analogues
DNA virus antivirals (primarily J05, also S01AD and D06BB) Baltimore I DNA-synthesis
inhibitorTK activatedguanine (Aciclovir#/Valacyclovir, Ganciclovir/Valganciclovir, Penciclovir/Famciclovir)
adenine (Vidarabine)Not TK activatedOtherImiquimod/Resiquimod • PodophyllotoxinHepatitis B (VII) Nucleoside analogues/NARTIs: Entecavir • Lamivudine • Telbivudine • Clevudine
Nucleotide analogues/NtRTIs: Adefovir • TenofovirMultiple/general Nucleic acid inhibitorsMultiple/unknownErbB2/PI3K PathwayNOV-205§ • NOV-002†#WHO-EM. ‡Withdrawn from market. Clinical trials: †Phase III. §Never to phase III This antiinfective drug article is a stub. You can help Wikipedia by expanding it. - deoxyadenosine analogues