Difference Between Nucleoside and Nucleotide Reverse Transcriptase Inhibitors

The major difference between them is that the nucleosides need to be phosphorylated by cellular kinases. The enzyme reverse transcriptase recognizes them as regular nucleotides and inserts them into the newly synthesized DNA chain.

1. What are nucleotide reverse transcriptase inhibitors?
2. What is the difference between nucleoside and non-nucleoside?
3. Is tenofovir a nucleoside or nucleotide?
4. Which drugs are nucleoside reverse transcriptase inhibitors?
5. How does nucleoside reverse transcriptase inhibitors work?
6. Do humans have reverse transcriptase?
7. What does Nrti mean?
8. How do NRTIs and NNRTIs work?
9. What is the mechanism of action of the nucleoside transcriptase inhibitors NRTIs?

What are nucleotide reverse transcriptase inhibitors?

The nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) were the first class of antiretroviral drugs to be approved by the FDA. NRTIs are taken as prodrugs and must be taken into the host cell and phosphorylated before they become active. Once inside the host cell, cellular kinases will activate the drug.

What is the difference between nucleoside and non-nucleoside?

NNRTIs are chemically distinct from nucleosides and, unlike the NRTIs, do not require intracellular metabolism for activity. In general, NNRTIs are a group of small (<600 Da) hydrophobic compounds with diverse structures that specifically inhibit HIV-1 RT, but not HIV-2 RT (De Clercq, 1998).

Is tenofovir a nucleoside or nucleotide?

Tenofovir, a novel nucleotide analog, belongs to the class of acyclic nucleoside phosphonates. Tenofovir is phosphorylated in situ to the virologically active tenofovir diphosphate. Tenofovir diphosphate inhibits human immunodeficiency virus (HIV-1 and HIV-2) DNA polymerases.

Which drugs are nucleoside reverse transcriptase inhibitors?

Available NRTIs

• zidovudine (Retrovir)
• lamivudine (Epivir)
• abacavir sulfate (Ziagen)
• didanosine (Videx)
• delayed-release didanosine (Videx EC)
• stavudine (Zerit)
• emtricitabine (Emtriva)
• tenofovir disoproxil fumarate (Viread)

How does nucleoside reverse transcriptase inhibitors work?

Nucleoside reverse transcriptase inhibitors (NRTIs) block reverse transcriptase (an HIV enzyme). HIV uses reverse transcriptase to convert its RNA into DNA (reverse transcription). Blocking reverse transcriptase and reverse transcription prevents HIV from replicating.

Do humans have reverse transcriptase?

In cellular life

They are found abundantly in the genomes of plants and animals. Telomerase is another reverse transcriptase found in many eukaryotes, including humans, which carries its own RNA template; this RNA is used as a template for DNA replication. ... In order to initiate synthesis of DNA, a primer is needed.

What does Nrti mean?

Definitions of NRTI. noun. an antiviral drug used against HIV; is incorporated into the DNA of the virus and stops the building process; results in incomplete DNA that cannot create a new virus; often used in combination with other drugs. synonyms: nucleoside reverse transcriptase inhibitor.

How do NRTIs and NNRTIs work?

NNRTIs work by binding to the HIV enzyme called reverse transcriptase, which is essential to the viral replication process, and therefore blocking HIV from making copies of itself. Dapivirine is an example of an NNRTI. NRTIs work by mimicking nucleotides that are the building blocks of viral DNA.

What is the mechanism of action of the nucleoside transcriptase inhibitors NRTIs?

Nucleoside Reverse Transcriptase Inhibitors (NRTIs) inhibit reverse transcription by causing chain termination after they have been incorporated into viral DNA. For these drugs to be active they need to be phosphorylated intracellularly. This was the first group of antiretroviral agents to be used against HIV.