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Antifolates act primarily as inhibitors of both RNA and DNA, and are often grouped with nucleic acid inhibitors in textbooks. However, they also act indirectly as protein synthesis inhibitors (because tetrahydrofolate is also involved in the synthesis of amino acids serine and methionine), so they are sometimes considered as their own category, antimetabolites. [6]
Nucleoside analog reverse-transcriptase inhibitors (NARTIs or NRTIs) compose the first class of antiretroviral drugs developed. In order to be incorporated into the viral DNA, NRTIs must be activated in the cell by the addition of three phosphate groups to their deoxyribose moiety, to form NRTI triphosphates.
[23] [24] It was developed by the synthesis and broad spectrum antiviral activity of 2,3-dihydroxypropyladenine. [24] Tenofovir DF was the first nucleotide reverse-transcriptase inhibitor approved by the FDA for the treatment of HIV-1 infection in October 2001. [18] [23]
It is nonenzymatically cleaved to mercaptopurine, a purine analogue that inhibits DNA synthesis. By preventing the clonal expansion of lymphocytes in the induction phase of the immune response, it affects both cell immunity and humoral immunity .
DON is a cytotoxic inhibitor of many enzymes of nucleotide synthesis. It could be shown in vitro that DON treatment led to apoptosis, or programmed cell death. Different pathways were investigated; it could be shown that the inner mitochondrial membrane was damaged, [14] and that single strand DNA breaks occurred. [15]
Pages in category "Nucleoside analog reverse transcriptase inhibitors" The following 21 pages are in this category, out of 21 total. This list may not reflect recent changes .
There are two classes of drugs that target the HIV-1 RT enzyme, nucleoside/nucleotide reverse-transcriptase inhibitors (NRTIs/NtRTIs) and non-nucleoside reverse-transcriptase inhibitors (NNRTIs). Drugs in these classes are important components of the HIV combination therapy called highly active antiretroviral therapy, better known as HAART.
There are three known classes of NS5B inhibitors: non-nucleoside analogue inhibitors, nucleoside/nucleotide analogue inhibitors, and pyrophosphate analogues. [2] The classes differ in their structure and where they bind to the NS5B protein: at allosteric binding sites, the enzyme active site, or the pyrophosphate binding site, respectively. [13]
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