Background HIV-1 reverse transcriptase (HIV-1 RT) is an essential enzyme for the replication cycle of HIV. HIV-1 RT inhibitors have been extensively investigated for their antiHIV properties. However, emergence of HIV drug resistance and side effects are the main reasons for failure of anti-HIV therapy. The aim of the present study was to evaluate the HIV reverse transcriptase inhibitory activi...

Using standard and ultrasensitive techniques, we detected nonnucleoside reverse-transcriptase inhibitor-associated resistance mutations in 11 (20%) of 54 subjects who discontinued virologically suppressive nonnucleoside reverse-transcriptase inhibitor-containing antiretroviral therapy. Resistance was detected in 45% and 14% of subjects with a baseline human immunodeficiency virus type 1 RNA lev...

Plants of the genus Euphorbia have been investigated for different bioactive natural products. I have isolated several new and bioactive diterpenoids from different species of Euphorbia of Iran with myrsinane type skeleton. The structure of the compounds was determined using high resolution mass spectroscopy, 1 D and 2 D NMR spectral data. The stereochemistry of the diterpenoids was determined ...

A few analogues of atevirdine or 1-[(5-methoxyindol-2-yl) carbonyl]-4-[3- (ethylamino)-2-pyridyl] piperazine – an anti-HIV belonging to non-nucleoside reverse transcriptase inhibitors were synthesized and evaluated for anti-HIV activity. Replacement of indolyl moiety with 2-alkylthio-1-benzyl-5-imidazolyl substituent afforded 1-[2-(alkylthio-1-benzyl-5-imidazolyl) carbonyl]-4-[3-(isopropylamino...

X-ray crystallographic studies of human immunodeficiency virus type 1 reverse transcriptase complexed with or without substrates or inhibitors show that the heterodimeric enzyme adopts distinct conformations that differ in the orientation of the so-called thumb subdomain in the large subunit. Site-directed spin labelling of mutated residue positions W24C and K287C is applied here to determine t...

Hepatitis B virus polymerase plays a critical role during HBV life cycle, and polymerase/reverse transcriptase (RT) activities are critical for HBV-pol during viral replication. To investigate RT domain of human HBV polymerase, a 5’ end Polyhistidine tagged RT DNA (304-693 amino acids) of HBV-pol was successfully expressed in Escherichia coli. Recombinant RT was purified in native condition emp...

We have determined the nucleotide sequence of the Drosophila retrotransposon 1731. 1731 is 4648 bp long and is flanked by 336 bp terminal repeats (LTRs) previously described as being reminiscent of provirus LTRs. The 1731 genome consists of two long open reading frames (ORFs 1 and 2) which slightly overlap each other. The ORF 1 and 2 present similarities with retroviral gag and pol genes respec...

The spreading of HIV infection still is a serious epidemic disease in the Asia, including Thailand, especially by transmission from mother to child and resistant HIV strains causing the tolerant drug treatment. Therefore, discovery of a new drug is the hope for curing resistant strains which need atomic resolution structure of target protein, reverse transcriptase. In this paper, we reported th...

ZAM is an LTR-retrotransposon from Drosophila melanogaster that belongs to the genus errantivirus, viruses similar in structure and replication cycle to vertebrate retroviruses. A key component to its lifecycle is its reverse transcriptase which copies single-stranded genomic RNA into DNA. Here, we provide a detailed characterization of the enzymatic activities of the reverse transcriptase enco...

DNA polymerases from different evolutionary families [Vent (exo-) DNA polymerase from the B-family polymerases, Taq DNA polymerase from the A-family polymerases and HIV reverse transcriptase from the reverse transcriptase family] were examined for their ability to incorporate the sugar-modified cyclohexenyl nucleoside triphosphates. All enzymes were able to use the cyclohexenyl nucleotides as a...