integrase


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integrase

(ĭn′tĕ-grās)
A retroviral enzyme that incorporates DNA derived from the virus into host cell chromosomes. The enzyme is a target for experimental antiretroviral therapies.
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In the ATLAS study, 616 participants taking two nucleoside reverse transcriptase inhibitors (NRTIs) and an integrase inhibitor, a non-NRTI, or a protease inhibitor, were randomized 1:1 to continue their regimen (CART arm) or switch to CAB/RPV, following a 4-week safety monitoring period of oral CAB/RPV After 48 weeks, 1.6% in the CAB/RPV arm and L0% in the CART arm had HIV-1 RNA greater than or equal to 50 copies/mL, which met the prespecified noninferiority margin.
The HIV drug TDF can be replaced by a similar but safer drug, and the integrase inhibitors are seeing more use in many places.
Fragment R4' in pPV989-94 encodes 11 genes that span from the phage integrase (ORF38) to PQQ-dependent catabolism-associated beta-propeller protein (HET-E-1, ORF22) in R4 and is 10.7 kb in length (Figure 2).
Currently dolutegravir (DTG) in combination with either abacavir (ABC) or rilpivirine (RPV) and the investigational integrase inhibitor cabotegravir (CAB) in combination with RPV are being studied in 2-drug regimens.
The integrase inhibitor, elvitegravir, requires boosting with the CYP3A inhibitor, cobicistat, and should be taken with food.
Integrase strand inhibitors (INSTI) are the newest class of antiretroviral (ARV) therapies to treat human immunodeficiency virus (HIV) infection.
Three pair primers were used to obtain the converse regions sequence of the three classes integrase genes respectively while the variable region of the integrons were determined with another pair primers.14 Using the internal primers for the class 2 integrase gene amplification reaction to detect the presence of class 2 integron was carried out as previously described.8 All primers are listed in Table-I.
Pol gene also encodes for a polyprotein which has similar fate like Gag-poly-protein as it is also cleaved by viral protease into three different proteins: reverse transcriptase, protease, and integrase, whereas the Env gene encodes for a single glycoprotein (gp160) which later is cleaved into two proteins: surface glycoprotein gp120 and transmembrane protein gp41.
The once-daily drug, which belongs to a novel class known as integrase inhibitors that block the virus causing AIDS from entering cells, is owned by ViiV Healthcare, a joint venture that is focused on HIV and in which GSK is the largest shareholder.
29 October 2012 a[euro]" Japanese pharmaceutical company Shionogi & Company Ltd (TYO:4507) will take a 10% stake in UK-based HIV drugs maker ViiV Healthcare Ltd in exchange for the transfer of the rights to the HIV integrase inhibitor portfolio of the firms' joint venture to ViiV Healthcare, the companies said.
The topics include advances in the diagnosis of respiratory tract infections, best practice example of pharmaceutical industry's engagement in the fight against malaria, the first oxazolidinone antibacterial agent, the discovery and development of rivaroxaban, and the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium.