A series of N-aryl heteroarylisopropanolamines in which an indole or a 3-arylpyrrole moiety was linked to an aryl group through an isopropanolamine linker, were designed and synthesized as potential anti-HIV-1-PR agents. Series was tested for their ability in blocking PR activity. As a rule, indole derivatives of class 1 exhibited more potency than pyrrole analogues of class 2 while tert-butyla...

The TRUGENE HIV-1 Genotyping Kit and OpenGene DNA Sequencing System are designed to sequence the protease (PR)- and reverse transcriptase (RT)-coding regions of human immunodeficiency virus type 1 (HIV-1) pol. Studies were undertaken to determine the accuracy of this assay system in detecting resistance-associated mutations and to determine the effects of RNA extraction methods, anticoagulants,...

The study aimed at defining protease (PR) resistance mutations associated with darunavir (DRV) failure and PR resistance evolution at DRV failure, in a large database of HIV patients. Overall, 1104 patients were included: only 118 (10.7%) failed at a median observation time of 16 months. The mean number of PR mutations at baseline was 2.7, but it was higher in patients who subsequently failed D...

HIV-1 protease (PR) is encoded by pol, which is initially translated as a Pr160gag-pol polyprotein by a ribosomal frameshift event. Within Gag-Pol, truncated p6gag is replaced by a transframe domain (referred to as p6* or p6pol) located directly upstream of PR. p6* has been proposed as playing a role in modulating PR activation. Overlapping reading frames between p6* and p6gag present a challen...

Previous studies demonstrated that blacks have less coronary artery calcification (CAC) than whites. We evaluated racial differences in plaque composition and stenosis in the Multicenter AIDS Cohort Study. HIV-positive and HIV-negative men underwent noncontrast cardiac computed tomography (CT) if they were aged 40 to 70 years, weighed <136 kg, and had no history of cardiac surgery or revascular...

One of the current pathways to develop inhibitors that target different steps in the life cycle of the human immunodeficiency virus (HIV) is blocking the function of the HIV-related proteins such as HIV-1 integrase (HIV-1 IN), HIV-1 reverse transcriptase (HIV-1 RT) and HIV-1 protease (HIV-1 PR), which are essential proteins that control the ability of HIV to infect cells, produce new copies of ...

OBJECTIVES To determine the prevalence and correlates of herpes simplex virus type 2 (HSV-2) seropositivity among fishermen along the shores of Lake Victoria in Kisumu district, Kenya. METHODS Sera from a random sample of 250 fishermen from 18 beaches were collected after a detailed sociodemographic interview. HSV-2 infection was tested by Kalon HSV-2 ELISA. RESULTS The HSV-2 seroprevalence...

Treatment of human immunodeficiency virus (HIV) type 1 (HIV-1)-infected individuals with antiretroviral (ARV) drugs is highly effective in inhibiting viral replication, increasing both the duration and the quality of life (71). Regimens consisting of combinations of protease (PR), reverse transcriptase (RT), and fusion inhibitors are the current standard of care and typically reduce the circula...

The conformational landscape of HIV-1 protease (PR) can be experimentally characterized by pulsed-EPR double electron-electron resonance (DEER). For this characterization, nitroxide spin labels are attached to an engineered cysteine residue in the flap region of HIV-1 PR. DEER distance measurements from spin-labels contained within each flap of the homodimer provide a detailed description of th...

The genome of human immunodeficiency virus type 1 (HIV-1) encodes 15 distinct proteins, three of which provide essential enzymatic functions: a reverse transcriptase (RT), an integrase (IN), and a protease (PR). Since these enzymes are all homodimers, pseudohomodimers or multimers, disruption of protein-protein interactions in these retroviral enzymes may constitute an alternative way to achiev...