Based on an established common pharmacophore of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNTTIs), a series of quinolin-2-one derivatives were synthesized and assayed for their in vitro activities against HIV-1 reverse transcriptase (RT) for
Pi Cheng +6 more
doaj +1 more source
Sensitive detection systems for infectious agents in xenotransplantation*
Abstract Xenotransplantation of pig cells, tissues, or organs may be associated with transmission of porcine microorganisms, first of all of viruses, to the transplant recipient, potentially inducing a disease (zoonosis). I would like to define detection systems as the complex of sample generation, sample preparation, sample origin, time of sampling ...
Joachim Denner
wiley +1 more source
Evolution of lamivudine resistance in human immunodeficiency virus type 1-infected individuals:the relative roles of drift and selection [PDF]
Human immunodeficiency virus type 1 (HIV-1) rapidly develops resistance to lamivudine during monotherapy, typically resulting in the appearance at position 184 in reverse transcriptase (RT) of isoleucine instead of the wild-type methionine (M184I) early ...
Frost, SDW +4 more
core +1 more source
Adaptation to Different Human Populations by HIV-1 Revealed by Codon-Based Analyses [PDF]
Several codon-based methods are available for detecting adaptive evolution in protein-coding sequences, but to date none specifically identify sites that are selected differentially in two populations, although such comparisons between populations have ...
Gravenor Michael B +18 more
core +2 more sources
Selected Milestones in Antiviral Drug Development
This review article will describe the (wide) variety of approaches that I envisaged to develop a specific therapy for viral infections: (i) interferon and its inducers, (ii) HSV, VZV and CMV inhibitors, (iii) NRTIs (nucleoside reverse transcriptase ...
Erik De Clercq
doaj +1 more source
Investigational reverse transcriptase inhibitors for the treatment of HIV [PDF]
While considerable advances have been made in the development of antiretroviral agents, there is still work to be done. Reverse transcriptase inhibitors are important drugs for the treatment of HIV, and considerable research is currently ongoing to develop new agents and to modify currently existing agents.Herein, the authors discuss both ...
Theodore J, Cory +3 more
openaire +2 more sources
Characterizing the emergence and persistence of drug resistant mutations in HIV-1 subtype C infections using 454 ultra deep pyrosequencing. [PDF]
BACKGROUND: The role of HIV-1 RNA in the emergence of resistance to antiretroviral therapies (ARTs) is well documented while less is known about the role of historical viruses stored in the proviral DNA. The primary focus of this work was to characterize
Grace P McCormack +29 more
core +2 more sources
Background The recently approved anti-AIDS drug rilpivirine (TMC278, Edurant) is a nonnucleoside inhibitor (NNRTI) that binds to reverse transcriptase (RT) and allosterically blocks the chemical step of DNA synthesis.
Johnson Barry C +11 more
doaj +1 more source
Strategies in the Design and Development of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
AIDS (acquired immunodeficiency syndrome) is a potentially life-threatening infectious disease caused by human immunodeficiency virus (HIV). To date, thousands of people have lost their lives annually due to HIV infection, and it continues to be a big ...
Murugesan Vanangamudi +3 more
doaj +1 more source
Nucleoside reverse transcriptase inhibitors and HIV mutagenesis [PDF]
Potent antiretroviral therapy (ART) of HIV-1 infection with anti-retroviral drugs consisting of nucleoside reverse transcriptase inhibitors(NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs)and protease inhibitors (PIs) has dramatically reduced the rate ofHIV- and AIDS-related morbidity and mortality. The lack of patientcompliance to drug
Nancy A, Jewell +3 more
openaire +2 more sources

