Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 19 of 19 for “"maraviroc"”.
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Mechanisms of CCR5 Agonist/Antagonist Inhibition of HIV-1 Entry and In Vitro Selection of Virus Resistant to Maraviroc
… of viruses resistant to the CCR5 antagonist maraviroc highlighted a novel mechanism of HIV-1 resistance to this type of inhibitor. Unlike previous studies, resistance was unrelated to changes in the V3 region of the glycoprotein. Rather, resistant virus harbored mutations in the CD4 binding …
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Effects of different antiretroviral treatments on gut microbiota of hiv-infected patients
… lesser HIV-related complications. In vitro, Maraviroc did not exert any bacteriostatic effect in the tested strains, and no significant effects were either found in gut microbiota composition when administered to mice fed a standard diet, while several and interesting actions were observed …
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Application of Genetically-Encoded Photoactivatable Crosslinkers to Map Ligand-Binding Sites on G Protein-Coupled Receptors
… structural biology data. A small molecule drug, maraviroc, photocrosslinked to multiple sites on CCR5 and the results were extended to develop a computer homology model of the CCR5-maraviroc complex. In summary, the application of a novel targeted cellbased photocrosslinking strategy provided …
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Diversity in APOBEC3 and CCR5 host genes and HIV-1 in a South African population
… CCR5 or CXCR4 co-receptors. Inhibitors, such as Maraviroc, which binds to CCR5 inhibiting entry of CCR5 utilizing viruses (R5 viruses), is currently reserved for salvage therapy in many countries including South Africa. In the course of HIV infection, CXCR4 utilizing viruses (X4 viruses) may …
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Dynamics of HIV coreceptors and their utilization by plasma and cerebrospinal fluid HIV-1 isolates
… use in late stage infection. A CCR5 antagonist (Maraviroc) is now available for the treatment of R5 HIV-1 infection. We found that pro- and anti-inflammatory substances oppositely regulate monocyte expression of two HIV coreceptors, CCR2 and BLT1. The findings provide information about the …
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Male genital tract versus blood HIV-1 compartmentalization and selection: the first step of the transmission bottleneck?
… were tested against HIV-1 entry inhibitors; Maraviroc, PSCRANTES, enfurvirtide (T-20) and JM2987. Maraviroc and PSC-RANTES are CCR5 inhibitors while JM2987 is a CXCR4 inhibitor. Enfurvirtide (T-20) is a fusion inhibitor blocking the virus from entering cells. The full-length clones used to …
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Single Molecule Ligand Binding Studies on CCR5 by Fluorescence Cross-Correlation Spectroscopy
… HIV particles to infect T cells. Currently, maraviroc is the only Food and Drug Administration (FDA) approved entry inhibitor for HIV-1 but resistance to maraviroc has been reported indicating the need for novel entry inhibitors. Recently, four peptides derived from RANTES (Regulated on …
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DEVELOPMENT OF ANTAGONISTS TARGETING CHEMOKINE RECEPTOR CCR5 AND THE CHEMOKINE RECEPTOR CCR5 – MU OPIOID RECEPTOR HETERODIMER
… for neuroAIDS where the known treatment, maraviroc, is less efficacious and fails to inhibit virus entry in the presence of morphine. Both projects illustrate the roles that CCR5 plays in these two unique diseases.
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Distinct Patterns of Ccr5 Versus Alternative Coreceptor Dependence in Non-Natural Host Versus Natural Host Simmian Immunodeficiency Virus Infection
… poor coreceptor of SIV. Using CCR5 antagonist Maraviroc to block CCR5-mediated infection in primary peripheral blood mononuclear cells (PBMCs), I determined that SIV were highly CCR5-dependent in rhesus macaque PBMCs, whereas SIV were partially CCR5-independent in sooty mangabey PBMCs, …
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Characterisation of HIV-1 Envelope features of breakthrough infections from the CAPRISA 004 Microbicide Trial
… using the following inhibitors: tenofovir, maraviroc, T20, PSC-RANTES and anti-CD4 antibody clone SK3. In addition, envs for 19 participants were cloned and used to generate pseudoviruses which were evaluated for entry efficiency. Viral isolates were identical or very similar to viruses in …
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Bioorthogonal Tethering of Drug Fragments to Engineered G Protein-Coupled Receptors
… near an allosteric binding site for the drug maraviroc (mvc). Molecular dynamics simulations were used to design heterobifunctional mvc analogues consisting of a drug fragment connected by a flexible linker to a reactive moiety capable of undergoing a bioorthogonal coupling reaction with the …
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Antiretroviral drugs differentially modulate glucocorticoid activity via the glucocorticoid receptor in vitro
… disoproxil fumarate (TDF), dapivirine (DPV), and maraviroc (MVC) on activation of the GR and GR-regulated mRNA expression were investigated, in the absence and presence of select GR ligands. The effects of TDF and DPV on GR protein levels and phosphorylation were also determined. The inhibitory …
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Characterisation of functional properties of Envelopes of highly neutralisation resistant HIV-1 isolates
… between susceptibility to the entry inhibitors Maraviroc and PSC RANTES (CCR5 antagonists) and the fusion inhibitor T20 and resistance, indicating that neutralisation resistance did not alter inhibitor target sites. Based on our findings, it is clear that reduced entry efficiency does not …
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Implementation of Solution and Solid Sate Nuclear Magnetic Resonance (NMR) Spectroscopic Techniques for Quantitative and Qualitative Analysis of Molecular Species
… then applied to study the real-time release of maraviroc from a microparticle formulation in a vaginal and seminal stimulated environment. Different possibilities were discussed to control the release profile such as the crosslinking process and a pH sensitive polymer. In chapter 5, the project …
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Developments and applications of methods for palladium- and copper-catalyzed carbon-nitrogen bond formation
… as demonstrated by the efficient synthesis of Maraviroc and the formal synthesis of other pharmaceutical agents including DMP 777, Rasagiline, Dapoxetine and Bifemelane.
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Development of Closomer And MIBG based Nanoformulation: Application to HIV Prevention and Neuroblastoma Therapy
… real time quantification and in vitro release of maraviroc (MVC) – a first in its class FDA approved HIV entry inhibitor. The calibration assay produced a linearity curve in concentration range (0.42 mg/ml – 15 mg/ml), and the limits of detection and quantification values were 0.97 mg/ml and 2.93 …
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Investigate the effect of Bacterial Vaginosis-associated bacteria on the efficacy of Anti-HIV therapy
… of TFV, tenofovir disoproxil fumarate (TDF), maraviroc (MVC) and abacavir (ABC) to G. vaginalis reduced extracellular ARV drug concentrations to a level unable to inhibit HIV infection and to determine whether L. crispatus was able to counteract this effect. G. vaginalis and L. crispatus were …
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Investigate the effect of Bacterial Vaginosis-associated bacteria on the efficacy of Anti-HIV therapy
… of TFV, tenofovir disoproxil fumarate (TDF), maraviroc (MVC) and abacavir (ABC) to G. vaginalis reduced extracellular ARV drug concentrations to a level unable to inhibit HIV infection and to determine whether L. crispatus was able to counteract this effect. G. vaginalis and L. crispatus were …
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Modulation of the progesterone receptor by progestogens, antiretroviral drugs and the glucocorticoid receptor
… disoproxil fumarate (TDF), dapivirine (DPV) and maraviroc (MVC), was investigated next using promoter-reporter assays and real-time qPCR in MDA-PR-B+ cells. The mechanism of ARV action on PR-B activity was investigated by competitive binding assays, as well as by determination of PR …