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 20 of 28 for “"HIV Protease"”.
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Nutrient Transporter targeted Delivery of HIV Protease Inhibitors
HIV/AIDS has become one of the greatest threats to human health. Although inclusion of protease inhibitors (PIs) in HAART has greatly slowed the disease progression and improved the outcome of clinical treatment, the eradication of HIV/AIDS remains as a major medical challenge. Saquinavir (Saq) is …
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Design and Construction of an Anti-HIV Protease Transducer
Current therapies against HIV, mainly the highly active anti-retroviral therapy (HAART), concentrate on reducing the viral load and recovering CD4 levels, however they are faced with a rebound of HIV levels on cessation of therapy. Also of concern is the number of reports on resistance to such …
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Autodocking Studies of Oxygenated Fullerenes as Inhibitors of The HIV Protease
… of C60O1-8, were shown to inhibit activities of HIV-Protease with IC50 (concentration for 50% inhibition) of 1 mg/mol in the in-vitro studies. The oxygenated fullerenes were shown to have epoxide, ketones, and hydroxyl functionalities. As expected, C60 interacted with ozone with alkene …
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HIV Protease Inhibitors Trigger Lipid Metabolism Dysregulation Through Endoplasmic Reticulum Stress and Autophagy
<p>HIV protease inhibitors (PI) are core components of Highly Active Antiretroviral Therapy (HAART). HIV PIs are extremely effective at suppressing viral load, but have been linked to lipodystrophy and dyslipidemia, which are major risk factors for cardiovascular disease. Recent studies indicate …
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Prodrug Approach to Improve Oral and Brain Absorption of HIV Protease Inhibitor, Lopinavir
The main objective of this project is to develop prodrug strategies to circumvent efflux pumps such as P-glycoprotein (P-gp) and multidrug resistance associated proteins (MRPs), thereby enhancing oral and brain absorption of lopinavir (LPV). Oral absorption of LPV is severly limited due to low …
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What can't be cured must be endured: Optimisation of HIV Protease Inhibitor-Containing Antiretroviral Therapy
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Identification of HIV protease mutants with improved specificities toward an Alzheimer's Disease associated peptide sequence
We have developed the first protease specificity engineering technology intended to serve as a general-purpose source of target-specific protease mutants with potential therapeutic applications. We used this E. coli-based screening system to isolate multiple HIV protease mutants with improved …
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Identification of features contributing to binding promiscuity of small-molecule inhibitors for rapidly mutating targets
HIV infection has become a persistent worldwide epidemic despite the continuous development of novel inhibitors. A key challenge in combating HIV and other pandemic viral infections is the ability of the virus to mutate at an enormous rate and rapidly develop resistance to existing drugs. Among the …
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Computational engineering of small molecules to treat infectious diseases
… clinical failures of current therapies. We use HIV protease as a model system to understand mutation resistance. HIV protease substrates are unaffected or only moderately affected by resistance mutations that greatly decrease inhibitor binding. This idea has led to the design of broadly binding …
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Discovery and development of novel antifungal agents for the treatment of Candida auris infections
… antifungals. This screening revealed that HIV protease inhibitors, such as lopinavir, atazanavir, saquinavir and ritonavir, significantly enhanced the antifungal activity of azoles (fluconazole, voriconazole, itraconazole, and posaconazole) and polyene (AmB). Mechanistic studies showed that …
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Development of a Modular Anti-HIV Transducer Protein
… (cART) suppresses Human Immunodeficiency Virus (HIV) infection and allows restored long-term health in people living with the HIV. Current treatment provided infection management but not a complete cure. In the absence of treatment, virus level rebound due to the latent reservoir of the virus in …
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Delaunay-Laguerre Geometry For Macromolecular Modeling And Implicit Solvation
… continuum mechanics to study the motion of the HIV protease dimer.
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Design and synthesis of substituted cyclopropanes as conformationally restrained dipeptide mimics
… the bound conformation of inhibitors. The HIV-1 protease has been the subject of several recent X-ray crystallographic studies, so the general topography of bound HIV-1 protease inhibitors is well established. In addition, numerous HIV protease inhibitor and substrate binding studies have …
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Disubstituted BIS-THF moieties as new P2 ligands in nonpeptidal HIV-1 protease inhibitors
HIV-1 protease inhibitors (PIs) remain a powerful tool in the battle against HIV. The recently approved nonpeptidal HIV-protease inhibitor darunavir has been reported to be highly active against the wild-type virus as well as against a series of mutant strains. A rigid bis-tetrahydrofuran (bis-THF) …
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Synthesis of proteasome inhibitors: analogues of nelfinavir
… been found to be a very successful nonpeptidic HIV-protease inhibitor. According to a previous investigation, nelfinavir 1 proved to have an inhibitory effect on chymotrypsin-like activity of 20S proteasome. Previous studies also show the promotion of acceleration of the apoptosis process within …
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Developing novel drug combinations for treatment of invasive fungal infections
… amphotericin B against resistant C. auris. The HIV protease inhibitors (lopinavir and ritonavir) were identified as potent enhancers to the antifungal activity of azole drugs (fluconazole, voriconazole and itraconazole). We confirmed that lopinavir and ritonavir have the capability to interfere …
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Biomolecular ligand design : enhancing binding affinity and specificity utilizing electrostatic charge optimization and packing techniques
… specificity of binding. An application to the protease of HIV was performed to explore the determinants of specificity. General principles were found in a narrow specificity study with HIV protease as a target and the human aspartyl proteases pepsin and cathepsin D as decoys that may help to …
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Synthesis and Characterization of Poly(lactide) Functional Oligomers and Block Copolymers
… of potential core-shell delivery vehicles for HIV drugs. PEO-b-PDLLA block copolymer was used as a polymeric nanocarrier to encapsulate the HIV protease inhibitor, Ritonavir, within magnetite nanoparticles. Well-defined multifunctional polymeric nanoparticles with controlled sizes and size …
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