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 105 for “"protease inhibitors"”.
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Nutrient Transporter targeted Delivery of HIV Protease Inhibitors
… 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 the first anti-HIV PI approved by …
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The Role of Serine Protease Inhibitors in Regulating Hepatotoxicity During Viral Infection
… of a family of intracellular serine proteinase inhibitors (serpins). PI-9 and SPI-6 expression in immune-privileged cells, antigen-presenting cells, and cytotoxic T cells protects these cells against the actions of granzyme B and when expressed in tumor cells, confers resistance to killing by …
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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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New aminoquinoline antimalarial cysteine protease inhibitors based on the isatin natural product scaffold
… previously demonstrated to inhibit cysteine proteases from mUltiple protozoan parasites. Synthesized compounds were tested against the enzyme falcipain-2 (Rec-FP-2) as well as the parasite source of this protease, Plasmodium Jalciparum (P.f. W2). The results of structure activity relationship …
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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 and biological evaluation of antiparasitic Cysteine protease inhibitors based on the Isatin Scaffold
… of new drugs. Meanwhile, the cysteine protease family of enzymes has been identified as potential targets for new modes of chemotherapy due to the numerous critical roles they play in the disease-causing agents. In this project, a non-peptidic and low molecular weight isatin (indole-2, …
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Engineering of the microviridin post-translational modification enzymes for the production of synthetic protease inhibitors
… and lactam rings, and their activity as serine protease inhibitors. The generalities of their biosynthetic pathway have already been described, however, the lack of information on details such as the protease responsible for cleaving off the leader peptide from the cyclic core peptide has …
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Isolation and characterization of starch, starch biosynthetic genes and protease inhibitors from Marama beab (Tylosema Esculentum)
… starch biosynthesis genes and detect serine protease inhibitor activities in green and mature marama seeds. The total starch content of marama bean tubers was determined by amyloglucosidase/α-amylase enzymatic digestion and amylose content by Concanavalin A precipitation. A complementary …
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Studies Toward the Synthesis of Salvinorin A and Synthesis of Broad-Spectrum DENV/WNV NS3 Protease Inhibitors
… features including a highly homologous NS3 protease. NS3 is essential for virion replication, making it an ideal target for a broad-spectrum inhibitor of the related viral proteases.
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Investigation of the efficacy of identified acetolactate synthase inhibitors, peptidyl cysteine protease inhibitors, thiolactomycins, and thiosemicarbazone compounds against Mycobacterium tuberculosis
… 121 derivatives from the acetolactate synthase inhibitors, cysteine protease inhibitors, thiosemicarbazones, and thiolactomycins classes of compounds for in vitro efficacy against M. tuberculosis using the resazurin microtitre plate assay afterwhich active compounds were assessed for …
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An Insight Into the Microbial Diversity and Expression of Cysteine Protease Inhibitors (Cystatin) in <i>Rickettsia parkeri</i> Infected <i>Amblyomma maculatum</i>
<p><em>Amblyomma maculatum</em> (Gulf Coast tick) is an emerging tick species of public health significance in United States. It is a competent vector of <em>Rickettsia parkeri</em>, an etiological agent of a human rickettsiosis. In this study, we investigated the spotted fever group of rickettsial …
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Risk of Cardiovascular Disease Inhibitors Among HIV seropositive Adults on Protease Inhibitors Containing Antiretroviral Therapy at Adult Infectious Disease Centre at the University Teaching Hospital
… in the presence of ART particularly Protease Inhibitors (PIs) in Sub-Saharan Africa. The objective of this study was to determine the risk associated with the use of PIs- containing ART in the development of CVD among HIV seropositive adult’s at the Adult Infectious Disease Centre …
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Methodologies For Attaching Polypyridyl Ligands Into Amino Acids And Synthesis And Biological Evaluation Of Novel Light Activated Peptidomimetic Cysteine Protease Inhibitors Caged By Ruii(bpy)2
… the synthesis of the first caged cysteine protease inhibitor. After an introductory survey of different Ru and Pt complexes used as potential therapeutic cancer agents, cysteine protease inhibitors are described. The syntheses of RuII(bpy)2 complexes caging cathepsin inhibitors are revealed …
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Mechanism of lipid disorder in HIV infection: apolipoprotein-B kinetics, fat distribution, insulin resistance and adipocytokines in patients taking protease inhibitors or non-nucleoside reverse transcriptase inhibitors
… taking two nucleoside analogues plus either a protease inhibitor (PI, n=15) or non-nucleoside reverse transcriptase inhibitor (NNRTI, n = 25). The HIV positive treatment groups had mild dyslipidaemia. The apo-B fractional clearance rate (FCR) was reduced in the HIV positive groups. Peripheral …
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Identification and bioactivity evaluation of an amphibian skin Bowman-Birk-like trypsin inhibitor from Hylarana nigrovittata
… Among these bioactive compounds, serine protease inhibitors have been found in amphibian skin. Serine proteases are a large family of conserved, proteolytic enzymes. They play a role in many bodily functions and some are digestive enzymes. Protease action can be controlled by protease …
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Identification of features contributing to binding promiscuity of small-molecule inhibitors for rapidly mutating targets
… 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 various strategies that have been explored for the …
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