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 98 for “"protease inhibitor"”.
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Antimalarial and cysteine protease inhibitor pharmacophores as scaffolds for new antimalarial agents
… mechanism-based inhibiotrs of parasitic cysteine proteases. (iii) Multicomponenet reactions offer the advantage of introducing chemical diversity in fewer steps than conventional multi step organic synthesis. New chloroquine-type compounds were designed and synthesized using the Ugi 4 component …
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Electrochemical dynamics of cytochrome P450-3A4 isoenzyme biosensor for protease inhibitor antiretroviral drug
… platform 2 was evaluated for the detection of protease inhibitor (PI) HAART drug, indinavir. Fourthly, this dissertation also reports on the use of genetic engineering as complimentary method during biosensor investigations, as source for continuous supply of catalytically active biological …
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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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Short term adherence tool predicts failure on second line protease inhibitor-based antiretroviral therapy
The management of patients failing second line antiretroviral therapy (ART) is a critical area of study considering the increasing numbers of patients on second line regimens, and the expense and poor availability of third line ART. Most patients who experience virologic failure (VF) on second line …
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Differential Stimulation of Monocytes to Secrete Secretory Leukocyte Protease Inhibitor by Lipopolysaccharide of Periodontal Pathogens
… mononuclear phagocyte cells. Secretory Leukocyte Protease Inhibitor (SLPI) is a single-chain serine protease inhibitor secreted from secretary and inflammatory cells that protects tissue from damage caused by the inflammatory response. The present study examined the interaction of LPS prepared …
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What can't be cured must be endured: Optimisation of HIV Protease Inhibitor-Containing Antiretroviral Therapy
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Cellular Uptake of Cystatin C. Subcellular localisation and intracellular effects of a secreted cysteine protease inhibitor
Cystatin C is a cysteine protease inhibitor, aimed for secretion, as it is produced with a signal peptide. Its target enzymes are thought to be the lysosomal cysteine cathepsins and legumain. Cystatin C has been considered to excert its enzyme inhibiting functions extracellularly, as a defense …
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Cloning and expression of a chimeric protease inhibitor encoding gene in Escherichia coli and Pichia pastoris
Squash family protease inhibitors are small peptides of 27-32 residues, hence they are ideal subjects for structure-function studies. Their small size is within the reach of peptide chemical synthesis, which enables one to produce enough peptide material for experimental purposes within a …
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Identification and bioactivity assessment of a protease inhibitor QUB-1833 from the skin secretion of Lithobates catesbeiana
… The peptide QUB-1833 showed a very efficient inhibitory effect on trypsin. While it did not have any inhibitory activity against the selected three microorganisms (S. aureus, E. coli, and C. albicans) and two human cancer cell lines (U251-MG and HCT-116). This peptide has a very low hemolysis …
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Environmental and genetic variation of the anti-cancer peptides lunasin and Bowman-Birk protease inhibitor in Glycine max
… Two of these compounds, the Bowman-Birk protease inhibitor (BBI) and the peptide lunasin, exhibit anti-cancer properties, and clinical studies suggest that the two may act in a complementary fashion. The present work surveys the levels of these two compounds across a time course of …
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Competition-based CRISPR-dCas9 transcriptional control mechanisms and application of dCas9 biosensors for high-throughput, cell-based protease inhibitor screens
… to create an in vivo selection system for protease inhibitors. By leveraging a previously-described dCas9 toolkit, I create a synthetic genetic circuit that responds to SARS-CoV-2 viral protease activity. Using this circuit as an in vivo biosensor, I integrate it with a RiPP-based molecular …
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Population pharmacokinetic models describing drug-drug interactions and variability in HIV infected South Africans on protease inhibitor-based antiretroviral regimens with and without tuberculosis
Lopinavir/ritonavir is an important component of the first-line and second-line antiretroviral treatment for young children and adults respectively in the current World Health Organization guidelines. Rifampicin, a key component of antituberculosis treatment, profoundly reduces lopinavir …
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A bioactive peptide from the frog skin secretion of Pelophylax nigromaculatus GAPKGCWTKSYPPKPCS-NH2
… Cys16 that is consistent with a Bowman–Birk type protease inhibitor, from the skin secretion of the frog Pelophylax nigromaculatus. The precursor was obtained from the Pelophylax nigromaculatus skin secretion by employing molecular cloning. The corresponding mature peptide, namely QUB-1804, was …
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Serpin polymers enforce molecular filtration in the endoplasmic reticulum
… cause disease. Alpha1-antitrypsin is the serine protease inhibitor (serpin) that is secreted mainly by hepatocytes and acts in lungs where its major function is to inhibit neutrophil elastase. Neuroserpin is a serine protease inhibitor expressed in the nervous system. Mutations in these two …
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Age related changes and tissue distribution of parvalbumin in both normal and dystrophic 129 ReJ mice.
… muscle contains a functionally defective thiol protease inhibitor (TPI) which has been implicated in the onset and progression of the disease in this strain of mice. More recently, and through the work of several researchers, this protease inhibitor has been identified as parvalbumin, a calcium …
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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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Pharmacological investigations into matrix metalloproteinase-activated anti-tumour prodrugs. In vitro metabolic and pharmacological investigations into a series of colchicine-based peptide prodrugs activated by tumour-expressed matrix metalloproteinases
… using leupeptin (serine, cysteine and threonine protease inhibitor), pepstatin A (aspartate protease inhibitor), phosphoramidon (nepralysin inhibitor), ilomastat (metalloproteinase inhibitor) and BML-P115 (matrix metalloproteinase inhibitor). Moreover, members of the MMP family responsible for …
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Drug resistance mechanisms and drug design strategies for human immunodeficiency virus and hepatitis c virus proteases
… represent heavy public health burdens. The viral protease plays an indispensable role in viral maturation and therefore becomes one of the most important targets for drug design. Nine HIV-1 protease inhibitors and two HCV protease inhibitors have been developed and approved by the U.S. Food and …
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Stimulating antibiotic development by targeting virulence and facilitating natural product discovery
… 2, I demonstrate that the FDA approved HIV protease inhibitor nelfinavir can be repurposed as an inhibitor of the biosynthesis of the Streptococcus pyogenes cytolytic toxin streptolysin S. Nelfinavir was utilized to explore the proteolytic processing step in streptolysin S biosynthesis and …
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