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 11 of 11 for “"Irreversible inhibition"”.
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Synthesis and evaluation of aziridine and symmetry-based epoxide affinity labels for HIV-1 protease
… to allow testing for both reversible and irreversible inhibition of HIV-1 protease, based on an internally-quenched fluorogenic substrate. Of eleven compounds assayed for reversible inhibition, five demonstrated modest to potent activities (K$\rm\sb{i}$'s ranging from 70 $\mu$M to 10 nM).
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Mechanisms and Targeting of Neurodevelopmental Regulator Rest In Medulloblastoma Dissemination
… has focused on targeting REST activity through inhibition of epigenetic cofactor, lysine specific demethylase 1 (LSD1). To this end, I examined human MB patient samples for LSD1 expression and discovered that while CXCR4 signaling was highly relevant to SHH-beta subgroups, LSD1 was increased in …
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Synthesis of cis- and trans-3-fluoroacrylate, and inhibition of BCL6 targeting a non-reactive cysteine
… peptide binding site in the BTB-domain of BCL6. Irreversible inhibition will block its function. These inhibitors are potential therapeutics for treating diffuse large B-cell lymphomas (DLBCLs) and triple negative breast cancers that are BCL6-dependent. In future work, the compound will be tested …
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Interactions between anticholinesterases in an in vitro central nervous system preparation
… in the proposed therapy is due to reversible inhibition of AChE, thereby protecting it from irreversible inhibition by nerve agent. To test this, extracellular field potentials were recorded from the molecular layer of the dentate gyrus in an in vitro slice model developed from the guinea pig. …
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The Effect of Anticholinesterase Action on Mammalian Skeletal Neuromuscular Transmission
… The work has been largely concerned with the irreversible inhibition of cholinesterase by ecothiopate (phospholine) at the neuromuscular junction, thereby altering the time course of transmitter action, and the subsequent effect on the contractile response of isolated mammalian diaphragm …
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Propoxyphene, Norpropoxyphene, and Proadifen (SKF-525A) Are Mechanism Based Inhibitors of CYP3A4, CYP3A5, and CYP3A in Human Liver Microsomes
… and norpropoxyphene are mechanism-based (irreversible) inhibitors of CYP3A, and to determine if propoxyphene and norpropoxyphene are reversible inhibitors of CYP3A. Mechanismbased inhibition is a type of irreversible inhibition that results from an inhibitor or its metabolite binding to an …
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Characterizing the Response of gdhA Transformed Tobacco to Glufosinate
… Glufosinate leads to plant death by the irreversible inhibition of glutamate synthetase (GS) leading to a disruption of subsequent GS-related processes resulting in elevated ammonium and disruption of photorespiration. Therefore, it was speculated that the …
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Targeting Mitochondrial Proline Dehydrogenase (PRODH) with a Suicide Inhibitor as a Novel Anticancer Strategy
… acid, 5-oxo) and irreversible/suicide (PPG) inhibitors of PRODH using cultured human breast cancer cells. PRODH knockdown or enzymatic inhibition each inhibited cell growth and induced variable degrees of apoptosis against malignant breast epithelial cell lines …
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Design, Synthesis and Evaluation of Covalent Inhibitors for Tissue Transglutaminase and Factor XIIIa
… The first project was concentrated on the inhibition of hTG2 activity. Ubiquitously expressed in tissues, hTG2 is a multifunctional enzyme. Its primary activity is the formation of isopeptide bonds between glutamine and lysine residues found on the surface of proteins or substrates. In …
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The Role of Polyamines in Osmotic Stress Tolerance in Gulf Killifish Fundulus Grandis
… challenge. In addition, the influence of irreversible inhibition of Odc by alpha-DL-difluoromethylornithine (DFMO) was assessed in the gills. Furthermore, the transcription and enzymatic activities of Arg, Odc and Pao was assessed in other tissues such as intestine and liver during …
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Conformational changes in the (Ca²⁺, Mg²⁺)-ATPase of sarcoplasmic reticulum during energy transduction
… Chem. 253, 5l40-5146) results in a progressive irreversible inhibition of calcium transport while (Ca²⁺, Mg²⁺)-ATPase activity is unimpaired. Possible conformational changes associated with this uncoupling were monitored by following alterations in kinetic mobility of sulphydryl (-SH) groups …