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 9 of 9 for “"allosteric inhibitor"”.
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Adenosine triphosphate is an allosteric inhibitor of coxsackievirus B3 3Dpol
… target for antiviral research. The only 3Dpol inhibitors that have been found to date are nucleoside analogues that act directly on the active site, even though global dynamics of the protein that are sensitive to allosteric effects of various mutations have been shown to be important …
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A Fragment-Based Drug Discovery Approach for the Development of Selective Inhibitors of Protein Kinase CK2
… associated with worse prognosis. A number of CK2 inhibitors are currently available displaying activity against multiple cancers in vitro and in the clinic, however the majority of these candidates target the ATP-binding site and thus display poor selectivity in kinase panel assays. Here we …
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Designing Allosteric Inhibitors of Thrombin
… that thrombin may be better regulated through an allosteric process mediated by small molecules binding to either exosite I or II. An appropriately designed allosteric regulator that reduces the procoagulant signal in a finely tuned manner may maintain a delicate balance between procoagulant and …
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HSP70 as a Target for Correction of Wilson Disease Causing ATP7B Mutants
… HSP70 suppression (with either RNAi or allosteric inhibitor) improved stability of the mutant and facilitated its export from the ER to the Golgi and post-Golgi copper excretion sites. These findings prompted me to look for a safe way to inhibit HSP70 and rescue the ATP7B mutant. To this …
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Computational and Pharmacological Approaches to Design Novel Allosteric Thymidylate Synthase Inhibitors
<p>The goal of this research is to develop new allosteric thymidylate synthase (TS) inhibitors in an effort to reduce cancer drug resistance. Resistance is associated with elevation in TS levels upon exposure to active site targeted drugs. Human TS exists in conformational equilibrium between …
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Structural and biochemical investigations into the Neisseria gonorrhoeae ribonucleotide reductase
… regulated at many levels including through allosteric regulation, which occurs in many organisms through oligomeric state changes. These quaternary shifts allow for radical transfer to the active site in the presence of allosteric activator ATP (active state) and prevent that radical …
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Interrogating novel functions of the I kappa B kinases via CRISPR-Cas9 gene editing and small molecule inhibition
… BMS-345541 is a commercially available allosteric inhibitor of IKKβ that has been used extensively in numerous studies, including a report that proposed novel functions for IKKβ in mitotic cell cycle progression (Blazkova et al., 2007). Similar antiproliferative effects to those reported …
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Calpain inhibitor design inspired by the natural inhibitor calpastatin
… great interest and medical relevance to design inhibitors that can specifically target calpain without interfering with the other numerous cellular cysteine proteases. The cytosolic and ubiquitous calpains-1 and -2 have a naturally occurring and specific inhibitor, calpastatin, which binds with …
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INVESTIGATION OF ANTIBIOFILM AND ANTIVIRULENCE ACTIVITY OF 5-FLUOROCYTOSINE IN ESCHERICHIA COLI
… studies suggested that 5-FUMP can bind the allosteric domain of carbamoyl phosphate synthetase, the first enzyme in de novo pyrimidine biosynthesis pathway, similar to its native allosteric inhibitor UMP and possibly mimic UMP’s negative feedback mechanism affecting the pyrimidine nucleotide …