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.
Results
Showing 1 to 11 of 11 for “"differential scanning fluorimetry"”.
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Building a rational model for the identification of allosteric sites
… showed good selectivity for DYRK2 over DYRK1A by Differential Scanning Fluorimetry (DSF). This oxyamidine hit was further investigated through a structure activity relationship (SAR) which enabled the synthesis of three compounds that showed a higher stabilization than the initial hit (Tm > 1.2 …
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Inhibition of enzymes from mycobacteria using fragment-based approaches
… were extensively utilised, including both differential scanning fluorimetry and isothermal titration calorimetry. This approach led to the development of novel inhibitors with low nanomolar affinity. Select compounds were screened by collaborators against both Mab and Mtb in vitro. In light …
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Biophysical and structural studies of novel F420-dependent oxidoreductases in Mycobacterium tuberculosis
… presence and absence of F420 using STD NMR and differential scanning fluorimetry. Rv1155 and Rv2991 show affinity for distinct classes of fragments. Using a computational method known as “virtual fragment linking,” fragment binding data was used to predict and test potential substrates. This …
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Large-scale studies and biophysical analysis of systems involved in plant immunity.
… Finally, we have adapted a biophysical method, differential scanning fluorimetry (DSF). We tested the usefulness of these methods by interrogating different immune proteins/genes of the model plant Arabidopsis thaliana. Here is a summary of the major results obtained. In the realm of basal …
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Structure guided discovery of inhibitors of indoleamine 2,3-dioxygenase (IDO1)
… tumour immunity. Work in this thesis used differential scanning fluorimetry and enzyme inhibition assays to screen a fragment library for novel IDO1 inhibitors. Thirty‐five small compounds that interacted with and inhibited the IDO1 enzyme were identified, and included compounds from the …
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Development of novel lysine targeting covalent inhibitors for Bruton’s tyrosine kinase and casein kinase 2 and synthesis of novel hybrid androgen receptor inhibitors
… was validated by protein mass spectrometry and differential scanning fluorimetry, whereby all analogues induce expected responses with the WT BTK, but fail to induce a response with the loss of function mutant R28C, as expected. A 6-fold improvement in binding affinity from the parent compound …
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Development of peptide inhibitors as molecular therapeutics against tandem-repeat proteins
… were tested using surface plasmon resonance and differential scanning fluorimetry assays using recombinant Cdc20. Furthermore, D-box peptides were able to bind exogenous Cdc20 in mammalian cell lysates using a Cellular Thermal Shift Assay (CETSA). Lastly, I determined the co-crystal structures of …
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Prozessentwicklung mit maßgeschneiderten rekombinanten Biokatalysatoren zur Synthese einer Bulk- und einer Feinchemikalie
… and cost-intensive process. By means of nano differential scanning fluorimetry a high-throughput protocoll could be devised enabling the determination of the melting temperature of even two simultaneously recombinant, overexpressed enzymes in crude extracts.<br /><br /> Finally, basics for the …
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Engineering nitrilases for enhanced thermostability
… by experimental validation using nanoscale differential fluorimetry, negative stain and cryogenic electron microscopy, and single-particle analysis. In this study, atomic resolution structures of wild-type CynDpum and its variant CynDpum (Q86R/H305K/H308K/H323K) were employed to predict, …
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Autoinhibition and Chloride Sensing in the WNK1 Kinase
… 130mM. Further biophysical investigation using differential scanning fluorimetry with the kinase domain shows that the domain undergoes substantial increases in domain stabilization as the concen- tration of salt is increased. Continued analysis of this phenomena has pointed toward evidence of …
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Fragment-based approaches to targeting EthR from mycobacterium tuberculosis
Tuberculosis affects millions of people worldwide every year. The current treatment for TB is divided into a regimen of both first- and second-line drugs, where first-line treatments are more tolerated and require shorter treatment lengths. With rising levels of resistance, alternative treatment …