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 3 of 3 for “"Electrophilic Warhead"”.
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The Development of Assays for Detecting Proximal Phosphorylation and Covalent Modification of Proteins
… in assay development was to assess a modular electrophilic warhead platform for novel covalent inhibitors. Through nucleophilic aromatic substitution methodology, selectively derivatized polyfluorinated benzene rings were synthesized to construct an electrophilic warhead library that could be …
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SALICYLALDEHYDE-TAGGED PEPTIDES FOR THE REVERSIBLE-COVALENT ENGAGEMENT OF PROTEIN LYSINE RESIDUES
… the use of salicylaldehyde (SA) as a reversible electrophilic warhead for peptide-based ligand design. The first part of this thesis focuses on the synthesis of SA-modified amino acids and their incorporation into model peptides. Later on, a more straightforward and versatile approach was …
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QUANTITATIVE PROTEOMIC APPROACHES TO STUDY DRUG MECHANISM OF ACTION
… obtained by introducing in these drugs an electrophilic warhead able to bind specific nucleophilic sites in the protein target. Covalent inhibition of oncogenic protein kinases allows to obtain a stronger and prolonged therapeutic effect compared to reversible inhibition; however, the …