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 4 of 4 for “"targeted covalent inhibitors"”.
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Development of stapled peptide targeted covalent inhibitors and synthesis of novel ADC payloads for applications in cancer therapy
… therapeutics. 1) Development of stapled peptide–targeted covalent inhibitors (SPTCIs) of p53–MDM2 protein–protein interaction (PPI). Herein, the development and synthesis of three novel electrophilic staples and four stapled peptides are described. The stapled peptides bear moieties to covalently …
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Towards targeted post-translational modification of endogenous proteins in complex environments
… can be exploited pharmacologically, as covalent inhibitors such as aspirin covalently bind, or attach a covalent payload, to the active sites of enzymes. Following this principle, rationally designed targeted covalent inhibitors (TCIs) adapt non-covalent ligands to react with …
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Investigating the structure-function relationships of Plasmodium Haem Detoxification Protein and Phosphatidylinositol 4-kinase
… on the development of both ATP-competitive and covalent Plasmodium PI4Kβ inhibitors. Two residues of interest in Plasmodium vivax PI4Kβ unique to Plasmodium, F832 and C1327, were mutated to alanine. F832 is thought to form key Pi-Pi interactions with inhibitors and C1327, found on the periphery …
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Discovery of covalent modifiers via the complexity to diversity strategy
Targeted covalent drugs have recently become integral parts of drug discovery. Given the advantages of high-throughput screening in drug discovery, many electrophilic fragment collections have been developed as a promising alternative to discover and validate novel targets. However, most covalent …