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Showing 1 to 17 of 17 for “"Diazirine"”.
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Design, synthesis, and biochemical evaluation of three types of hexestrol-based probes for estrogen receptor: Fluorine-18 radiopharmaceuticals, bivalent ligands and diazirine photoaffinity reagents
The estrogen receptor (ER) has become a major focus of biological and clinical investigation in diagnostic and therapeutic drug design for human breast carcinoma. Molecular probes, such as fluorine-18 radiopharmaceuticals, bivalent ligands, and affinity labels, provide information toward a better …
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Photochemistry of 5-Membered Heteroaryl(trifluoromethyl)carbenes in Low Temperature Matrices
… before. The 3-benzothienyl(trifluoromethyl)diazirine led us to a new realm of UV-vis transparent diazirines, which behave as normal diazirine photochemically, but have very weak n<em>f</em>à<em>f</em>x<em>f</em>nabsorptions which are not visible in experimental UV-vis spectra. Also, we were …
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Utilisation des diazirines comme source d'azote électrophile pour la synthèse d'hydrazines et d'hétérocycles
… la faible diversité des produits obtenus. Les diazirines présentent un fort potentiel pour être utilisées comme alternative à ces préparations, puisque ces molécules peuvent réagir avec des nucléophiles pour donner les diaziridines substituées correspondantes, puis être hydrolysées pour …
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Study of Glycan-Mediated Interactions by Photocrosslinking GlcNAc and GalNAc Analogs
… to characterize. To address this challenge, diazirine-functionalized sugar analogs that can be metabolically incorporated into cellular glycans were designed. Upon UV irradiation, a covalent bond forms between the diazirine group and nearby molecules. The formation of a covalent bond makes it …
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Structural Studies on the Estrogen Receptor Ligand Binding Domain Using Electrospray Ionization Mass Spectrometry
… attachment of the photoaffinity label hexestrol diazirine. The application of tandem MS/MS sequencing permitted the identification of several residues near the C-terminus of the protein.
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I.~Design, Synthesis, and Evaluation of a Rigidly Constrained Peptidomimetic as a Potential Type I Beta-Turn. II.~Development of Novel Estrogen Receptor Ligands With Unique Endocrine Profiles. III.~Design, Synthesis and Biological Evaluation of Potential Aspartic Protease Inhibitors Based on the Diaziridine and Diazirine Isostere
… inhibitors based on the diaziridine and diazirine isostere, as potential transition-state mimics of the tetrahedral intermediate found along the reaction pathway for enzyme mediated peptide bond hydrolysis. These isosteres (143 and 144) have been incorporated into substrates for the …
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MODIFIED BODIPY PROBES TO EXPLORE PEROXISOME FUNCTION
… meso-substituents. 3-Methoxy trifluoromethyl diazirine was successfully synthesised with the aim at coupling to the BODIPY dyes. However, although many borylation and bromination reactions on meta and para methoxy substituted trifluoromethyl diazirines, were attempted these were not …
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Pioneering investigations into organometallic electrochemistry
… are also reported. In chapter 5, the use of diazirines as carbene precursors for carbon surface modification is investigated, via the synthesis and characterisation of diazirine derivatised cymantrene and cyrhetrene. The surface modification of glassy carbon electrodes was attempted via …
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Making Nuclear Magnetic Hyperpolarization Practical through Storage in Disconnected Eigenstates
… hyperpolarize long lived spin order in a diazirine containing molecule. Diazirine rings are three member N=N-C groups that can replace a methylene group and serve as a versatile MR and optical molecular tag. Hyperpolarization is accomplished by bubbling parahydrogen through a solution …
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Total Synthesis of Verticillin A and Application of Diazene-Directed Fragment Assembly to the Synthesis of Heterodimeric Epidithiodiketopiperazine Derivatives
… ETP derivatives, we have synthesized an ETP-diazirine photoaffinity labelling probe, which we hope can be used to study the interactions of ETPs with cellular targets.
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New approaches for the synthesis of unusual amino acids
… of photoactivatable amino acids incorporating a diazirine ring, such as photo-leucine, which generate a reactive carbene after the light induced loss of nitrogen.
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Chemical and enzymatic tools to study proteins in their native cellular environment
… specific photocrosslinker than aryl azide and diazirine, its high geometric constraint to its proximal crosslinkable C-H bonds may decrease its crosslinking yield. Knowing the protein structure and amino acid environment surrounding benzophenone could help in choosing the most optimal position …
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Development of New Photocrosslinking Approaches to Discover Binding Partners of O-GlcNAc-Modified Proteins
… we reported a method to incorporate the diazirine photocrosslinking group onto O-GlcNAc residues in cellular proteins. Photocrosslinking O-GlcNAc, O-GlcNDAz, yields covalent crosslinking between O-GlcNAc-ylated proteins and their binding partners, which further analysis can confirm these …
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Proteomic Approaches For Profiling Cofactor-Dependent Proteins In Mycobacterium Tuberculosis
… inhibitor of PLP-dependent enzymes, a linear diazirine for UV-crosslinking, and an alkyne moiety to enable enrichment of crosslinked proteins. Our molecule was utilized to study PLP-dependent enzymes in vitro as well as look at whole cell lysates of Mycobacterium tuberculosis and assess …
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Targeting Transcription Factors in Neuroblastoma: Development of Aurora Kinase A/N-Myc Degraders and ID2 Chemical Probes
… To decipher the unknown target(s) of 6.1, a diazirine photo-crosslinking probe, 6.6 (HLB-0535030), has been successfully developed and validated as a viable probe for the subsequent target identification studies. Finally, Appendix A reports the development of a cellular thermal shift assay …
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Enzymology And Medicinal Chemistry Of N5-Carboxyaminoimidazole Ribonucleotide Synthetase : A Novel Antibacterial Target
… II, non-competitive inhibitors, we developed a diazirine-based photocrosslinking agent to identify the binding site of these inhibitors. These studies revealed that the isatin core of class II inhibitors is capable of undergoing photochemical conversion to isatoic anhydride. Once formed, the …
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O-GlcNAc-Mediated Protein-Protein Interactions in Cell Signaling
… O-GlcNAc using a GlcNAc analog containing a diazirine photocrosslinking moiety (GlcNDAz). We used this approach to identify proteins engaging in O-GlcNAc-mediated protein-protein interactions, including vimentin, an O-GlcNAcylated intermediate filament (IF) protein. Vimentin is important for …