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Full-Text Articles in Medicine and Health Sciences
Leveraging Bio-Inspired Molecules For Cancer Theranostics, Douglas S. Macpherson
Leveraging Bio-Inspired Molecules For Cancer Theranostics, Douglas S. Macpherson
Dissertations, Theses, and Capstone Projects
A variety of molecules can be radiolabeled and delivered to a cancer site for the purposes of diagnostics and therapy. Among the most promising of tumor targeting molecules are peptides and antibodies. These bio-inspired molecules can be designed and synthesized to target and respond to cancer cells based on the properties of those cells. Matrix metalloproteinase (MMP) enzymes are over-expressed by some metastatic cancers, in which they are responsible for the degradation and remodeling of the extracellular matrix. In recent years, MMPs have emerged as promising targets for enzyme-responsive diagnostic probes because oligopeptides can be designed to be selectively hydrolyzed …
Synthesis Of Fluoroorganics And Applications Of Novel Fluorinated Building Blocks, Wei Wei
Synthesis Of Fluoroorganics And Applications Of Novel Fluorinated Building Blocks, Wei Wei
Dissertations, Theses, and Capstone Projects
Diastereoselectivity of fluorination of a carbanion alpha to a sulfone in enantiomerically pure N-Boc protected (R)- and (S)-2,2-dimethyl-4-((arylsulfonyl)methyl)oxazolidines has been studied. Fluorination proceeded with good to excellent diastereoselectivity, which was base-dependent and was highest with lithium diisopropylamide (LDA). Diastereoselectivity also depended on the aryl moiety of the aryl sulfone and was highest with benzothiazole-derived sulfones. Under basic conditions, epimerization at the C–F stereogenic center alpha to the sulfone has been achieved for the first time and proceeded with good to excellent diastereoselectivity, which was highest in the case of a benzothiazole sulfone and with a lithium base. …
Second Generation Phenyloxadiazolyl Methyl Sulfones For Thiol-Specific Bioconjugations, Guillaume Dewaele-Le Roi
Second Generation Phenyloxadiazolyl Methyl Sulfones For Thiol-Specific Bioconjugations, Guillaume Dewaele-Le Roi
Dissertations, Theses, and Capstone Projects
The role of antibody-based molecular agents for diagnosis and therapy of cancer has expanded significantly over the past decades. However, most of these constructs are synthesized using traditional bioconjugation methods based on the random ligations between the molecular cargo and lysine residues within the protein. These non-specific approaches can create poorly defined conjugates with suboptimal immunoreactivity and in vivo performance while Site-specific approaches to antibody bioconjugation based on ligations between maleimides and free cysteine residues have long stood as attractive alternatives. Yet the inherent instability of the thiol-maleimide linkage has fueled the search for new, more stable thiol-reactive prosthetic groups. …