Molecular Innovations Toward Theranostics of Aggressive Prostate Cancer
Technical Report,01 Sep 2015,31 Aug 2016
Texas Christian University Fort Worth United States
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The effort explores the preparation theranostics comprising a therapeutic peptide and a chelating group based on DOTA. Methods to develop a series of dendrimers bearing an imaging group at the core evolved from late-stage alkyne functionalization to early incorporation of the imaging group. Efforts showed that dendrimers of varying sizes can be accessed with this strategy. Methods for the accelerated synthesis of these targets were developed. Solubility parameters were also defined. Methods to incorporate multiple copies of a therapeutic peptide rested on the utilization of linkers that were either biolabile or stable. Efforts with biolabile linkers revealed a new class of hydrazones that show promise in multiple areas of therapeutic research, although more limited utility to date with highly soluble cargos the peptide of interest. Efforts with stable linkers included maleimide and therapeutics bearing a thiol cysteine and covalent ligation resulting from selective triazine addition of a functionalized therapeutic. The latter strategy is favored based on the instability of the maleimide and the need for long reaction times.
- Medicine and Medical Research
- Genetic Engineering and Molecular Biology