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Full-Text Articles in Medicinal-Pharmaceutical Chemistry
Development Of A Gallium-Containing One-Bead One-Compound Peptide Library For The Discovery Of New Molecular Imaging Probes, Fernanda C. Bononi
Development Of A Gallium-Containing One-Bead One-Compound Peptide Library For The Discovery Of New Molecular Imaging Probes, Fernanda C. Bononi
Electronic Thesis and Dissertation Repository
An eight amino acid one-bead one-compound (OBOC) peptide library, containing a gallium-DOTA complex, was developed in an attempt to overcome common issues associated with the later addition of radionuclides to peptide chains of imaging probes. The further addition of a radionuclide often changes the binding properties of a peptide, as it adds bulk, and possibly charges. MALDI (matrix-assisted laser desorption ionization) tandem mass spectrometry was determined to be the method of choice in order to deconvolute gallium-containing peptide sequences. The library obtained was screened against the breast cancer cell lines MDA-MB-231 and MCF-7. Positive beads were isolated and sequences were …
Peptidomimetic Ghs-R1a Agonists As Pet Imaging Agents For Prostate Cancer, Milan M. Fowkes
Peptidomimetic Ghs-R1a Agonists As Pet Imaging Agents For Prostate Cancer, Milan M. Fowkes
Electronic Thesis and Dissertation Repository
Contemporary diagnostic techniques for prostate cancer (PCa) have a limited ability to distinguish between benign and malignant disease. The ghrelin receptor has a differential expression in normal, benign and cancerous prostatic tissue. Targeting this receptor with 18F-radiolabelled peptidomimetics would enable differentiation between these disease states via PET imaging. A series of 19F-peptidomimetics were synthesized and characterized by HRMS, HPLC and 1 H-NMR spectroscopy in order to test locations for 18F radioisotope insertion. Competitive receptor binding assays using HEK293/GHS-R1a cells were used to evaluate compound binding affinities. This led to the identification of two lead compounds: [1-Nal4,Lys5(4-FB)]G-7039 (IC50 = 69 nM) …