Photosensitizing effect of antimicrobial drug nitrofuran derivative--furagin N-(5-nitro-2-furil)-allylidencamino-hydantoin) under irradiation with light longer than 280 nm was found. The method of investigation is based on photochemiluminescence of Gly-Trp peptide in aqueous solution. Maximum photosensitizing efficiency was observed at the furagin concentration 0.08 mM when chemiluminescence yield was 33 times greater than photochemiluminescence of Gly-Trp peptide in absence of drug. It was shown that photochemiluminescence sensitized by furagin occurred via free radical way. Life time of the triplet state of furagin determined by flash photolysis was 40 microseconds. A comparison of experimental data with kinetic calculation allowed us to estimate the rate constant of triplet quenching by oxygen ((2.2 +/- 0.3)10(8) M-1.s-1) and the total rate constants of physical quenching and chemical reaction with Gly-Trp peptide ((2.0 +/- 0.4)10(8) M-1.s-1). It was also found in experiments with photochemiluminescence of Gly-Trp peptide sensitized by riboflavin (irradiation with monochromatic light 436 nm) that furagin possesses antioxidant properties twice reducing the intensity of chemiluminescence at the drug concentration 0.029 mM.
Download full-text PDF |
Source |
---|
J Nucl Med
January 2025
Department of Nuclear Medicine, Medical University of Innsbruck, Innsbruck, Austria
Several exploratory studies have demonstrated the feasibility of cholecystokinin-2 receptor (CCK2R) targeting in patients with medullary thyroid carcinoma (MTC) and other neuroendocrine tumors (NETs). We report the results of a prospective phase I/IIA pilot study (clinicaltrials.gov NCT06155994) conducted at our center with the Ga-labeled peptide analog DOTA-DGlu-Ala-Tyr-Gly-Trp-(N-Me)Nle-Asp-1-Nal-Phe-NH (Ga-DOTA-MGS5).
View Article and Find Full Text PDFSpectrochim Acta A Mol Biomol Spectrosc
August 2024
Instituto de Estructura de la Materia, IEM-CSIC, Serrano 121, 28006 Madrid, Spain. Electronic address:
Tryptophan (Trp) residue provides characteristic vibrational markers to the middle wavenumber spectral region of the Raman spectra recorded from peptides and proteins. In this report, we were particularly interested in eight Trp Raman markers, referred to as W (i = 1,…,8). All responsible for pronounced Raman lines, these markers originate from indole moiety, a bicyclic conjugated segment involved in the Trp structure.
View Article and Find Full Text PDFJ Nucl Med
January 2024
Department of Chemistry, Chair of Pharmaceutical Radiochemistry, TUM School of Natural Sciences, Technical University of Munich, Garching, Germany; and.
Because of the need for radiolabeled theranostics for the detection and treatment of medullary thyroid cancer (MTC), and the yet unresolved stability issues of minigastrin analogs targeting the cholecystokinin-2 receptor (CCK-2R), our aim was to address in vivo stability, our motivation being to develop and evaluate DOTA-CCK-66 (DOTA-γ-glu-PEG-Trp-(-Me)Nle-Asp-1-Nal-NH, PEG: polyethylene glycol) and DOTA-CCK-66.2 (DOTA-glu-PEG-Trp-(-Me)Nle-Asp-1-Nal-NH), both derived from DOTA-MGS5 (DOTA-glu-Ala-Tyr-Gly-Trp-(-Me)Nle-Asp-1-Nal-NH), and clinically translate [Ga]Ga-DOTA-CCK-66. Cu and Ga labeling of DOTA-CCK-66, DOTA-CCK-66.
View Article and Find Full Text PDFEJNMMI Res
July 2023
Department of Chemistry, Technical University of Munich, 85748, Garching, Germany.
Background: Over the last years, several strategies have been reported to improve the metabolic stability of minigastrin analogs. However, currently applied compounds still reveal limited in vitro and in vivo stability. We thus performed a glycine scan at the N-terminus of DOTA-MGS5 (DOTA-D-Glu-Ala-Tyr-Gly-Trp-(N-Me)Nle-Asp-1-Nal) to systematically analyze the peptide structure.
View Article and Find Full Text PDFPharmaceuticals (Basel)
February 2023
Department of Nuclear Medicine, Medical University of Innsbruck, 6020 Innsbruck, Austria.
Different attempts have been made in the past two decades to develop radiolabeled peptide conjugates with enhanced pharmacokinetic properties in order to improve the application for tumor imaging and peptide receptor radionuclide therapy (PRRT), which targets the cholecystokinin-2 receptor (CCK2R). In this paper, the influence of different side chain and peptide bond modifications has been explored for the minigastrin analog DOTA-DGlu-Ala-Tyr-Gly-Trp-(-Me)Nle-Asp-1Nal-NH (DOTA-MGS5). Based on this lead structure, five new derivatives were synthesized for radiolabeling with trivalent radiometals.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!