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3. One-step conjugation of glycylglycine with [18F]FDG and a pilot PET imaging study.

Author

Şenışık, A. M., İçhedef, Ç., Kılçar, A. Y., Uçar, E., Arı, K., Göksoy, D., Parlak, Y., Sayıt Bilgin, Bedriye Elvan, and Teksöz, S.

Subjects
*GLYCINE, *RADIOLABELING, *CHEMOSELECTIVITY, *POSITRON emission tomography, *RADIOPHARMACEUTICALS
Abstract

This study describes a single step conjugation of Glycylglycine (GlyGly) which is a small peptide, with [18F]FDG via oxime formation. Amiooxy-functionalization of GlyGly (AO-GlyGly) was accomplished through the reaction of Boc-aminooxy succinimide ester. Conjugation reaction was performed at 100 °C for 30 min in a vial containing AO-GlyGly and [18F]FDG solution. The radiolabeled product ([18F]FDG-GlyGly) was obtained with 98.65 ± 0.35% yield without any purification step which makes this method more attractive for 18F radiolabeling. The present study is concluded with an in vivo pilot animal PET study to assess biodistribution and kinetics of chemoselectively [18F]FDG tagged GlyGly in vivo. [ABSTRACT FROM AUTHOR]

Published
2018
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4. Evaluation of New 99mTc(CO)3+ Radiolabeled Glycylglycine In Vivo

Author

Şenışık, Ahmet M., İçhedef, Çiğdem, Kılçar, Ayfer Y., Uçar, Eser, Arı, Kadir, Parlak, Yasemin, Bilgin, Elvan S., and Teksöz, Serap

Abstract

Background: Peptide-based agents are used in molecular imaging due to their unique properties, such as rapid clearance from the circulation, high affinity and target selectivity. Many of the radiolabeled peptides have been clinically experienced with diagnostic accuracy. The aim of this study was to investigate in vivo biological behavior of [99mTc(CO)3(H2O)3]+ radiolabeled glycylglycine (GlyGly). Methods: Glycylglycine was radiolabeled with a high radiolabeling yield of 94.69±2%, and quality control of the radiolabeling process was performed by thin layer radiochromatography (TLRC) and High-Performance Liquid Radiochromatography (HPLRC). Lipophilicity study for radiolabeled complex (99mTc(CO)3-Gly-Gly) was carried out using solvent extraction. The in vivo evaluation was performed by both biodistribution and SPECT imaging. Results: The high radiolabelling yield of 99mTc(CO)3-GlyGly was obtained and verified by TLRC and HPLRC as well. According to the in vivo results, SPECT images and biodistribution data are in good accordance. The excretion route from the body was both hepatobiliary and renal. Conclusion: This study shows that 99mTc(CO)3-GlyGly has the potential to be used as a peptide-based imaging agent. Further studies, 99mTc(CO)3-GlyGly can be performed on tumor-bearing animals.

Published
2019
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5. One-step conjugation of glycylglycine with [18F]FDG and a pilot PET imaging study

Author

Çiğdem İçhedef, Ahmet Murat Senisik, D. Göksoy, Ayfer Yurt Kilcar, Serap Teksöz, Kadir Ari, Bedriye Elvan Sayit Bilgin, Yasemin Parlak, Eser Uçar, Vocational School of Health Services/Radiotheraphy, Istanbul Kemerburgaz University, Bağcılar, İstanbul 34217, Turkey, Department of Nuclear Applications, Institute of Nuclear Sciences, Ege University, Bornova, İzmir 35100, Turkey, Departmant of Nuclear Medicine, Celal Bayar University, Manisa, 45030, Turkey, and Şenışık, A. M.

Subjects
Biodistribution, FDG, Health, Toxicology and Mutagenesis, Kinetics, One-Step, 010403 inorganic & nuclear chemistry, 01 natural sciences, Imaging, 030218 nuclear medicine & medical imaging, Analytical Chemistry, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Succinimide, In vivo, Radiology, Nuclear Medicine and imaging, Spectroscopy, Glycylglycine, Radiochemistry, Public Health, Environmental and Occupational Health, Oxime, Pollution, 0104 chemical sciences, PET, Nuclear Energy and Engineering, chemistry, Yield (chemistry), Radiopharmaceuticals
Abstract

KILCAR, AYFER YURT/0000-0003-0866-7515; Senisik, Ahmet Murat/0000-0002-7781-3355; KILCAR, AYFER YURT/0000-0003-0866-7515; ichedef, cigdem/0000-0002-1586-9521 WOS:000431040600006 This study describes a single step conjugation of Glycylglycine (GlyGly) which is a small peptide, with [F-18]FDG via oxime formation. Amiooxy-functionalization of GlyGly (AO-GlyGly) was accomplished through the reaction of Boc-aminooxy succinimide ester. Conjugation reaction was performed at 100 A degrees C for 30 min in a vial containing AO-GlyGly and [F-18]FDG solution. The radiolabeled product ([F-18]FDG-GlyGly) was obtained with 98.65 +/- 0.35% yield without any purification step which makes this method more attractive for F-18 radiolabeling. The present study is concluded with an in vivo pilot animal PET study to assess biodistribution and kinetics of chemoselectively [F-18]FDG tagged GlyGly in vivo. Ege University Scientific Research Project (Bomova, Izmir, Turkey)Ege University [2012 NBE 004] This study was financially supported by the Ege University Scientific Research Project numbered 2012 NBE 004 (Bomova, Izmir, Turkey).

Published
2018

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