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Title: Complexes of gastrin with In3+, Ru3+ or Ga3+ ions are not recognised by the cholecystokinin 2 receptor.
Austin Authors: Laval, Marie;Marshall, Kathryn M;Sachinidis, John;Scott, Andrew M ;Eutick, Mal;Baldwin, Graham S
Affiliation: Department of Molecular Imaging and Therapy, Austin Health, Heidelberg, Victoria, Australia
Phebra Pty. Ltd, Hunters Hill, NSW, Australia
Olivia Newton-John Cancer Research Institute, Heidelberg, Victoria, Australia
La Trobe University, Melbourne, Victoria, Australia
Department of Medicine, University of Melbourne, Melbourne, Victoria, Australia
Department of Surgery, Austin Health, The University of Melbourne, Heidelberg, Victoria, Australia
Issue Date: Oct-2017
Date: 2017-07-12
Publication information: Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry 2017; 22(7): 999-1006
Abstract: The peptide hormone gastrin (Gamide) binds trivalent metal ions, including indium (In), ruthenium (Ru) and gallium (Ga), with high affinity. Complexes of gastrin with chelated isotopes of In and Ga have previously been used for the location of tumours expressing the cholecystokinin 2 receptor (CCK2R). The aim of the present study was to purify the complexes of Gamide with radioactive isotopes of In, Ru or Ga and to investigate their ability to bind to the CCK2R. The radioactive Gamide complexes were purified on Sep-Pak C18 cartridges or by anion exchange HPLC. Binding to the CCK2R was assessed with a stably transfected clone of the gastric carcinoma cell line AGS. The 106Ru-Gamide complex could be eluted from the C18 cartridge; the 111In-Gamide and 68Ga-Gamide complexes bound irreversibly. All three complexes were successfully purified by anion exchange HPLC. The failure to detect binding of the 111In-Gamide, 106Ru-Gamide and 68Ga-Gamide complexes to the CCK2R suggests that formation of these complexes will not be useful for the detection of tumours expressing this receptor, but may instead provide alternative ways to block the actions of Gamide as a growth factor or a stimulant of gastric acid secretion. The complexes between the hormone gastrin and radioactive 111In, 106Ru or 68Ga ions were purified by anion exchange HPLC using a NaCl gradient. The failure to detect binding of the complexes to the cholecystokinin 2 receptor suggests that metal ion treatment may provide novel approaches to block the biological actions of gastrin.
DOI: 10.1007/s00775-017-1478-8
ORCID: 0000-0002-6656-295X
Journal: Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry
PubMed URL: 28702751
Type: Journal Article
Subjects: Gallium
Appears in Collections:Journal articles

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