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68Ga-1,4,7,10-Tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid-Gly-Gly-Gly-Gly-Lys-Gly-Gly-Gly-Gly.


Leung K.


Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2008 Mar 01 [updated 2008 May 15].


Endothelial cells are important cells in inflammatory responses (1, 2). Bacterial lipopolysaccharide (LPS), virus, inflammation, and tissue injury increase tumor necrosis factor α (TNFα), interleukin-1 (IL-1), and other cytokine and chemokine secretion. Leukocyte emigration from blood is dependent on their ability to roll along endothelial cell surfaces and subsequently adhere to endothelial cell surfaces. Inflammatory mediators and cytokines induce chemokine secretion from endothelial cells and other vascular cells and increase their expression of cell-surface adhesion molecules, such as intracellular adhesion molecule-1 (ICAM-1), vascular cell adhesion molecule-1 (VCAM-1), integrins, and selectins. Chemokines are chemotactic toward leukocytes and toward sites of inflammation and tissue injury. The movements of leukocytes through endothelial junctions into the extravascular space are highly orchestrated through various interactions with different adhesion molecules on endothelial cells (3). Cell adhesion protein 1 (VAP-1) is not usually expressed on the cell surface of resting endothelial cells (4, 5). VAP-1 is a dual-function protein with adhesion properties and semicarbazide-sensitive monoamine oxidase (SSAO) activity. VAP-1 binds to its counterpart receptors on the cell surface of leukocytes. Inflammation increases expression of VAP-1 and other cell adhesion molecules on the vascular endothelial cells (4, 5), which leads to leukocyte adhesion to the activated endothelium and transmigration (6). Using a molecular model of VAP-1, a linear peptide of nine amino acids (Gly-Gly-Gly-Gly-Lys-Gly-Gly-Gly-Gly) (VAP-P1) was found to inhibit the SSAO activity of recombinant VAP-1 and block leukocyte–endothelium interactions (7). 68Ga (half-life = 68 min, 89% β+ decay) is an attractive radionuclide for labeling VAP-P1 and is readily available from a commercial 68Ge/68Ga generator (8). Cells retain 68Ga well, providing a good signal/background ratio. For evaluation as a positron emission tomography (PET) imaging agent for inflammatory and infectious processes in healing bones, 68Ga has been attached to VAP-P1 via 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA) to form 68Ga-DOTA-VAP-P1 (9).

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