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64Cu-1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid-cyclo(CGNSNPKSC).


Leung K1.


Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2012 Jan 30 [updated 2012 May 03].

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National for Biotechnology Information, NLM, NIH, Bethesda, MD


Angiogenesis is an essential process in the development of new blood vessels in normal physiological states and in diseases (1, 2). Targeting of tumor vasculature is a promising strategy for tumor imaging and therapy because tumor growth and metastasis largely depend on angiogenesis (3, 4). A cyclic 9-mer peptide (CGNSNPKSC (GX1)) was initially identified as a recognition motif for binding to the human gastric tumor vasculature (5-7). GX1 has also been shown to bind to a variety of human cancer vasculatures. The molecular target of GX1 has not been identified; however, GX1 inhibits endothelial cell proliferation in vitro and neovascularization in vivo. The Lys (K) residue of GX1 was conjugated with Cy5.5 to study in vivo biodistribution of the tracer in mice bearing U89MG human glioblastoma tumors (8). Cy5.5-GX1 exhibited high near-infrared fluorescence intensity in U89MG tumors in nude mice. For positron emission tomography (PET) imaging, 64Cu-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-GX1 (64Cu-DOTA-GX1) was prepared and evaluated in nude mice bearing U89MG tumors (9).

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