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111In-1,4,7,10-Tetraazacyclododecane-1,4,7,10-triacetic acid-8-aminooctanoic acid-Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH2.

Authors

Leung K1.

Source

Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2012 Jun 20 [updated 2012 Oct 04].

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1
National Center for Biotechnology Information, NLM, NIH

Excerpt

The amphibian bombesin (BBN or BN, a peptide of 14 amino acids) is an analog of human gastrin-releasing peptide (GRP, a peptide of 27 amino acids) that binds to GRP receptors (GRPR) with high affinity and specificity (1, 2). Both GRP and BBN share an amidated C-terminus sequence homology of seven amino acids, Trp-Ala-Val-Gly-His-Leu-Met-NH2. BBN-Like peptides have been shown to induce various biological responses in diverse tissues, including the central nervous system and the gastrointestinal system. They also act as potential growth factors for both normal and neoplastic tissues (3). Specific BBN receptors (BBN-R) have been identified on central nervous system and gastrointestinal tissues and on a number of tumor cell lines (4). The BBN-R superfamily includes at least four different subtypes, namely the GRPR subtype (BB2), the neuromedin B (NMB) receptor subtype (BB1), the BB3 subtype, and the BB4 subtype. The findings of GRPR overexpression in various human tumors, such as breast, prostate, lung, colon, ovarian, and pancreatic cancers, provide opportunities for tumor imaging by designing specific molecular imaging agents to target the GRPR (5, 6). Various BBN analogs have been labeled with 99mTc and 111In for single-photon emission computed tomography (SPECT) imaging studies (7) and with 64Cu, 68Ga, and 86Y for positron emission tomography imaging studies (8, 9). Hoffman et al. (10) used 1,4,7,10-tetraazacyclododecane-1,4,7,10-triacetic acid (DOTA) as a bifunctional chelator for labeling 8-aminooctanoic acid-Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH2 (8-Aoc-BBN[7-14]NH2) with 111In (t1/2, 2.8 d). 111In-DOTA-8-Aoc-BBN[7-14]NH2 has been evaluated as a SPECT imaging agent of GRPR in nude mice bearing human PC-3 prostate cancer cells.

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