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99m Tc-(Hydrazinonicotinic acid-β-Ala-Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH 2)(tricine)(TPPTS)

Kam Leung

PMID: 20641678

Abstract:

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 7 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 (CNS) and the gastrointestinal (GI) system. They also act as potential growth factors for both normal and neoplastic tissues (3). Specific BBN receptors (BBN-R) have been identified on CNS and GI tissues and a number of tumor cell lines (4). The BBN-R superfamily includes at least 4 different subtypes, namely neuromedin B (NMB or BB1), the GRPR subtype (BB2), BB3, and BB4. 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).
Shi et al. (7) have used a ternary ligand system (HYNIC, tricine and TPPTS) for labeling β-Ala-Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH2 (ABN). HYNIC (hydrazinonicotinic acid) is a bifunctional coupling agent for 99mTc-labeling, while tricine and TPPTS (trisodium triphenylphosphine-3,3',3''-trisulfonate) were used as coligands to prepare the ternary ligand complex [99mTc(HYNIC-ABN)(tricine)(TPPTS)] for SPECT imaging GRPR of colon cancer.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP39537230-B Ala-Gln Ala-Gln 39537-23-0 Price
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