| pubmed-article:21544226 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:21544226 | lifeskim:mentions | umls-concept:C0376358 | lld:lifeskim |
| pubmed-article:21544226 | lifeskim:mentions | umls-concept:C0011923 | lld:lifeskim |
| pubmed-article:21544226 | lifeskim:mentions | umls-concept:C1415314 | lld:lifeskim |
| pubmed-article:21544226 | lifeskim:mentions | umls-concept:C1579762 | lld:lifeskim |
| pubmed-article:21544226 | lifeskim:mentions | umls-concept:C0009491 | lld:lifeskim |
| pubmed-article:21544226 | lifeskim:mentions | umls-concept:C0682770 | lld:lifeskim |
| pubmed-article:21544226 | pubmed:dateCreated | 2011-5-6 | lld:pubmed |
| pubmed-article:21544226 | pubmed:abstractText | Radiolabeled bombesin analogs are promising probes for cancer imaging of gastrin-releasing peptide receptor (GRPR). In this study, we developed (18)F-labeled GRPR agonists and antagonists for positron emission tomography (PET) imaging of prostate cancer. GRPR antagonists ATBBN (D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-NHCH(2)CH(3)) and MATBBN (Gly-Gly-Gly-Arg-Asp-Asn-D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-NHCH(2)CH(3)), and agonists AGBBN (Gln-Trp-Ala-Val-Gly-His-Leu-MetNH(2)) and MAGBBN (Gly-Gly-Gly-Arg-Asp-Asn-Gln-Trp-Ala-Val-Gly-His-Leu-MetNH(2)) were radiolabeled with (18)F via 4-nitrophenyl 2-(18)F-fluoropropionate. The in vitro receptor binding, cell uptake, and efflux properties of the radiotracers were studied on PC-3 cells. An in vivo PET study was performed on mice bearing PC-3 tumors. Direct (18)F-labeling of known GRPR antagonist ATBBN and agonist AGBBN did not result in good tumor targeting or appropriate pharmacokinetics. Modification was made by introducing a highly hydrophilic linker Gly-Gly-Gly-Arg-Asp-Asn. Higher receptor binding affinity, much higher cell uptake and slower washout were observed for the agonist (18)F-FP-MAGBBN over the antagonist (18)F-FP-MATBBN. Both tracers showed good tumor/background contrast, with the agonist (18)F-FP-MAGBBN having significantly higher tumor uptake than the antagonist (18)F-FP-MATBBN (P < 0.01). In conclusion, Gly-Gly-Gly-Arg-Asp-Asn linker significantly improved the pharmacokinetics of the otherwise hydrophobic BBN radiotracers. (18)F-labeled BBN peptide agonists may be the probes of choice for prostate cancer imaging due to their relatively high tumor uptake and retention as compared with the antagonist counterparts. | lld:pubmed |
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| pubmed-article:21544226 | pubmed:language | eng | lld:pubmed |
| pubmed-article:21544226 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:21544226 | pubmed:status | PubMed-not-MEDLINE | lld:pubmed |
| pubmed-article:21544226 | pubmed:issn | 1838-7640 | lld:pubmed |
| pubmed-article:21544226 | pubmed:author | pubmed-author:ChaiM CMC | lld:pubmed |
| pubmed-article:21544226 | pubmed:author | pubmed-author:MaYingY | lld:pubmed |
| pubmed-article:21544226 | pubmed:author | pubmed-author:LangLixinL | lld:pubmed |
| pubmed-article:21544226 | pubmed:author | pubmed-author:YangMinM | lld:pubmed |
| pubmed-article:21544226 | pubmed:author | pubmed-author:ChenXiaoyuanX | lld:pubmed |
| pubmed-article:21544226 | pubmed:author | pubmed-author:NiuGangG | lld:pubmed |
| pubmed-article:21544226 | pubmed:author | pubmed-author:YanYongjunY | lld:pubmed |
| pubmed-article:21544226 | pubmed:author | pubmed-author:GaoHaokaoH | lld:pubmed |
| pubmed-article:21544226 | pubmed:author | pubmed-author:QuanQimengQ | lld:pubmed |
| pubmed-article:21544226 | pubmed:author | pubmed-author:ZhouYaruY | lld:pubmed |
| pubmed-article:21544226 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:21544226 | pubmed:volume | 1 | lld:pubmed |
| pubmed-article:21544226 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:21544226 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:21544226 | pubmed:pagination | 220-9 | lld:pubmed |
| pubmed-article:21544226 | pubmed:dateRevised | 2011-7-28 | lld:pubmed |
| pubmed-article:21544226 | pubmed:year | 2011 | lld:pubmed |
| pubmed-article:21544226 | pubmed:articleTitle | F-Labeled GRPR Agonists and Antagonists: A Comparative Study in Prostate Cancer Imaging. | lld:pubmed |
| pubmed-article:21544226 | pubmed:affiliation | Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, Jiangsu, 214063, China. | lld:pubmed |
| pubmed-article:21544226 | pubmed:publicationType | Journal Article | lld:pubmed |
