ArticleBioconjugate chemistry2008
Design, synthesis, and biological evaluation of an antagonist-bombesin analogue as targeting vector.
Article in Bioconjugate chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
18 citing papers in PubMed, 55 citations in OpenAlex.
- Development of bombesin-tubulysin conjugates using multicomponent chemistry to functionalize both the payload and the homing peptide.Frontiers in pharmacology · 2024Article
- Copper-67-Labeled Bombesin Peptide for Targeted Radionuclide Therapy of Prostate Cancer.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Stability Evaluation and Stabilization of a Gastrin-Releasing Peptide Receptor (GRPR) Targeting Imaging Pharmaceutical.Molecules (Basel, Switzerland) · 2019Article
- The tetraamine chelator outperforms HYNIC in a new technetium-99m-labelled somatostatin receptor 2 antagonist.EJNMMI research · 2018Article
- Comparison of [(11)C]Choline ([(11)C]CHO) and [(18)F]Bombesin (BAY 86-4367) as Imaging Probes for Prostate Cancer in a PC-3 Prostate Cancer Xenograft Model.Molecular imaging and biology · 2016Article
- Synthesis and biological evaluation of copper-64 radiolabeled [DUPA-6-Ahx-(NODAGA)-5-Ava-BBN(7-14)NH2], a novel bivalent targeting vector having affinity for two distinct biomarkers (GRPr/PSMA) of prostate cancer.Nuclear medicine and biology · 2014Article
- A comparative study of radiolabeled bombesin analogs for the PET imaging of prostate cancer.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2013Article
- Synthesis and in vitro and in vivo evaluation of hypoxia-enhanced 111In-bombesin conjugates for prostate cancer imaging.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2013Article
- Evaluation of fluorine-labeled gastrin-releasing peptide receptor (GRPR) agonists and antagonists by LC/MS.Amino acids · 2012Article
- Radiolabelled peptides for oncological diagnosis.European journal of nuclear medicine and molecular imaging · 2012Review
- Article
- The development of copper radiopharmaceuticals for imaging and therapy.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2011Review
- F-Labeled GRPR Agonists and Antagonists: A Comparative Study in Prostate Cancer Imaging.Theranostics · 2011Article
- Bombesin receptor-mediated imaging and cytotoxicity: review and current status.Current drug delivery · 2011Review
- Development of a potent DOTA-conjugated bombesin antagonist for targeting GRPr-positive tumours.European journal of nuclear medicine and molecular imaging · 2011Article
- Gastrin-releasing peptide links stressor to cancer progression.Journal of cancer research and clinical oncology · 2010Review
- Gastrin releasing protein receptor specific gold nanorods: breast and prostate tumor avid nanovectors for molecular imaging.Nano letters · 2009Article
- Radiolabelled GLP-1 analogues for in vivo targeting of insulinomas.Contrast media & molecular imagingArticle
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
The gastrin releasing peptide receptor (GRP-R) is overexpressed on a number of tumors and cancer cell lines including pancreas, prostate, breast, gastrointestinal, and small cell lung cancer (SCLC). Radiolabeled bombesin (BBN) analogues have exhibited high binding affinity and specificity to the GRP-R. A bombesin analogue with an antagonist targeting vector at the C-terminus, DOTA-aminohexanoyl-[D-Phe(6), Leu-NHCH 2CH 2CH3(13), des Met(14)] BBN[6-14] (1, "Bomproamide"), has been synthesized and displays high binding affinity (IC50 = 1.36 +/- 0.09 nM) against (125)I-Tyr (4)-BBN in in vitro competitive assays using PC-3 cells. Maximum internalization of (111)In-1 reached 14% in PC-3 cells after 45 min of incubation. Rapid (0.25 h PI) and high (12.21 +/- 3.2%ID/g) pancreatic uptake of (111)In-1 was observed in healthy CF-1 mice, and 90% of the activity was blocked by coinjection of 100 mug of BBN. Rapid (0.25 h PI) and high uptake (6.90 +/- 1.06%ID/g) was observed in PC-3 prostate cancer xenografts in SCID mice, as well as visualized clearly in a SPECT/CT study. These results support the use of a bombesin construct with an antagonist C-terminal vector as a candidate of choice for specific in vivo imaging of tumors overexpressing GRP-receptors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.