ArticleNuclear medicine and biology2014
A heterodimeric [RGD-Glu-[(64)Cu-NO2A]-6-Ahx-RM2] αvβ3/GRPr-targeting antagonist radiotracer for PET imaging of prostate tumors.
Article in Nuclear medicine and biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- Molecular targets and the emerging role of copper radionuclides in prostate cancer theranostics.EJNMMI research · 2025Review
- Survival benefit of radical prostatectomy for non-metastatic prostate cancer: a propensity score-matched SEER database analysis.International urology and nephrology · 2025Article
- Fibroblast activation protein targeting radiopharmaceuticals: From drug design to clinical translation.Acta pharmaceutica Sinica. B · 2025Review
- Bispecific Radioligands (BRLs): Two Is Better Than One.Journal of clinical medicine · 2025Review
- Elevating theranostics: The emergence and promise of radiopharmaceutical cell-targeting heterodimers in human cancers.iRadiology · 2024Article
- Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy.Pharmaceuticals (Basel, Switzerland) · 2020Review
- Photo-Click-Facilitated Screening Platform for the Development of Hetero-Bivalent Agents with High Potency.The Journal of organic chemistry · 2020Article
- New Frontiers in Molecular Imaging Using Peptide-Based Radiopharmaceuticals for Prostate Cancer.Frontiers in chemistry · 2020Review
- Recent applications of a single quadrupole mass spectrometer inJournal of fluorine chemistry · 2018Article
- In Vitro Mouse and Human Serum Stability of a Heterobivalent Dual-Target Probe That Has Strong Affinity to Gastrin-Releasing Peptide and Neuropeptide Y1 Receptors on Tumor Cells.Cancer biotherapy & radiopharmaceuticals · 2017Article
- Clinical Translation of a Dual Integrin αvβ3- and Gastrin-Releasing Peptide Receptor-Targeting PET Radiotracer, 68Ga-BBN-RGD.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2017Article
- A Comprehensive Evaluation of the Activity and Selectivity Profile of Ligands for RGD-binding Integrins.Scientific reports · 2017Article
- Bombesin related peptides/receptors and their promising therapeutic roles in cancer imaging, targeting and treatment.Expert opinion on therapeutic targets · 2016Review
- Detection of pulmonary metastases with the novel radiolabeled molecular probe, (99m)Tc-RRL.International journal of clinical and experimental medicine · 2015Article
- Matched-pair,Nuclear medicine and biologyArticle
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11 authors.
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Abstract
introductionIn the present study, we describe a (64)Cu-radiolabeled heterodimeric peptide conjugate for dual αvβ3/GRPr (αvβ3 integrin/gastrin releasing peptide receptor) targeting of the form [RGD-Glu-[(64)Cu-NO2A]-6-Ahx-RM2] (RGD: the amino acid sequence [Arg-Gly-Asp], a nonregulatory peptide used for αvβ3 integrin receptor targeting; Glu: glutamic acid; NO2A: 1,4,7-triazacyclononane-1,4-diacetic acid; 6-Ahx: 6-amino hexanoic acid; and RM2: (D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2), an antagonist analogue of bombesin (BBN) peptide used for GRPr targeting).
methodsRGD-Glu-6Ahx-RM2] was conjugated to a NOTA (1,4,7-triazacyclononane-1,4,7-triacetic acid) complexing agent to produce [RGD-Glu-[NO2A]-6-Ahx-RM2], which was purified by reversed-phase high-performance liquid chromatography (RP-HPLC) and characterized by electrospray ionization-mass spectrometry (ESI-MS). Radiolabeling of the conjugate with (64)Cu produced [RGD-Glu-[(64)Cu-NO2A]-6-Ahx-RM2 in high radiochemical yield (≥95%). In vivo behavior of the radiolabeled peptide conjugate was investigated in normal CF-1 mice and in the PC-3 human prostate cancer experimental model.
resultsA competitive displacement receptor binding assay in human prostate PC-3 cells using (125)I-[Tyr(4)]BBN as the radioligand showed high binding affinity of [RGD-Glu-[(nat)Cu-NO2A]-6-Ahx-RM2] conjugate for the GRPr (3.09±0.34 nM). A similar assay in human, glioblastoma U87-MG cells using (125)I-Echistatin as the radioligand indicated a moderate receptor-binding affinity for the αvβ3 integrin (518±37.5 nM). In vivo studies of [RGD-Glu-[(64)Cu-NO2A]-6-Ahx-RM2] showed high accumulation (4.86±1.01 %ID/g, 1h post-intravenous injection (p.i.)) and prolonged retention (4.26±1.23 %ID/g, 24h p.i.) of tracer in PC-3 tumor-bearing mice. Micro-positron emission tomography (microPET) molecular imaging studies produced high-quality, high contrast images in PC-3 tumor-bearing mice at 4h p.i.
conclusionsThe favorable pharmacokinetics and enhanced tumor uptake of (64)Cu-NOTA-RGD-Glu-6Ahx-RM2 warrant further investigations for dual integrin and GRPr-positive tumor imaging and possible radiotherapy.
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