ArticleMolecular imaging and biology2013
Effects of chelator modifications on (68)Ga-labeled [Tyr (3)]octreotide conjugates.
Article in Molecular imaging and biology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 32 citations in OpenAlex.
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- The effects of novel macrocyclic chelates on the targeting properties of theEJNMMI research · 2023Article
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- Positron Emission Tomography Imaging of Prostate Cancer with Ga-68-Labeled Gastrin-Releasing Peptide Receptor Agonist BBNBioconjugate chemistry · 2018Article
- Preliminary PET/CT Imaging with Somatostatin Analogs [Molecular imaging and biology · 2017Article
- DATATOC: a novel conjugate for kit-typeEJNMMI radiopharmacy and chemistry · 2017Article
- Preclinical evaluation of [(68)Ga]NOTA-pentixafor for PET imaging of CXCR4 expression in vivo - a comparison to [(68)Ga]pentixafor.EJNMMI research · 2016Article
- Evaluation of Cu-64 and Ga-68 Radiolabeled Glucagon-Like Peptide-1 Receptor Agonists as PET Tracers for Pancreatic β cell Imaging.Molecular imaging and biology · 2016Article
- Underscoring the influence of inorganic chemistry on nuclear imaging with radiometals.Inorganic chemistry · 2014Article
- Positron emission tomographic imaging of copper 64- and gallium 68-labeled chelator conjugates of the somatostatin agonist tyr3-octreotate.Molecular imaging · 2014Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
purposeSomatostatin receptors (SSTR) have been reported as promising targets for imaging agents for cancer. Recently, (68)Ga-DOTATOC-based PET imaging has been used successfully for diagnosis and management of SSTR-expressing tumors. The purpose of this study was to evaluate the influence of chelator modifications and charge on (68)Ga-labeled peptide conjugates. PROCEDURES: We have synthesized a series of [Tyr(3)]octreotide conjugates that consisted of different NOTA-based chelators with two to five carboxylate moieties, and compared our results with (68)Ga-DOTATOC in both in vitro and in vivo studies.
resultsWith the exception of (68)Ga-1 (three carboxylates), the increased number of carboxylates on the NOTA-based chelators resulted in a reduced binding affinity and internalization. Additionally, the tumor uptake for (68)Ga-2 (four carboxylates) and (68)Ga-3 (five carboxylates) was reduced compared to that of (68)Ga-DOTATOC (three carboxylates) and (68)Ga-NO2ATOC (two carboxylates) and (68)Ga-1 (three carboxylates) at 2 h p.i. suggesting the presence of an optimal charge for this compound.
conclusionsChelator modifications can lead to the altered pharmacokinetics. These results may impact further design considerations for peptide-based imaging agents.
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