ArticleNuclear medicine and biology2013
Comparison of two cross-bridged macrocyclic chelators for the evaluation of 64Cu-labeled-LLP2A, a peptidomimetic ligand targeting VLA-4-positive tumors.
Article in Nuclear medicine and biology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 38 citations in OpenAlex.
- Review
- Molecular targets and the emerging role of copper radionuclides in prostate cancer theranostics.EJNMMI research · 2025Review
- Evaluation of VLA-4 (Integrin α4β1) as a Shared Target for Radiopharmaceutical Therapy across Solid Tumors.Molecular cancer therapeutics · 2025Article
- NOTA and NODAGA Radionuclide Complexing Agents: Versatile Approaches for Advancements in Radiochemistry.Molecules (Basel, Switzerland) · 2025Review
- Current and Future PET Imaging for Multiple Myeloma.Life (Basel, Switzerland) · 2023Review
- NovelMolecular pharmaceutics · 2022Article
- It's Time to Shift the Paradigm: Translation and Clinical Application of Non-αvβ3 Integrin Targeting Radiopharmaceuticals.Cancers · 2021Review
- Advances in Receptor-Targeted Radiolabeled Peptides for Melanoma Imaging and Therapy.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2021Review
- Review
- Comparison of AlJournal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2020Article
- Identification, Characterization, and Optimization of Integrin αMolecules (Basel, Switzerland) · 2019Article
- Article
- PET and SPECT imaging of melanoma: the state of the art.European journal of nuclear medicine and molecular imaging · 2018Review
- High-Throughput Approaches to the Development of Molecular Imaging Agents.Molecular imaging and biology · 2017Review
- New Bifunctional Chelator p-SCN-PhPr-NE3TA for Copper-64: Synthesis, Peptidomimetic Conjugation, Radiolabeling, and Evaluation for PET Imaging.Inorganic chemistry · 2016Article
- PET imaging of very late antigen-4 in melanoma: comparison of 68Ga- and 64Cu-labeled NODAGA and CB-TE1A1P-LLP2A conjugates.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2014Article
- New radiotracers for imaging of vascular targets in angiogenesis-related diseases.Advanced drug delivery reviews · 2014Review
- Characterization and evaluation of (64)Cu-labeled A20FMDV2 conjugates for imaging the integrin αvβ 6.Molecular imaging and biology · 2014Article
- Chelators for copper radionuclides in positron emission tomography radiopharmaceuticals.Journal of labelled compounds & radiopharmaceuticals · 2014Review
- Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Integrin α(4)β(1) (also called very late antigen-4 or VLA-4) plays an important role in tumor growth, angiogenesis and metastasis, and there has been increasing interest in targeting this receptor for cancer imaging and therapy. In this study, we conjugated a peptidomimetic ligand known to have good binding affinity for α(4)β(1) integrin to a cross-bridged macrocyclic chelator with a methane phosphonic acid pendant arm, CB-TE1A1P. CB-TE1A1P-LLP2A was labeled with (64)Cu under mild conditions in high specific activity, in contrast to conjugates based on the "gold standard" di-acid cross-bridged chelator, CB-TE2A, which require high temperatures for efficient radiolabeling. Saturation binding assays demonstrated that (64)Cu-CB-TE1A1P-LLP2A had comparable binding affinity (1.2 nM vs 1.6 nM) but more binding sites (B(max)=471 fmol/mg) in B16F10 melanoma tumor cells than (64)Cu-CB-TE2A-LLP2A (B(max)=304 fmol/mg, p<0.03). In biodistribution studies, (64)Cu-CB-TE1A1P-LLP2A had less renal retention but higher uptake in tumor (11.4±2.3 %ID/g versus 3.1±0.6 %ID/g, p<0.001) and other receptor-rich tissues compared to(64)Cu-CB-TE2A-LLP2A. At 2h post-injection, (64)Cu-CB-TE1A1P-LLP2A also had significantly higher tumor:blood and tumor:muscle ratios than (64)Cu-CB-TE2A-LLP2A (CB-TE1A1P=19.5±3.0 and 13.0±1.4, respectively, CB-TE2A=4.2±1.4 and 5.5±0.9, respectively, p<0.001). These data demonstrate that (64)Cu-CB-TE1A1P-LLP2A is an excellent PET radiopharmaceutical for the imaging of α(4)β(1) positive tumors and also has potential for imaging other α(4)β(1) positive cells such as those of the pre-metastatic niche.
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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.