ArticleBioconjugate chemistry2012
Synthesis and characterization of a melanoma-targeted fluorescence imaging probe by conjugation of a melanocortin 1 receptor (MC1R) specific ligand.
Article in Bioconjugate chemistry, 2012. 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, 33 citations in OpenAlex.
- Amelanotic Melanoma-Biochemical and Molecular Induction Pathways.International journal of molecular sciences · 2024Review
- Investigation of the Effect on the Albumin Binding Moiety for the Pharmacokinetic Properties ofPharmaceuticals (Basel, Switzerland) · 2023Article
- Skin Cancer Pathobiology at a Glance: A Focus on Imaging Techniques and Their Potential for Improved Diagnosis and Surveillance in Clinical Cohorts.International journal of molecular sciences · 2023Review
- Lipophilicity Determines Routes of Uptake and Clearance, and Toxicity of an Alpha-Particle-Emitting Peptide Receptor Radiotherapy.ACS pharmacology & translational science · 2021Article
- Biodistribution and Multicompartment Pharmacokinetic Analysis of a Targeted α Particle Therapy.Molecular pharmaceutics · 2020Article
- Development of Ligand-Drug Conjugates Targeting Melanoma through the Overexpressed Melanocortin 1 Receptor.ACS pharmacology & translational science · 2020Article
- Ultrasensitive detection of malignant melanoma using PET molecular imaging probes.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Assessment of Nonradioactive Multispectral Optoacoustic Tomographic Imaging With Conventional Lymphoscintigraphic Imaging for Sentinel Lymph Node Biopsy in Melanoma.JAMA network open · 2019Article
- Melanocortin 1 Receptor-Targeted α-Particle Therapy for Metastatic Uveal Melanoma.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2019Article
- PET and SPECT imaging of melanoma: the state of the art.European journal of nuclear medicine and molecular imaging · 2018Review
- Cell-surface marker discovery for lung cancer.Oncotarget · 2017Article
- Delta-Opioid Receptor (δOR) Targeted Near-Infrared Fluorescent Agent for Imaging of Lung Cancer: Synthesis and Evaluation In Vitro and In Vivo.Bioconjugate chemistry · 2016Article
- Trigonal scaffolds for multivalent targeting of melanocortin receptors.Organic & biomolecular chemistry · 2015Article
- Nanoparticle ligand presentation for targeting solid tumors.AAPS PharmSciTech · 2014Review
- BMVC test, an improved fluorescence assay for detection of malignant pleural effusions.Cancer medicine · 2014Article
- Development and in vivo quantitative magnetic resonance imaging of polymer micelles targeted to the melanocortin 1 receptor.Journal of medicinal chemistry · 2013Article
- In vivo and in silico pharmacokinetics and biodistribution of a melanocortin receptor 1 targeted agent in preclinical models of melanoma.Molecular pharmaceutics · 2013Article
- Molecular Imaging and Radionuclide Therapy of Melanoma Targeting the Melanocortin 1 Receptor.Molecular imagingReview
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
The incidence of malignant melanoma is rising more rapidly than that of any other cancer in the United States. The melanocortin 1 receptor (MC1R) is overexpressed in most human melanoma metastases, thus making it a promising target for imaging and therapy of melanomas. We have previously reported the development of a peptidomimetic ligand with high specificity and affinity for MC1R. Here, we have conjugated near-infrared fluorescent dyes to the C-terminus of this ligand via lysine-mercaptopropionic acid linkers to generate MC1R specific optical probes (MC1RL-800, 0.4 nM K(i); and MC1RL-Cy5, 0.3 nM K(i)). Internalization of the imaging probe was studied in vitro by fluorescence microscopy using engineered A375/MC1R cells and B16F10 cells with endogenous MC1R expression. The in vivo tumor targeting of MC1RL-800 was evaluated by intravenous injection of probe into nude mice bearing bilateral subcutaneous A375 xenograft tumors with low MC1R expression and engineered A375/MC1R tumors with high receptor expression. Melanotic B16F10 xenografts were also studied. Fluorescence imaging showed that the agent has higher uptake values in tumors with high expression compared to low (p < 0.05), demonstrating the effect of expression levels on image contrast-to-noise. In addition, tumor uptake was significantly blocked by coinjection of excess NDP-α-MSH peptide (p < 0.05). In conclusion, the MC1R-specific imaging probe developed in this study displays excellent potential for the intraoperative detection of regional node involvement and for margin detection during melanoma metastasis resection.
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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.