ArticleJournal of medicinal chemistry2011
Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
What it found
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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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
29 citing papers in PubMed, 46 citations in OpenAlex.
- Synthesis and in vivo evaluation of a bifunctional, glutamic acid derived chelator for theEJNMMI radiopharmacy and chemistry · 2026Article
- Advances in Materials Science for Precision Melanoma Therapy: Nanotechnology-Enhanced Drug Delivery Systems.Pharmaceutics · 2025Review
- Preclinical evaluation of [European journal of nuclear medicine and molecular imaging · 2021Article
- 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
- Melanocortin 5 receptor signaling pathway in health and disease.Cellular and molecular life sciences : CMLS · 2020Review
- Ultrasensitive detection of malignant melanoma using PET molecular imaging probes.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Melanocortin 1 Receptor-Targeted α-Particle Therapy for Metastatic Uveal Melanoma.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2019Article
- Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist.Journal of medicinal chemistry · 2019Article
- Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors.Journal of medicinal chemistry · 2019Article
- Melanocortin-1 Receptor-Targeting Ultrasmall Silica Nanoparticles for Dual-Modality Human Melanoma Imaging.ACS applied materials & interfaces · 2018Article
- PET and SPECT imaging of melanoma: the state of the art.European journal of nuclear medicine and molecular imaging · 2018Review
- Bench-top to clinical therapies: A review of melanocortin ligands from 1954 to 2016.Biochimica et biophysica acta. Molecular basis of disease · 2017Review
- NMR Insights into the Structure-Function Relationships in the Binding of Melanocortin Analogues to the MC1R Receptor.Molecules (Basel, Switzerland) · 2017Article
- Self-assembling Morphologies Obtained from Helical Polycarbodiimide Copolymers and Their Triazole Derivatives.Journal of visualized experiments : JoVE · 2017Article
- An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.Journal of medicinal chemistry · 2016Article
- The Melanocortin Receptor System: A Target for Multiple Degenerative Diseases.Current protein & peptide science · 2016Review
- In situ gelling silk-elastinlike protein polymer for transarterial chemoembolization.Biomaterials · 2015Article
- Development of a time-resolved fluorescence probe for evaluation of competitive binding to the cholecystokinin 2 receptor.Bioorganic & medicinal chemistry · 2015Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 1 country.
Funding
Abstract
The incidence of malignant melanoma is rising faster than that of any other cancer in the United States. Because of its high expression on the surface of melanomas, MC1R has been investigated as a target for selective imaging and therapeutic agents against melanoma. Eight ligands were screened against cell lines engineered to overexpress MC1R, MC4R, or MC5R. Of these, compound 1 (4-phenylbutyryl-His-dPhe-Arg-Trp-NH(2)) exhibited high (0.2 nM) binding affinity for MC1R and low (high nanomolar) affinities for MC4R and MC5R. Functionalization of the ligand at the C-terminus with an alkyne for use in Cu-catalyzed click chemistry was shown not to affect the binding affinity. Finally, formation of the targeted polymer, as well as the targeted micelle formulation, also resulted in constructs with low nanomolar binding affinity.
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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.