ArticleJournal of medicinal chemistry2011
Design, synthesis, and biological studies of efficient multivalent melanotropin ligands: tools toward melanoma diagnosis and treatment.
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 28 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.
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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.
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Who cites it
28 citing papers in PubMed, 43 citations in OpenAlex.
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- Simultaneous ultrasound- and microwave-assisted one-pot 'click' synthesis of 3-formyl-indole clubbed 1,2,3-triazole derivatives and their biological evaluation.Molecular diversity · 2022Article
- On the role of phase separation in the biogenesis of membraneless compartments.The EMBO journal · 2022Article
- Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy.Pharmaceuticals (Basel, Switzerland) · 2020Review
- 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
- Multivalent activation of GLP-1 and sulfonylurea receptors modulates β-cell second-messenger signaling and insulin secretion.American journal of physiology. Cell physiology · 2019Article
- Bench-top to clinical therapies: A review of melanocortin ligands from 1954 to 2016.Biochimica et biophysica acta. Molecular basis of disease · 2017Review
- A Direct in Vivo Comparison of the Melanocortin Monovalent Agonist Ac-His-DPhe-Arg-Trp-NHACS chemical neuroscience · 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
- Small Molecule Radiopharmaceuticals - A Review of Current Approaches.Frontiers in medicine · 2016Review
- Plasticity of an ultrafast interaction between nucleoporins and nuclear transport receptors.Cell · 2015Article
- Design, synthesis and biological evaluation of multifunctional ligands targeting opioid and bradykinin 2 receptors.Bioorganic & medicinal chemistry letters · 2015Article
- A Synthetic Heterobivalent Ligand Composed of Glucagon-Like Peptide 1 and Yohimbine Specifically Targets β Cells Within the Pancreas.Molecular imaging and biology · 2015Article
- Synthesis and bioactivity of MSH4 oligomers prepared by an ATetrahedron letters · 2015Article
- Trigonal scaffolds for multivalent targeting of melanocortin receptors.Organic & biomolecular chemistry · 2015Article
- Recent advances in engineering polyvalent biological interactions.Biomacromolecules · 2015Review
- In vitro and in vivo pharmacological characterization of nociceptin/orphanin FQ tetrabranched derivatives.British journal of pharmacology · 2014Article
- Hetero-bivalent GLP-1/glibenclamide for targeting pancreatic β-cells.Chembiochem : a European journal of chemical biology · 2014Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
To achieve early detection and specific cancer treatment, we propose the use of multivalent interactions in which a series of binding events leads to increased affinity and consequently to selectivity. Using melanotropin (MSH) ligands, our aim is to target melanoma cells which overexpress melanocortin receptors. In this study, we report the design and efficient synthesis of new trivalent ligands bearing MSH ligands. Evaluation of these multimers on a cell model engineered to overexpress melanocortin 4 receptors (MC4R) showed up to a 350-fold increase in binding compared to the monomer, resulting in a trivalent construct with nanomolar affinity starting from a micromolar affinity ligand. Cyclic adenosine monophosphate (cAMP) production was also investigated, leading to more insights into the effects of multivalent compounds on transduction mechanisms.
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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.