ArticleBioconjugate chemistry
Synthesis and evaluation of bivalent NDP-alpha-MSH(7) peptide ligands for binding to the human melanocortin receptor 4 (hMC4R).
Article in Bioconjugate chemistry. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 60 citations in OpenAlex.
- ScrepYard: An online resource for disulfide-stabilized tandem repeat peptides.Protein science : a publication of the Protein Society · 2023Article
- Peptidomimetic-based antibody surrogate for HER2.Acta pharmaceutica Sinica. B · 2021Article
- 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
- Bench-top to clinical therapies: A review of melanocortin ligands from 1954 to 2016.Biochimica et biophysica acta. Molecular basis of disease · 2017Review
- A unique mid-sequence linker used to multimerize the lipid-phosphatidylserine (PS) binding peptide-peptoid hybrid PPS1.European journal of medicinal chemistry · 2017Article
- A Direct in Vivo Comparison of the Melanocortin Monovalent Agonist Ac-His-DPhe-Arg-Trp-NHACS chemical neuroscience · 2017Article
- Design, synthesis, and biological characterization of novel PEG-linked dimeric modulators for CXCR4.Bioorganic & medicinal chemistry · 2016Article
- 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
- Synthesis and evaluation of multivalent M2pep peptides for targeting alternatively activated M2 macrophages.Journal of controlled release : official journal of the Controlled Release Society · 2016Article
- Development of Follicle-Stimulating Hormone Receptor Binding Probes to Image Ovarian Xenografts.Journal of biotechnology & biomaterials · 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
- Synthesis and evaluation of bivalent ligands for binding to the human melanocortin-4 receptor.Bioorganic & medicinal chemistry · 2014Article
- Hetero-bivalent GLP-1/glibenclamide for targeting pancreatic β-cells.Chembiochem : a European journal of chemical biology · 2014Article
- Polydopamine-enabled surface functionalization of gold nanorods for cancer cell-targeted imaging and photothermal therapy.Nanomedicine (London, England) · 2013Article
- Evaluation of novel 99mTc(I)-labeled homobivalent α-melanocyte-stimulating hormone analogs for melanocortin-1 receptor targeting.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2012Article
- Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand.Journal of medicinal chemistry · 2011Article
- A sucrose-derived scaffold for multimerization of bioactive peptides.Bioorganic & medicinal chemistry · 2011Article
- Design, synthesis, and biological studies of efficient multivalent melanotropin ligands: tools toward melanoma diagnosis and treatment.Journal of medicinal chemistry · 2011Article
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
We demonstrate the potential utility of multivalent ligands as targeting agents for cancer imaging or therapy by determining the binding of homobivalent ligands to their corresponding receptors. This manuscript details the synthesis and evaluation of a series of bivalent ligands containing two copies of the truncated heptapeptide version of [Nle4-D-Phe7]-alpha-melanocyte stimulating hormone (NDP-alpha-MSH), referred to as MSH(7). These were connected with various semirigid linkers containing Pro-Gly repeats, with or without flexible poly(ethylene glycol) (PEGO) moieties at their termini. Modeling data suggest a distance of 20-50 A between the ligand binding sites of two adjacent G-protein coupled receptors, GPCRs. These bivalent ligands were observed to bind with higher affinity compared to their monovalent counterparts. Data suggest these ligands may be capable of cross-linking adjacent receptors. An optimal linker length of 25 +/- 10 A, inferred from these ligands, correlated well with the inter-receptor distance estimated through modeling. Although there was no difference in maximal binding affinities between the ligands constructed with the Pro-Gly repeats versus those constructed with the PEGO inserts, the PEGO-containing ligands bound with high affinities over a greater range of linker lengths.
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