ArticleMolecular cancer therapeutics2009
Enhanced targeting with heterobivalent ligands.
Article in Molecular cancer therapeutics, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 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
32 citing papers in PubMed, 52 citations in OpenAlex.
- Development and biological evaluation of a novel CEACAM6-targeted PET tracer for distinguishing malignant nodules in early-stage lung adenocarcinoma.European journal of nuclear medicine and molecular imaging · 2025Article
- Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy.Pharmaceuticals (Basel, Switzerland) · 2020Review
- Multivalent activation of GLP-1 and sulfonylurea receptors modulates β-cell second-messenger signaling and insulin secretion.American journal of physiology. Cell physiology · 2019Article
- Dual-modal in vivo fluorescence and photoacoustic imaging using a heterodimeric peptide.Chemical communications (Cambridge, England) · 2018Article
- Multiplexed Targeting of Barrett's Neoplasia with a Heterobivalent Ligand: Imaging Study on Mouse Xenograft in Vivo and Human Specimens ex Vivo.Journal of medicinal chemistry · 2018Article
- 5-Ene-4-thiazolidinones - An efficient tool in medicinal chemistry.European journal of medicinal chemistry · 2017Review
- Bench-top to clinical therapies: A review of melanocortin ligands from 1954 to 2016.Biochimica et biophysica acta. Molecular basis of disease · 2017Review
- 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
- Tumor Targeting and Pharmacokinetics of a Near-Infrared Fluorescent-Labeled δ-Opioid Receptor Antagonist Agent, Dmt-Tic-Cy5.Molecular pharmaceutics · 2016Article
- 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
- Development of a time-resolved fluorescence probe for evaluation of competitive binding to the cholecystokinin 2 receptor.Bioorganic & medicinal chemistry · 2015Article
- Trigonal scaffolds for multivalent targeting of melanocortin receptors.Organic & biomolecular chemistry · 2015Article
- Design and applications of bispecific heterodimers: molecular imaging and beyond.Molecular pharmaceutics · 2014Review
- Peptides and peptidomimetics as immunomodulators.Immunotherapy · 2014Review
- Synthesis and characterization of time-resolved fluorescence probes for evaluation of competitive binding to melanocortin receptors.Bioorganic & medicinal chemistry · 2013Article
- Synthesis and evaluation of cholecystokinin trimers: a multivalent approach to pancreatic cancer detection and treatment.Bioorganic & medicinal chemistry letters · 2013Article
- Targeting receptor-mediated endocytotic pathways with nanoparticles: rationale and advances.Advanced drug delivery reviews · 2013Review
- Heterobivalent ligands target cell-surface receptor combinations in vivo.Proceedings of the National Academy of Sciences of the United States of America · 2012Article
- NIR-activated content release from plasmon resonant liposomes for probing single-cell responses.ACS nano · 2012Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
A novel approach to specifically target tumor cells for detection and treatment is the proposed use of heteromultivalent ligands, which are designed to interact with, and noncovalently crosslink, multiple different cell surface receptors. Although enhanced binding has been shown for synthetic homomultivalent ligands, proof of cross-linking requires the use of ligands with two or more different binding moieties. As proof-of-concept, we have examined the binding of synthetic heterobivalent ligands to cell lines that were engineered to coexpress two different G-protein-coupled human receptors, i.e., the human melanocortin 4 receptor (MC4R) expressed in combination with either the human delta-opioid receptor (deltaOR) or the human cholecystokinin-2 receptor (CCK2R). Expression levels of these receptors were characterized by time-resolved fluorescence saturation binding assays using Europium-labeled ligands; Eu-DPLCE, Eu-NDP-alpha-MSH, and Eu-CCK8 for the deltaOR, MC4R, and CCK2R, respectively. Heterobivalent ligands were synthesized to contain a MC4R agonist connected via chemical linkers to either a deltaOR or a CCK2R agonist. In both cell systems, the heterobivalent constructs bound with much higher affinity to cells expressing both receptors, compared with cells with single receptors or to cells where one of the receptors was competitively blocked. These results indicate that synthetic heterobivalent ligands can noncovalently crosslink two unrelated cell surface receptors, making feasible the targeting of receptor combinations. The in vitro cell models described herein will lead to the development of multivalent ligands for target combinations identified in human cancers.
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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.