ArticleEJNMMI research2016
Discovery and characterization of a high-affinity and high-specificity peptide ligand LXY30 for in vivo targeting of α3 integrin-expressing human tumors.
Article in EJNMMI research, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 33 citations in OpenAlex.
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- The epidermal integrin-mediated secretome regulates the skin microenvironment during tumorigenesis and repair.Matrix biology : journal of the International Society for Matrix Biology · 2024Review
- Modified bone marrow mesenchymal stem cells derived exosomes loaded with MiRNA ameliorates non-small cell lung cancer.Journal of cellular and molecular medicine · 2024Article
- Programmable Bispecific Nano-immunoengager That Captures T Cells and Reprograms Tumor Microenvironment.Nano letters · 2022Article
- Development and Characterization of a Novel Peptide-Drug Conjugate with DM1 for Treatment of FGFR2-Positive Tumors.Biomedicines · 2021Article
- High integrin α3 expression is associated with poor prognosis in patients with non-small cell lung cancer.Translational lung cancer research · 2020Article
- Transformable peptide nanoparticles arrest HER2 signalling and cause cancer cell death in vivo.Nature nanotechnology · 2020Article
- Research Progress Evaluating the Function and Mechanism of Anti-Tumor Peptides.Cancer management and research · 2020Review
- Extracellular Matrix Mimicking Nanofibrous Scaffolds Modified With Mesenchymal Stem Cell-Derived Extracellular Vesicles for Improved Vascularization.Frontiers in bioengineering and biotechnology · 2020Article
- One-bead one-compound combinatorial library derived targeting ligands for detection and treatment of oral squamous cancer.Oncotarget · 2019Article
- High-affinity peptide ligand LXY30 for targeting α3β1 integrin in non-small cell lung cancer.Journal of hematology & oncology · 2019Article
- Identification of integrin drug targets for 17 solid tumor types.Oncotarget · 2018Article
- Surface Functionalization of Hepatitis E Virus Nanoparticles Using Chemical Conjugation Methods.Journal of visualized experiments : JoVE · 2018Article
- A Novel Galectin-1 Inhibitor Discovered through One-Bead Two-Compound Library Potentiates the Antitumor Effects of PaclitaxelMolecular cancer therapeutics · 2017Article
- Targeting Tumor-Associated Exosomes with Integrin-Binding Peptides.Advanced biosystems · 2017Article
- High-Throughput Approaches to the Development of Molecular Imaging Agents.Molecular imaging and biology · 2017Review
- Tumor-targeting peptides from combinatorial libraries.Advanced drug delivery reviews · 2017Review
- Dominant Suppression of β1 Integrin by Ectopic CD98-ICD Inhibits Hepatocellular Carcinoma Progression.International journal of molecular sciences · 2016Article
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Authors and funding
14 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundα3β1 integrin is overexpressed in several types of human cancer and is associated with poor prognosis, metastasis, and resistance to cancer treatment. We previously identified a cyclic peptide ligand LXY1 that specifically binds to the α3β1 integrin on human glioblastoma U-87MG cells. Here, we optimized LXY1 through one-bead one-compound combinatorial library screening and site-specific modifications to improve its in vivo binding property.
methodsThree bead libraries were synthesized and whole-cell binding assays were performed. The binding capacity of individual peptide ligands against different tumor cells was determined by flow cytometry and confirmed by optical imaging. A complex joining biotinylated ligand with streptavidin-Cy5.5 was used for in vivo target imaging in both subcutaneous and orthotopic U-87MG xenograft mouse models.
resultsLXY30, a cyclic peptide with the sequence cdG-Phe(3,5-diF)-G-Hyp-NcR, emerged as the most potent and selective ligand for the α3 subunit of α3β1 integrin with improved in vitro and in vivo tumor-targeting effects compared to LXY1 in U-87MG cells. LXY30 is considerably stable in plasma as demonstrated in an in vitro stability study in 90 % human plasma. LXY30 also binds to several other known α3β1 integrin-expressing glioblastoma, lung, and breast cancer cell lines with various affinities.
conclusionsOur data support further investigating the role of LXY30 as a human tumor-targeting peptide ligand for systemic and intracranial delivery of imaging agents and cancer therapeutics.
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