Evaluation of HER2-specific peptide ligand for its employment as radiolabeled imaging probe (340 views)
Sci Rep (ISSN: 2045-2322linking, 2045-2322electronic), 2018 Feb 14; 8(1): 2998-2998.
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Paper type: Abstract, Conference, Journal Article , Research Support, Non-U. S. Gov'T
Impact factor: 4.259, 5-year impact factor: 4.847
Url: https://www.scopus.com/inward/record.uri?eid=2-s2.0-85042070303&doi=10.1038%2fs41598-018-21283-3&partnerID=40&md5=fb4f45441c08f76bffa7fa8f1e649ebe
Keywords: Animals , Outbred Strains , Breast Neoplasms Diagnosis Pathology , Cell Line, Tumor , Drug Delivery Systems , Female , Humans , Immunoglobulin Fab Fragments Genetics , Mice , Molecular Probes Genetics Metabolism , Peptides Genetics Metabolism , Protein Binding , Radioimmunodetection Methods , Receptor, Erbb-2 Immunology , Trastuzumab Genetics
Affiliations:
*** IBB - CNR ***
Department of Surgical Sciences, Radiology, Uppsala University Hospital, Uppsala, Sweden.
Institute of Biostructures and Bioimaging, National Research Council, Naples, Italy.
Division of Molecular Imaging, Department of Medicinal Chemistry, Uppsala University, Uppsala, Sweden.
Department of Clinical Medicine and Surgery, University of Naples "Federico II", Naples, Italy.
Institute of Crystallography, National Research Council, Bari, Italy.
Department of Immunology, Genetics and Pathology, Uppsala University, Uppsala, Sweden. vladimir.tolmachev@igp.uu.se.
References:
Not available.
Sci Rep (ISSN: 2045-2322linking, 2045-2322electronic), 2018 Feb 14; 8(1): 2998-2998.
Export to BibTeX Export to EndNote
Paper type: Abstract, Conference, Journal Article , Research Support, Non-U. S. Gov'T
Impact factor: 4.259, 5-year impact factor: 4.847
Url: https://www.scopus.com/inward/record.uri?eid=2-s2.0-85042070303&doi=10.1038%2fs41598-018-21283-3&partnerID=40&md5=fb4f45441c08f76bffa7fa8f1e649ebe
Keywords: Animals , Outbred Strains , Breast Neoplasms Diagnosis Pathology , Cell Line, Tumor , Drug Delivery Systems , Female , Humans , Immunoglobulin Fab Fragments Genetics , Mice , Molecular Probes Genetics Metabolism , Peptides Genetics Metabolism , Protein Binding , Radioimmunodetection Methods , Receptor, Erbb-2 Immunology , Trastuzumab Genetics
Affiliations:
*** IBB - CNR ***
Department of Surgical Sciences, Radiology, Uppsala University Hospital, Uppsala, Sweden.
Institute of Biostructures and Bioimaging, National Research Council, Naples, Italy.
Division of Molecular Imaging, Department of Medicinal Chemistry, Uppsala University, Uppsala, Sweden.
Department of Clinical Medicine and Surgery, University of Naples "Federico II", Naples, Italy.
Institute of Crystallography, National Research Council, Bari, Italy.
Department of Immunology, Genetics and Pathology, Uppsala University, Uppsala, Sweden. vladimir.tolmachev@igp.uu.se.
References:
Not available.
Evaluation of HER2-specific peptide ligand for its employment as radiolabeled imaging probe
HER2 transmembrane receptor is an important target in immunotherapy treatment of breast and gastroesophageal cancer. Molecular imaging of HER2 expression may provide essential prognostic and predictive information concerning disseminated cancer and aid in selection of an optimal therapy. Radiolabeled low molecular weight peptide ligands are particularly attractive as probes for molecular imaging, since they reach and bind to the target and clear from non-target organs and blood stream faster than bulky antibodies. In this study, we evaluated a potential HER2-imaging probe, an A9 nonapeptide, derived from the trastuzumab-Fab portion. Its cellular uptake was investigated by mass spectrometry analysis of the cytoplasmic cellular extracts. Moreover, based on in-silico modeling, DTPA chelator was conjugated to N-terminus of A9. (111)In-labeled A9 demonstrated nanomolar affinity to HER2-expressing BT474 cells and favorable biodistribution profile in NMRI mice. This study suggests that the peptide A9 represents a good lead candidate for development of molecular probe, to be used for imaging purposes and for the delivery of cytotoxic agents.
HER2 transmembrane receptor is an important target in immunotherapy treatment of breast and gastroesophageal cancer. Molecular imaging of HER2 expression may provide essential prognostic and predictive information concerning disseminated cancer and aid in selection of an optimal therapy. Radiolabeled low molecular weight peptide ligands are particularly attractive as probes for molecular imaging, since they reach and bind to the target and clear from non-target organs and blood stream faster than bulky antibodies. In this study, we evaluated a potential HER2-imaging probe, an A9 nonapeptide, derived from the trastuzumab-Fab portion. Its cellular uptake was investigated by mass spectrometry analysis of the cytoplasmic cellular extracts. Moreover, based on in-silico modeling, DTPA chelator was conjugated to N-terminus of A9. (111)In-labeled A9 demonstrated nanomolar affinity to HER2-expressing BT474 cells and favorable biodistribution profile in NMRI mice. This study suggests that the peptide A9 represents a good lead candidate for development of molecular probe, to be used for imaging purposes and for the delivery of cytotoxic agents.
Evaluation of HER2-specific peptide ligand for its employment as radiolabeled imaging probe
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Evaluation of HER2-specific peptide ligand for its employment as radiolabeled imaging probe
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10 Records (10 excluding Abstracts).
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Total 5 year impact factor: 30.315 (30.315 excluding Abstracts).
Total impact factor: 29.091 (29.091 excluding Abstracts).
Total 5 year impact factor: 30.315 (30.315 excluding Abstracts).
340 views. Last view on Saturday 01 June 2024, 4:11:15
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