dc.contributor.author | Da Pieve, C | |
dc.contributor.author | Allott, L | |
dc.contributor.author | Martins, CD | |
dc.contributor.author | Vardon, A | |
dc.contributor.author | Ciobota, DM | |
dc.contributor.author | Kramer-Marek, G | |
dc.contributor.author | Smith, G | |
dc.date.accessioned | 2016-08-17T12:52:29Z | |
dc.date.issued | 2016-08-17 | |
dc.identifier.citation | Bioconjugate chemistry, 2016, 27 (8), pp. 1839 - 1849 | |
dc.identifier.issn | 1043-1802 | |
dc.identifier.uri | https://repository.icr.ac.uk/handle/internal/61 | |
dc.identifier.eissn | 1520-4812 | |
dc.identifier.doi | 10.1021/acs.bioconjchem.6b00259 | |
dc.description.abstract | The human epidermal growth factor receptor 3 (HER3) is overexpressed in several cancers, being linked to a more resistant phenotype and hence leading to poor patient prognosis. Imaging HER3 is challenging owing to the modest receptor number (<50000 receptors/cell) in overexpressing cancer cells. Therefore, to image HER3 in vivo, high target affinity PET probes need to be developed. This work describes two different [(18)F]AlF radiolabeling strategies of the ZHER3:8698 affibody molecule specifically targeting HER3. The one-pot radiolabeling of ZHER3:8698 performed at 100 °C and using 1,4,7-triazanonane-1,4,7-triacetate (NOTA) as chelator resulted in radiolabeled products with variable purity attributed to radioconjugate thermolysis. An alternative approach based on the inverse electron demand Diels-Alder (IEDDA) reaction between a novel tetrazine functionalized 1,4,7-triazacyclononane-1,4-diacetate (NODA) chelator and the trans-cyclooctene (TCO) functionalized affibody molecule was also investigated. This method enabled the radiolabeling of the protein at room temperature. The [(18)F]AlF-NOTA-ZHER3:8698 and [(18)F]AlF-NODA-ZHER3:8698 conjugates showed a specific uptake at 1 h after injection in high HER3-expressing MCF-7 tumors of 4.36 ± 0.92% ID/g and 4.96 ± 0.65% ID/g, respectively. The current results are encouraging for further investigation of [(18)F]AlF-NOTA-ZHER3:8698 as a HER3 imaging agent. | |
dc.format | Print-Electronic | |
dc.format.extent | 1839 - 1849 | |
dc.language | eng | |
dc.language.iso | eng | |
dc.publisher | AMER CHEMICAL SOC | |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0 | |
dc.subject | Animals | |
dc.subject | Humans | |
dc.subject | Mice | |
dc.subject | Cell Transformation, Neoplastic | |
dc.subject | Aluminum | |
dc.subject | Fluorine Radioisotopes | |
dc.subject | Heterocyclic Compounds | |
dc.subject | Heterocyclic Compounds, 1-Ring | |
dc.subject | Receptor, erbB-3 | |
dc.subject | Antibodies, Monoclonal | |
dc.subject | Positron-Emission Tomography | |
dc.subject | Isotope Labeling | |
dc.subject | Protein Conformation | |
dc.subject | Models, Molecular | |
dc.subject | Female | |
dc.subject | Protein Stability | |
dc.subject | MCF-7 Cells | |
dc.title | Efficient [(18)F]AlF Radiolabeling of ZHER3:8698 Affibody Molecule for Imaging of HER3 Positive Tumors. | |
dc.type | Journal Article | |
dcterms.dateAccepted | 2016-06-29 | |
rioxxterms.versionofrecord | 10.1021/acs.bioconjchem.6b00259 | |
rioxxterms.licenseref.uri | https://creativecommons.org/licenses/by/4.0 | |
rioxxterms.licenseref.startdate | 2016-08 | |
rioxxterms.type | Journal Article/Review | |
dc.relation.isPartOf | Bioconjugate chemistry | |
pubs.issue | 8 | |
pubs.notes | No embargo | |
pubs.organisational-group | /ICR | |
pubs.organisational-group | /ICR/Primary Group | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Preclinical Molecular Imaging | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Closed research teams | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Closed research teams/PET Radiochemistry | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Radiotherapy and Imaging | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Radiotherapy and Imaging/Preclinical Molecular Imaging | |
pubs.organisational-group | /ICR | |
pubs.organisational-group | /ICR/Primary Group | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Preclinical Molecular Imaging | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Closed research teams | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Closed research teams/PET Radiochemistry | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Radiotherapy and Imaging | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Radiotherapy and Imaging/Preclinical Molecular Imaging | |
pubs.publication-status | Published | |
pubs.volume | 27 | |
pubs.embargo.terms | No embargo | |
icr.researchteam | PET Radiochemistry | |
icr.researchteam | Preclinical Molecular Imaging | |
dc.contributor.icrauthor | Da Pieve, Chiara | |
dc.contributor.icrauthor | Kramer-Marek, Gabriela | |
dc.contributor.icrauthor | Smith, Graham | |