A HER2 Specific Nanobody–Drug Conjugate: Site-Selective Bioconjugation and In Vitro Evaluation in Breast Cancer Models
A human epidermal growth factor receptor 2 (HER2)-specific nanobody called 2Rs15d, containing a His3LysHis6 segment at the C-terminus, was recombinantly produced. Subsequent site-selective acylation on the C-terminally activated lysine residue allowed installation of the cytotoxin monomethyl aurista...
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MDPI AG
2025-01-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/30/2/391 |
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| author | Anders H. Hansen Kasper I. H. Andersen Li Xin Oliver Krigslund Niels Behrendt Lars H. Engelholm Claus H. Bang-Bertelsen Sanne Schoffelen Katrine Qvortrup |
| author_facet | Anders H. Hansen Kasper I. H. Andersen Li Xin Oliver Krigslund Niels Behrendt Lars H. Engelholm Claus H. Bang-Bertelsen Sanne Schoffelen Katrine Qvortrup |
| author_sort | Anders H. Hansen |
| collection | DOAJ |
| description | A human epidermal growth factor receptor 2 (HER2)-specific nanobody called 2Rs15d, containing a His3LysHis6 segment at the C-terminus, was recombinantly produced. Subsequent site-selective acylation on the C-terminally activated lysine residue allowed installation of the cytotoxin monomethyl auristatin E-functionalized cathepsin B-sensitive payload to provide a highly homogenous nanobody–drug conjugate (NBC), which demonstrated high potency and selectivity for HER2-positive breast cancer models. |
| format | Article |
| id | doaj-art-6862de08b4d0445796da906b1f191462 |
| institution | Kabale University |
| issn | 1420-3049 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj-art-6862de08b4d0445796da906b1f1914622025-01-24T13:43:53ZengMDPI AGMolecules1420-30492025-01-0130239110.3390/molecules30020391A HER2 Specific Nanobody–Drug Conjugate: Site-Selective Bioconjugation and In Vitro Evaluation in Breast Cancer ModelsAnders H. Hansen0Kasper I. H. Andersen1Li Xin2Oliver Krigslund3Niels Behrendt4Lars H. Engelholm5Claus H. Bang-Bertelsen6Sanne Schoffelen7Katrine Qvortrup8Department of Chemistry, Technical University of Denmark, 206 Kemitorvet, 2800 Kgs Lyngby, DenmarkNational Food Institute, Technical University of Denmark, 2800 Kgs Lyngby, DenmarkDepartment of Health Technology, Technical University of Denmark, 2800 Kgs Lyngby, DenmarkFinsen Laboratory, Rigshospitalet/Biotech Research and Innovation Center (BRIC), University of Copenhagen, 2200 Copenhagen, DenmarkFinsen Laboratory, Rigshospitalet/Biotech Research and Innovation Center (BRIC), University of Copenhagen, 2200 Copenhagen, DenmarkFinsen Laboratory, Rigshospitalet/Biotech Research and Innovation Center (BRIC), University of Copenhagen, 2200 Copenhagen, DenmarkNational Food Institute, Technical University of Denmark, 2800 Kgs Lyngby, DenmarkThe Novo Nordisk Foundation Center for Biosustainability, Technical University of Denmark, 2800 Kgs Lyngby, DenmarkDepartment of Chemistry, Technical University of Denmark, 206 Kemitorvet, 2800 Kgs Lyngby, DenmarkA human epidermal growth factor receptor 2 (HER2)-specific nanobody called 2Rs15d, containing a His3LysHis6 segment at the C-terminus, was recombinantly produced. Subsequent site-selective acylation on the C-terminally activated lysine residue allowed installation of the cytotoxin monomethyl auristatin E-functionalized cathepsin B-sensitive payload to provide a highly homogenous nanobody–drug conjugate (NBC), which demonstrated high potency and selectivity for HER2-positive breast cancer models.https://www.mdpi.com/1420-3049/30/2/391breast cancertargeted treatmentnanobodysite-selective conjugation |
| spellingShingle | Anders H. Hansen Kasper I. H. Andersen Li Xin Oliver Krigslund Niels Behrendt Lars H. Engelholm Claus H. Bang-Bertelsen Sanne Schoffelen Katrine Qvortrup A HER2 Specific Nanobody–Drug Conjugate: Site-Selective Bioconjugation and In Vitro Evaluation in Breast Cancer Models Molecules breast cancer targeted treatment nanobody site-selective conjugation |
| title | A HER2 Specific Nanobody–Drug Conjugate: Site-Selective Bioconjugation and In Vitro Evaluation in Breast Cancer Models |
| title_full | A HER2 Specific Nanobody–Drug Conjugate: Site-Selective Bioconjugation and In Vitro Evaluation in Breast Cancer Models |
| title_fullStr | A HER2 Specific Nanobody–Drug Conjugate: Site-Selective Bioconjugation and In Vitro Evaluation in Breast Cancer Models |
| title_full_unstemmed | A HER2 Specific Nanobody–Drug Conjugate: Site-Selective Bioconjugation and In Vitro Evaluation in Breast Cancer Models |
| title_short | A HER2 Specific Nanobody–Drug Conjugate: Site-Selective Bioconjugation and In Vitro Evaluation in Breast Cancer Models |
| title_sort | her2 specific nanobody drug conjugate site selective bioconjugation and in vitro evaluation in breast cancer models |
| topic | breast cancer targeted treatment nanobody site-selective conjugation |
| url | https://www.mdpi.com/1420-3049/30/2/391 |
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