A HER2 Specific Nanobody–Drug Conjugate: Site-Selective Bioconjugation and In Vitro Evaluation in Breast Cancer Models

Anders H. Hansen, Kasper I. H. Andersen, Li Xin, Oliver Krigslund, Niels Behrendt, Lars H. Engelholm, Claus H. Bang-Bertelsen, Sanne Schoffelen, Katrine Qvortrup*

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

4 Downloads (Pure)

Abstract

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.
Original languageEnglish
Article number391
JournalMolecules
Volume30
Issue number2
Number of pages12
ISSN1420-3049
DOIs
Publication statusPublished - 2025

Keywords

  • Breast cancer
  • Targeted treatment
  • Nanobody
  • Site-selective conjugation

Fingerprint

Dive into the research topics of 'A HER2 Specific Nanobody–Drug Conjugate: Site-Selective Bioconjugation and In Vitro Evaluation in Breast Cancer Models'. Together they form a unique fingerprint.

Cite this