FGF2-Derived PeptibodyF2-MMAE Conjugate for Targeted Delivery of Cytotoxic Drugs into Cancer Cells Overexpressing FGFR1

Jendryczko, K., Chudzian, J., Skinder, N., Opaliński, Ł., Rzeszótko, J., Wiedlocha, A., Otlewski, J. & Szlachcic, A., 15-Oct-2020, In : Cancers. 12, 10, 17 p., 12102992.

Research output: Contribution to journalArticleAcademicpeer-review

  • Karolina Jendryczko
  • Julia Chudzian
  • Natalia Skinder
  • Łukasz Opaliński
  • Jakub Rzeszótko
  • Antoni Wiedlocha
  • Jacek Otlewski
  • Anna Szlachcic

Fibroblast growth factor receptors (FGFRs) are emerging targets for directed cancer therapy. Presented here is a new FGFR1-targeting conjugate, the peptibodyF2, which employs peptibody, a fusion of peptide and the Fc fragment of human IgG as a selective targeting agent and drug carrier. Short peptide based on FGF2 sequence was used to construct a FGFR1-targeting peptibody. We have shown that this peptide ensures specific delivery of peptibodyF2 into FGFR1-expressing cells. In order to use peptibodyF2 as a delivery vehicle for cytotoxic drugs, we have conjugated it with MMAE, a drug widely used in antibody-drug conjugates for targeted therapy. Resulting conjugate shows high and specific cytotoxicity towards FGFR1-positive cells, i.e., squamous cell lung carcinoma NCI-H520, while remaining non-toxic for FGFR1-negative cells. Such peptibody-drug conjugate can serve as a basis for development of therapy for tumors with overexpressed or malfunctioning FGFRs.

Original languageEnglish
Article number12102992
Number of pages17
Issue number10
Publication statusPublished - 15-Oct-2020

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