Introduction

The invention refers to in vivo stable branched peptides, conjugated to functional units for specific targeting of cancer cells, either for diagnosis or therapy of tumours.

Technical features

The use of peptides in vivo has largely been limited due to their short half-life. Synthesis of peptides in branched multimeric form results in molecules keeping their biological activity and resisting proteolysis in biological fluids, thus having a markedly higher half-life with respect to correspondent monomeric peptides. Moreover, by conjugating functional units to these stable cancer-selective peptides, cancer cells can be specifically targeted for either diagnosis or therapy. The selectivity of these peptides is due to the affinity towards sulphated glycosaminoglycans. The inventors designed and synthesized different peptide-based branched molecules, where four copies of peptides reproducing the same sequence (NT4) were linked together by a core of three lysine residues and coupled to different functional units allowing to either trace cancer cells in vivo or ex vivo or to deliver cytotoxic moieties to tumour cells.

Possible Applications

• Treatment of neoplastic diseases and tumour localization by tracers;
• Selective binding to tumour cells and tissues, by means of affinity towards sulphated glycosaminoglycans;
• NT4 peptides can be used as tracers and as therapeutics;
• Selective cancer theranostics in the field of new cancer biotherapies.

Advantages

• Early diagnosis tools and tracers for micrometastasis;
• Stable multimeric specific peptides;
• Cancer cells can be specifically targeted for either diagnosis or therapy;
• Easily achieved by standard peptide chemistry.