Introduction

The present invention relates to:

1. Peptides binding to human thymidylate synthase for the treatment of cancer. The peptides of 4-8 amino acids bind to each subunit of the protein dimer interface, stabilizing the inactive form.
2. Pharmaceutical composition of these compounds as active agents, and user for the treatment of cancer and to reverse or/and be active in cancer drug resistance.

Technical features

The present invention relates to peptides and their conjugates with targeting and /or transposrters agents binding to the thymidylate synthase protein for the treatment of cancer, peptides of 4 to 8 amino acids, can bind at a site located at the Thymidylate synthase dimer interface, anticancer drugs able to reverse cancer resistance to known anticancer drugs.

Possible Applications

• The peptides can be used as such or as biocongiugates with a targeting agent, with a transport agent;
• Treatment of ovarian cancer;
• Recover sensitivity of ovarian cancer cells resistant to known anticancer drugs;
• Use in pharmaceutical composition with different formulations

Advantages

• Peptides has novel mechanism of action;
• Stabilize the dimeric form of the protein;
• Inhibit the protein catalytic activity;
• Does not increase the human thymidylate synthase level in cancer cells after treatment;
• Inhibit the cancer cell growth;
• formulation and conjugates work as anticancer agents.