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Tetrapetide molecule antagonist of leptin

Amino acidsBreast cancercancerfibroblastsLepR receptorLeptinTetrapetide LDFI


This invention concerns a synthetic tetrapetide molecule antagonist of leptin in which the sequence of the four amino acids is characterized by the fact that the central amino acids are aspartic acid and phenylalanine. This invention concerns also the pharmaceutical use of this molecule as anti-cancer drug in cells where leptin promotes tumor growth and progression.

Technical features

The proposed tetrapeptide is a simple and small molecule which inhibits the leptin receptor (LepR) acting as antagonist of leptin both in vitro and in vivo. Since this tetrapeptide molecule does not act as receptor agonist in the absence of leptin, it overcomes the therapeutic limit of other known peptide antagonists. Compared to other anti-tumor small molecules, peptide molecules have higher target affinity and specificity and reduced immunogenic profile. On the basis of in vitro, in vivo and ex-vivo data, the tetrapeptide LDFI, will be useful to block development and progression of human breast cancer as well as human testicular seminoma, by inhibiting leptin action at endocrine and paracrine levels. The proposed tetrapeptide, after further experiments and biological and medical assessments, will provide a drug useful for the treatment of breast cancer especially in obese women and other leptin-related cancers.

Possible Applications

  • Development of antitumor drugs;
  • Pharmacological research.


  • The tetrapeptide does not act as a receptor agonist;
  • Easy and low-cost synthesis;
  • Reduced immunogenic profile;
  • High affinity;
  • High specificity.