Patent Granted to RBI Scientists
The National Department for Intellectual Property in the Republic of Croatia granted a patent entitled "Synthetic peptides containing unnatural adamantane related amino acids for use as antitumor drugs" (no. P20050242) on September 4th, 2010. The patent was granted to several investigators including RBI scientists Dr. Štefica Horvat, Dr. Kata Majerski, Dr. Andreja Jakas and Dr. Jelena Veljković.
The Patent relates to the preparation and bioevaluation of adamantnane substituted methionine-enkephalin an endogenous opioid growth factor (OGF) which was identified as a regulator of cancer growth in different types of tumour cells, particularly gastrointestinal cancer and neuroblastoma.
The invention refers to the synthesis of dipeptides, tripeptides, tetrapeptides, pentapeptides and hexapeptides containing different unnatural amino acids of the adamantane type, and the uses of such peptides as medicaments, especially for the treatment of various malignant tumours.
Incorporation of the unnatural amino acids into peptides allows for a more precise change in the steric or electronic properties of the peptide and expands the scope of structural perturbations that can be made. Changes in hydrophobicity, packing effects and conformation caused by the adamantane moiety all play important roles in peptide stability.