PEPTIDE ANTAGONISTS OF CALCITONIN CGRP FAMILY OF PEPTIDE HORMONES AND THEIR USE Russian patent published in 2021 - IPC C07K14/585 A61K38/22 A61P25/06 

FIELD: biotechnology.

SUBSTANCE: invention relates to peptide antagonists of calcitonin gene-associated peptide (CGRP), and can be used in medicine for treating a condition associated with high CGRP, including migraine. Disclosed is a peptide having the structure X¹-Y¹-Z¹, where X¹ is a modified N-terminal CGRP fragment containing from 5 to 7 amino acid residues, where 2 amino acids of said N-terminal fragment are cysteine residues (Cys), wherein the C-terminal amino acid residue of the N-terminal fragment is Cys, residue immediately before C-terminal Cys residue of said N-terminal fragment is a substitution of a residue of threonine (Thr) by nethreonine, wherein two cysteine residues are separated by 4, 5 or 6 amino acids and wherein said 2 Cys residues can form a disulphide bond; Y¹ is selected from Val-Leu-Gly-Arg-Leu-Ser-Gln-Glu-Leu-His-Arg-Leu-Gln-Thr-Tyr-Pro-Thr-Asn, Val-Leu-Gly-Arg-Leu-Ser-Gln-Glu-Leu-His-Arg-Leu-Gln-Thr-Tyr-Pro-Val-Asp; and Z¹ is selected from Thr-Gly-Ser-Gly-Thr-Pro-NH₂, Pro-Ser-Ser-Pro-His-Ser-Tyr-NH₂ or Val-Gly-Ser-Lys-Ala-Phe-NH₂.

EFFECT: invention provides preparing an effective CGRP antagonist.

13 cl, 7 tbl, 1 ex