FIELD: biotechnology.
SUBSTANCE: group of inventions relates to double agonists GLP-1/GIP. Disclosed is a polypeptide with GLP-1R/GIPR agonist activity, having a sequence presented in formula (II): YAibEGT FTSDY SIAibLD KIAQK AFVKW LIAGG PSSGA PPPS0, which is presented in SEQ ID NO: 1. In a specific embodiment, the polypeptide has an amino acid sequence selected from SEQ ID NO: 3–11. Amino groups on side chains of lysine in positions 17 and 20 or in positions 20 and 24 are attached to 
, and in the polypeptide sequence of formula (II) are additionally replaced from 0 to 2 amino acids. Also disclosed is a pharmaceutical composition based on said polypeptide and use thereof in preparing drugs for treating non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH).
EFFECT: disclosed polypeptide exhibits very strong agonist activity with respect to GLP-1R/GIPR, exhibits excellent pharmacokinetic properties, plasma stability and extremely strong binding to plasma proteins.
19 cl, 12 tbl, 7 ex
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| 1-[1-(4-BENZYLOXY-3,5-DIFLUORO-BENZOYL)-4-FLUORO-PYRROLIDINE-2-CARBONYL]-PYRROLIDINE-2-CARBONITRILE | 2021 |
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RU2841064C1 |
