Acylated oxyntomodulin peptide analog
AssigneeDong-A St Co., Ltd.
InventorsJae-Sung Yang, Kyung-Seok Lee, Yu-Na Chae, Gye-Rim Baek, Tae-Hyoung Kim, Ill-Hun Jung, Chae-Lim Ryu, Weon-Bin Im
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Abstract
The present invention relates to a novel peptide analog of acylated oxyntomodulin and a pharmaceutical composition comprising the same for preventing and treating obesity or overweightness, or diabetes accompanied by obesity and overweightness. The peptides are superior to those of natural oxyntomodulin in dual agonism on GLP-1 and glucagon receptors and longer in vivo half-life. A pharmaceutical composition comprising said peptides is effective in the treatment of metabolic diseases such as obesity and diabetes mellitus.
Claims9
An oxyntomodulin peptide analog of the following formula I:
- (SEQ ID NO.49)
- His-X1-Gln-Gly-Thr-Phe-Thr-Ser-X2-X3-X4-X5-X6-X7-
- X8-X9-Arg-Arg-Ala-X10-Asp-Phe-Val-Gln-Trp-Leu-X11-
- X12-X13-X14-X15-X16,
- wherein:
- X1 is Aib (aminoisobutyric acid);
- X2 is Asp;
- X3 is Tyr or Z;
- X4 is Ser;
- X5 is Lys;
- X6 is Tyr;
- X7 is Leu;
- X8 is Asp;
- X9 is Ser, Aib (aminoisobutyric acid) or Z;
- X10 is Gln or Z;
- X11 is Met or Leu;
- X12 is Asn or Arg;
- X13 is Thr or Ala;
- X14 is Lys;
- X15 is absent;
- X16 is absent;
- C-terminal amino acid may optionally be amidated;
- wherein
- one of X3, X9, and X10 is Z;
- Z is modified Lys to which Z1-Z2 of the following formulas is attached;
- Z1 is Formula (1);
- and
- Z2 is Formula (3);
- wherein * of Formula (1) is directly bound to a side chain of Lys, and
- wherein ** of Formula (1) and ** of formula (3) are bond between Z1 and Z2.
Dependencies are inferred from the claim text.