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US 10,479,819 B2Granted
Oxyntomodulin analogue
AssigneeJiang, Xianxing
InventorsXianxing Jiang, Yuanwen Chen
Life of this patent
Estimating the term…
Abstract
Provided is an oxyntomodulin analogue. The analogue comprises GCGR and GLP-1R dual agonist activity, improved enzymolysis stability and biological activity, and no adverse reactions. The analogue can be used to prepare medication for treating hyperphagia, obesity and diabetes.
Claims10
An oxyntomodulin analogue, comprising a parent peptide having the following amino acid sequence (SEQ ID NO:
- 29):
- His-Xaa2-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Xaa10-Ser-
- Lys-Xaa13-Leu-Asp-Xaa16-Xaa17-Xaa18-Ala-Xaa20-
- Xaa21-Phe-Xaa23-Xaa24-Trp-Leu-Xaa27-Xaa28-Xaa29-
- Xaa30-Xaa31-Xaa32-Xaa33-Xaa34-Xaa35-Xaa36-Xaa37-
- Xaa38-Xaa39-Xaa40-COR1
- wherein, R1=—OH or —NH2;
- Xaa2=Aib, Ser or D-Ser;
- Xaa10=Lys or Tyr;
- Xaa13=Lys or Tyr;
- Xaa16=Ser, Aib, Lys;
- Xaa17=Lys or Arg;
- Xaa18=Arg or Ala;
- Xaa20=His, Gln or Lys;
- Xaa21=Asp or Glu;
- Xaa23=IIe, Leu or Val;
- Xaa24=Glu or Gln;
- Xaa27=Met or Leu;
- Xaa28=Ser, Asn, Asp, or Arg;
- Xaa29=Ala, Gly, or Thr;
- Xaa30=Gly;
- Xaa31=Gly;
- Xaa32=Pro;
- Xaa33=Ser;
- Xaa34=Ser;
- Xaa35=Gly;
- Xaa36=Ala;
- Xaa37=Pro;
- Xaa38=Pro;
- Xaa39=Pro;
- and
- Xaa40=Ser;
- in the amino acid sequence of the parent peptide, at least one of Xaa10, Xaa16, Xaa17 or Xaa20 is Lys, the side chain of said at least one Lys or the Lys at position 12 is attached to a lipophilic substituent in such a way that a carboxyl group of the lipophilic substituent forms an amide bond with an amino group of a bridging group, the bridging group is attached to the parent peptide by means of a carboxy group of the amino acid residue of the bridging group which forms an amide bond with the amino group of the side chain of said at least one Lys or the Lys of the parent peptide;
- the bridging group is Glu-(PEG)m or Asp-(PEG)m or (PEG)m, wherein m is an integer of 2-10;
- and the lipophilic substituent is an acyl group selected from CH3(CH2)nCO— or HOOC(CH2)nCO—, wherein n is an integer of 10-24.
32 more elements
Dependencies are inferred from the claim text.