Patent ID: 7737251

Claim:
A gastrointestinal tissue growth promoter derivative comprising: a GLP-2 peptide having gastrointestinal tissue growth promoting activity; and a single maleimide or a maleimido-containing group, wherein the maleimide or maleimido-containing group is coupled, optionally via a linker, to the GLP-2 peptide at a His or Lys residue, wherein the GLP-2 peptide is of the sequence: R 1 -(Y 1 ) m -X 1 -X 2 -X 3 -X 4 -X 5 -Phe 6 -Ser 7 -Asp 8 -(P 1 )-X 14 -Asp 15 -X 16 -X 17 -Ala 18 -X 19 -X 20 -X 21 -Phe 22 -(P 2 )-Trp 25 -Leu 26 -X 27 -X 28 -Thr 29 -Lys 30 -P 3 -(Y 2 ) n -R 2 (SEQ ID NOs: 2 and 29-252) wherein X 1 is His or Tyr; X 2 is Gly, D-Ala, Pro, Ile, Nor-Val, α-aminobutyric acid, or an Ala-replacement amino acid conferring on said analog resistance to DPP-IV enzyme; X 3 is Asp, Glu, Pro, HPro; or X 2 -X 3 are X 2ψ (CH(OH)CH 2 )X 3 ; X 2ψ (CH 2 NH 2 )X 3 or X 2ψ (CHCH)X 3 wherein X 2 and X 3 are as defined above; X 4 is Gly or Ala; X 5 is Ser or Ala; P 1 is Glu-X 10 -Asn-Thr-Ile (SEQ ID NO: 253), Gly-X 10 -Asn-Thr-Val (SEQ ID NO: 254) or Tyr-Ser-Lys-Tyr (SEQ ID NO: 255); X 10 is Met, Leu, Ile or an oxidatively stable Met-replacement amino acid; X 14 is Leu or Lys; X 16 is Asn, Lys or Ala; X 17 is Leu or Lys; X 19 is Ala or Thr; X 20 is Arg, Lys, His or Ala; X 21 is Asp or Lys; X 27 is Ile or Leu; X 28 is Gin or His; P 2 is IIe-Asn, lIe-Ala or Val-Gin; P 3 is a covalent bond, or is lIe, Ile-Thr, Ile-Thr-Asp or Ile-Thr-Asn; R 1 is NH 2 or a N-terminal blocking group; R 2 is COOH, CONH2 or a C-terminal blocking group; Y 1 is one or two of Arg, Lys, and His; Y 2 is one or two of Arg, Lys, and His; and m and n are independently 0 or 1.