Peptide and use thereof
View Patent ↗A peptide is composed of an amino acid sequence represented by general formula (I), and accumulates in cancer-associated fibroblasts. (In general formula (I), X 11 is a peptide residue composed of an amino acid sequence of (a) or (b) below: (a) an amino acid sequence represented by any one of SEQ ID NOs: 1 to 4, (b) an amino acid sequence in which one or two amino acids have been deleted, substituted or added in an amino acid sequence represented by any one of SEQ ID NOs: 1 to 4; Y 11 is a peptide linker composed of an amino acid residue of at least 1 but not more than 10 amino acids, wherein each amino acid residue is independently a glycine residue, a proline residue, a serine residue, a cysteine residue or a lysine residue; X 12 is either a peptide residue composed of an amino acid sequence of (a) or (b) above, or a retro-inverso peptide residue thereof; and n11 represents an integer of at least 0 but not more than 9.) [ Formula 1 ] X 11 - ( Y 11 - X 12 ) n 11 ( I )
1 . A peptide composed of an amino acid sequence represented by general formula (I) shown below:
X
11
-
(
Y
11
-
X
12
)
n
11
(
I
)
wherein in general formula (I), X 11 is a peptide residue composed of an amino acid sequence of (a), (b), or (c) below:
(a) an amino acid sequence represented by any one of SEQ ID NOs: 1 to 4,
(b) an amino acid sequence in which the first lysine from the N-terminus of SEQ ID NO: 1 is substituted with glycine, alanine, arginine, histidine, serine, or threonine;
(c) an amino acid sequence in which one or two amino acids are deleted, substituted, or added in an amino acid sequence represented by any one of SEQ ID NOs: 2 to 4;
Y 11 is a peptide linker composed of an amino acid residue of at least 1 but not more than 10 amino acids, wherein each amino acid residue is independently a glycine residue, a proline residue, a serine residue, a cysteine residue, or a lysine residue;
X 12 is either a peptide residue composed of an amino acid sequence of (a) or (b) above, or a retro-inverso peptide residue thereof; and
n11 is an integer of at least 1 but not more than 4.
2 . The peptide according to claim 1 , wherein Y 11 is a peptide linker composed of a glycine residue of at least 1 but not more than 10 amino acids.
3 . The peptide according to claim 1 , wherein X 11 and X 12 are peptide residues composed of the same amino acid sequence.
4 . The peptide according to claim 1 , composed of an amino acid sequence represented by SEQ ID NO: 5.
5 . A peptide-drug-conjugate comprising a peptide of claim 1 and a biologically active substance.
6 . A pharmaceutical composition comprising a peptide-drug-conjugate of claim 5 .
7 . The pharmaceutical composition according to claim 6 , wherein the biologically active substance is an anticancer drug.
8 . A labeled peptide comprising a peptide of claim 1 and a labeling substance.
9 . The labeled peptide according to claim 8 , wherein the labeling substance is biotin, avidin, streptavidin, a stable isotope, a radioisotope, or a fluorescent substance.
10 . An imaging composition comprising a labeled peptide of claim 8 .
11 . The peptide according to claim 2 , wherein Y11 is a peptide linker composed of an amino acid residue of at least 1 but not more than 5 amino acids.
12 . A nucleic acid that encodes a peptide of claim 1 .
13 . A peptide-drug-conjugate expression vector comprising a nucleic acid of claim 12 and a nucleic acid that encodes a biologically active substance.
14 . A labeled peptide expression vector comprising a nucleic acid of claim 12 and a nucleic acid that encodes a labeling substance.