Peptide ligand targeting carbonic anhydrase IX, peptide construct comprising same, and uses thereof
Inventors
Lee, Song Gil • Ha, Hye Sook • PARK, Jin Hwi • KIM, Se Won • Oh, Yoo Joung • Park, Seo Hyun • PARK, Shin Young • Cha, Jun Hoe
Assignees
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Publication Number
US-12486304-B2
Publication Date
2025-12-02
Expiration Date
Abstract
The present invention relates to a peptide ligand that specifically binds to carbonic anhydrase IX (CAIX), a peptide construct comprising the ligand, and a use thereof. The CAIX-binding peptide ligand of the present invention includes D-amino acids, so it is stable in the body and has high binding specificity to CAIX. And the linear or cyclic CAIX-binding peptide construct comprising the ligand can bind to CAIX with high affinity in the body. Therefore, it is useful for diagnosis, prevention, suppression or treatment of diseases mediated by CAIX.
Core Innovation
The invention relates to a CAIX-specific peptide construct comprising a peptide ligand consisting of amino acid sequence selected from SEQ ID NOs 1 to 44, in which at least one constituent amino acid is composed of D-amino acids and a lysine (Lys) residue among the constituent amino acids may be substituted with a chemical functional group at the side chain ε-amino group. The construct includes a sulfonamide functional group-containing amino acid residue linked to the peptide ligand directly or through a spacer.
The peptide construct has a cyclic structure represented by Formula 1, where P is the peptide ligand and glycine or sulfonamide-containing residues occupy defined positions. The structure also defines F4 as a group of the general formula —(S1)o—(F5)p—(S2)q—(F6)r—NH2, wherein S1 and S2 are each independently a spacer and F5 and F6 are each independently a functional group-containing amino acid residue other than sulfonamide.
The functional group other than sulfonamide is selected from chelator, cycloalkane having 5 to 15 carbon atoms, biotin, glucoheptonic acid, 4-(p-iodophenyl) butyric acid (IB), fluorescent dye, or cytotoxic agent. The described constructs thereby provide CAIX-specific cyclic peptide ligands featuring D-amino acid content and sulfonamide functional group(s) incorporated into a defined cyclic framework.
Claims Coverage
The independent claim covers one CAIX-specific cyclic peptide construct. The claim identifies three inventive features centered on a CAIX-targeting peptide ligand, a defined cyclic structure, and selected non-sulfonamide functional groups.
CAIX-specific cyclic peptide construct with D-amino acids and sulfonamide residues
A CAIX-specific peptide construct comprising a peptide ligand consisting of amino acid sequence selected from SEQ ID NOs 1 to 44, wherein at least one constituent amino acid is composed of D-amino acids, a lysine (Lys) residue among the constituent amino acids may be substituted with a chemical functional group at the side chain ε-amino group, and a sulfonamide functional group-containing amino acid residue is linked to the peptide ligand directly or through a spacer.
Defined cyclic structure with spacer-and-functional-group general formula
The cyclic structure is defined with P as the peptide ligand, F1 as glycine (Gly) or a sulfonamide functional group-containing amino acid residue, F2 as a sulfonamide functional group-containing amino acid residue, F3 as glycine (Gly) or a functional group-containing amino acid residue other than sulfonamide, and n and m each independently 0 or 1; and F4 as —(S1)o—(F5)p—(S2)q—(F6)r—NH2, wherein S1 and S2 are spacers and F5 and F6 are functional group-containing amino acid residues other than sulfonamide, with o, p, q and r each independently an integer of 0 to 6.
Non-sulfonamide functional groups selected from chelator, cycloalkane, and diagnostic/therapeutic payloads
The functional group other than sulfonamide is selected from chelator, cycloalkane having 5 to 15 carbon atoms, biotin, glucoheptonic acid, 4-(p-iodophenyl) butyric acid (IB), fluorescent dye, or cytotoxic agent.
The claim coverage centers on CAIX-specific cyclic peptide constructs built from peptide ligands selected from SEQ ID NOs 1 to 44, incorporating D-amino acids and sulfonamide functional group-containing amino acid residues, and arranged in a cyclic structure defined by Formula 1 with spacers and selected non-sulfonamide functional groups.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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