Ligand capable of multivalently binding to glutamine transporter, and composition comprising same

Patent metadata

Field	Value
Publication number	US-11707530-B2
Application number	US-201716326657-A
Country	US
Kind code	B2
Filing date	Aug 17, 2017
Priority date	Aug 22, 2016
Publication date	Jul 25, 2023
Grant date	Jul 25, 2023

Abstract

The present invention pertains to a ligand that contains a plurality of groups represented by formula (1) and is capable of multivalently binding to a glutamine transporter expressed in excess in a cancer cell compared to a normal cell.

First claim

The invention claimed is:

1. A ligand capable of multivalently binding to a glutamine transporter that is expressed in excess in a cancer cell as compared with a normal cell, wherein the ligand comprising a polymer, wherein the polymer is represented by the following monomeric unit:

wherein n represents an integer of 10 to 500.

2. The ligand according to claim 1 , wherein the number average molecular weight of the ligand is 6000 Da to 70,000 Da.

3. The ligand according to claim 1 , wherein the terminal primary amino groups of some of a plurality of groups represented by formula (X1) are capped with a protective group that is eliminated in a low pH environment.

4. The ligand according to claim 3 , wherein the protective group that is eliminated in a low pH environment is selected from the group consisting of a phthaloyl group, maleoyl group, 2-carboxybenzoyl group and (2Z)-3-carboxy-2-propenoyl group.

5. The ligand according to claim 1 , further comprising, wherein the ligand contains at least one detectable label or anticancer drug.

6. The ligand according to claim 5 , wherein the at least one detectable label is selected from the group consisting of a fluorescent label; a luminescent label; a contrast agent; a detectable metal atom; a compound containing one or more detectable metal atoms; a radioisotope; a compound containing one or more radioisotopes; a detectable nanoparticle; and a detectable liposome.

7. The ligand according to claim 5 , wherein the ligand is a compound represented by the following formula (4) or a pharmaceutically acceptable salt thereof:

wherein n represents an integer of 10 to 500.

8. A composition comprising the ligand according to claim 1 .

Assignees

• Tokyo Inst Tech
• Univ Osaka

Inventors

• Nishiyama Nobuhiro
• Takemoto Hiroyasu
• Nomoto Takahiro
• Tomoda Keishiro
• Matsui Makoto
• Yamada Naoki
• Honda Yuto
• Ishii Hideshi
• Mori Masaki
• Konno Masamitsu

Classifications

• A61K47/6455 Primary

  Polycationic oligopeptides, polypeptides or polyamino acids, e.g. for complexing nucleic acids · CPC title

• A61K49/146

  the peptide being a polyamino acid, e.g. poly-lysine · CPC title

• A61P35/00 Primary

  Antineoplastic agents · CPC title

• A61K47/645

  Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT · CPC title

• A61K47/542

  Carboxylic acids, e.g. a fatty acid or an amino acid · CPC title