Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limited

Yuji Kawamata

Shuji Hinuma

Ryo Fujii

Masaki Hosoya

Shoji Fukusumi

Chieko Kitada

Yugo Habata

Hideyuki Tanaka

Naoyuki Kanzaki

Makoto Kobayashi

Kazuhiro Ogi

Fumio Itoh

Masataka Harada

Shoichi Ohkubo

Yuji Ishichi

Taisuke Tawaraishi

Yasuaki Ito

Hideki Kizawa

Syuji Hinuma

Mariko Hirohashi

Masanori Miwa

It is intended to provide a TGR5 receptor agonist containing a fused ring compound represented by the following general formula, its salt or a prodrug thereof: (1) wherein ring A represents an optionally substituted aromatic ring; and the ring B' represents a 5- to 8-membered ring having one or more substituents; which is useful in treating various diseases. 

Receptor agonists

The present invention intends to provide a screening of agonist/antagonist and the like. Specifically, the invention provides a method of screening a compound or its salt that alters the binding property between a novel G protein-coupled receptor protein or its salt, and a substance relating to cholesterol metabolism, which comprises using the receptor protein or its salt, which contains the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, SEQ ID NO: 5, SEQ ID NO: 7, SEQ ID NO: 14 or SEQ ID NO: 16, and the substance relating to cholesterol metabolism.

Screening method

By using (1) a G protein-coupled receptor protein having the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1 or its salt and (2) a fatty acid or an eicosanoid, a compound or its salt that can change the binding properties of the receptor protein or its salt to the fatty acid or the eicosanoid can be screened efficiently.

The present invention relates to the ligand polypeptide for the human pituitary- and mouse pancreas-derived G protein-coupled receptor proteins. The ligand polypeptide or the DNA which codes for the ligand polypeptide can be used for (1) development of medicines such as pituitary function modulators, central nervious system function modulators, and pancreatic function modulators, and (2) development of receptor binding assay systems using the expression of recombinant receptor proteins and screening of pharmaceutical candidate compounds. In particular, by the receptor binding assay systems utilizing the expression of recombinant G protein-coupled receptor proteins in accordance with the invention, agonists and antagonists of G protein-coupled receptors which are specific to human and other warm-blooded animals can be screened and the agonists or antagonists obtained can be used as therapeutic and prophylactic agents for various diseases.

Polypeptides, their production and use

The present invention relates to the ligand polypeptide for the human pituitary- and mouse pancreas-derived G protein-coupled receptor proteins. The ligand polypeptide or the DNA which codes for the ligand polypeptide can be used for (1) development of medicines such as pituitary function modulators, central nervous system function modulators, and pancreatic function modulators, and (2) development of recombinant receptor proteins and screening of pharmaceutical candidate compounds. In particular, by the receptor binding assay systems utilizing the expression of recombinant G protein-coupled receptor proteins in accordance with the invention, agonists and antagonists of G protein-coupled receptors which are specific to human and other warm-blooded animals can be screened and the agonists or antagonists obtained can be used as therapeutic and prophylactic agents for various diseases.

Polypeptides their production and use

A novel G-protein coupled receptor protein, a partial peptide and their salts are disclosed. DNA encoding the receptor protein, production of the receptor protein, determination of a ligand to the receptor protein, a method for screening for compounds which inhibit ligand binding to the receptor protein, a kit for screening for such compounds are also disclosed. The receptor protein, its partial peptide and their salts are used for screening for candidate compounds of drugs and the like.

Human G-protein coupled receptor polynucleotides

Growing community of inventors

Tsukuba, Japan

Yuji Kawamata