Takeda Pharmaceutical Company Limited

Takeda Chemical Industries, Inc.

Takeda Gmbh

Human Genome Sciences, Inc.

Human Gene Sciences

Ryo Fujii

Shuji Hinuma

Masaki Hosoya

Shoji Fukusumi

Chieko Kitada

Yugo Habata

Yuji Kawamata

Makoto Kobayashi

Masaaki Mori

Yasushi Shintani

Masataka Harada

Yasuaki Ito

Kazuhiko Tatemoto

Steven M Ruben

Yi Li

Takuya Watanabe

Daniel R Soppet

Tetsuya Ohtaki

Kazunori Nishi

Yasuko Terao

Shoichi Okubo

Kazuhiro Ohgi

Kuniko Kikuchi

Yasuhiro Tanaka

Toshio Tanaka

Hideyuki Tanaka

Haruo Onda

Jinichi Yonemori

Kazuhiro Ogi

Shoichi Ohkubo

Tadatoshi Hashimoto

Hiromi Yoshida

Kohji Fukatsu

Hideki Kizawa

Hideki Matsui

Takeo Moriya

Syuji Hinuma

Masanori Miwa

Hidetoshi Komatsu

Yuko Noguchi

Makoto c/o Takeda Pharm Co Ltd Kobayashi

Tadatoshi c/o Takeda Pharm Co Ltd Hashimoto

An agent for regulating 14273 receptor function, which is useful as a preventing or treating drug for diabetes mellitus, hyperlipidemia or the like, is provided. An agent for regulating 14273 receptor function comprising a compound containing an aromatic ring and a group capable of releasing a cation.

Receptor function regulating agent

By using a G protein-coupled receptor protein comprising an amino acid sequence, which is the same or substantially the same as the amino acid sequence represented by SEQ ID NO: 1, or a salt thereof, and an ionizable metal element or a salt thereof, an agonist for or an antagonist to the above receptor protein or a salt thereof can be efficiently screened.

Screening method for binding property or signal transduction alterations

The present invention provides a method of screening an agonist or antagonist to a G protein-coupled receptor protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, or a salt thereof, which comprises using the receptor protein or a salt thereof and the ligand or a salt thereof; etc. The present invention is useful for screening agents for the prevention/treatment of, e.g., leukopenia, leukemia, lymphoma, malignant tumor, ulcerative colitis, rheumatoid arthritis, inflammatory bowel disorders, tonsil disorders, collagen disease, inflammatory disease, leukocytosis, heart failure, inherited muscle disorders, muscular dystrophy, neuromuscular degenerative disease, myocardial infarction, obesity, mellitus diabetes, hyperlipemia, arteriosclerosis, metabolic syndrome, thrombocytopenia, thrombocytosis, cancer, pulmonary edema, multiple organ failure, etc.

Methods of screening for compounds which bind G protein-coupled receptors

The present invention provides a method of screening an agonist/antagonist of a G protein-coupled receptor protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, or a salt thereof, which comprises using the receptor protein or its salt and a ligand or its salt; and so on. The screening method of the present invention is useful for screening an agent for the prevention/treatment of nervous system diseases or neuropathic pains.

Ligands for G protein-coupled receptor protein and use thereof

This invention relates to a novel polypeptide involving in the modulation of central nervous system function, circulatory function, immune function, gastrointestinal function, metabolic function, reproductive function, etc., it can be used as a drug for treating or preventing a variety of diseases, e.g. HIV infection or AIDS (acquired immune deficiency syndrome) or the like.

Polypeptides, their production and use

The present invention relates to screening of an agonist/antagonist, etc. Specifically, the present invention provides a method of screening an agonist or antagonist of a G protein-coupled receptor protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, or a salt thereof, which comprises using the receptor protein or a salt thereof and a cholesterol metabolism-related substance, and so on.

Method of screening compounds which alter the binding properties of GPR39, and homologs thereof, to bile acid

The polypeptides in the present invention possess the effects of promoting and inhibiting the secretion of prolactin, and are thus useful as drugs for the prevention and treatment of various diseases, in terms of prolactin secretion stimulants, which are associated with the secretion of prolactin, such as hypoovarianism, spermatic underdevelopment, menopausal symptoms, hypothyroidism, etc. The polypeptides are useful as drugs for the prevention and treatment of various diseases, in terms of prolactin secretion inhibitors, which are associated with the secretion of prolactin, such as pituitary tumor, diencephalon tumor, menstrual disorder, autoimmune diseases, prolactinoma, sterility, impotence, amenorrhea, lactorrhea, acromegaly, Chiari-Frommel syndrome, Argonz-del Castilo syndrome, Forbes-Albright syndrome, lymphoma, Sheehan's syndrome, spermatogenesis disorder, etc.

Use of a G protein-coupled receptor and its cognizant ligand in the identification of compounds that affect prolactin secretion

The use of a G-protein coupled receptor protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, or a salt thereof and a ligand peptide comprising the amino acid sequence represented by any of SEQ ID NO: 3 to 7, or a salt thereof, enables efficient screening of an agonist or antagonist for the above receptor protein or a salt thereof.

Methods of screening for ligands for FPRL2

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

A GPR7 ligand containing the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO:1 wherein the N-terminal amino acid residue may optionally be brominated, is useful in developing a receptor-binding assay system with the use of the GPR7 expression system, in screening a candidate compound for a drug such as an antiobestic, etc.

Ligand of G protein-coupled receptor protein and DNA thereof

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.

G protein-coupled receptor protein, its DNA and ligand thereof

By using a G protein-coupled receptor protein containing an amino acid sequence, which is the same or the substantially the same as an amino acid sequence represented by SEQ ID NO:1, SEQ ID NO:10, SEQ ID NO:12 or SEQ ID NO:14, or its salt together with humanin, a compound or its salt capable of changing the binding properties of the above receptor protein or its salt to humanin can be efficiently screened.

Method of screening therapeutic agents for nerve degeneration associated diseases

The screening method for a compound or a salt thereof that alters the binding property between Neuromedin U or a salt thereof and TGR-1 or a salt thereof, characterized by using Neuromedin U, a derivative thereof or a salt thereof and TGR-1 or a salt thereof, can be useful for screening a therapeutic and/or prophylactic agent for hypertension and stress-related diseases, etc. A TGR-1 antagonist can be useful as a therapeutic and/or prophylactic agent for hypertension and stress-related diseases, etc.

Growing community of inventors

Ibaraki, Japan

Ryo Fujii