Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limited

Takeda Gmbh

Human Genome Sciences, Inc.

Takeda Chemical Ind., Ltd.

Human Gene Sciences

Shuji Hinuma

Ryo Fujii

Masaki Hosoya

Chieko Kitada

Shoji Fukusumi

Yugo Habata

Yuji Kawamata

Shuichi Furuya

Koichi Kato

Nobuo Choh

Haruo Onda

Masataka Harada

Makoto Kobayashi

Shoichi Ohkubo

Yasuaki Ito

Hiromi Yoshida

Hirokazu Matsumoto

Yukio Fujisawa

Yasushi Shintani

Kazuhiko Tatemoto

Steven M Ruben

Yi Li

Takuya Watanabe

Masaaki Mori

Daniel R Soppet

Tetsuya Ohtaki

Kazunori Nishi

Yasuko Terao

Shoichi Okubo

Kazuhiro Ohgi

Kuniko Kikuchi

Aki Mayumi

Tsuneo Yasuma

Hideyuki Tanaka

Naoyuki Kanzaki

Nobuhiro Suzuki

Naoki Nishizawa

Kazuhiro Ogi

Shinobu Sasaki

Fumio Itoh

Hidekazu Sawada

Yuji Ishichi

Taisuke Tawaraishi

Tadatoshi Hashimoto

Hideki Kizawa

Kohji Fukatsu

Hideki Matsui

Takeo Moriya

Kyozo Tsukamoto

Yasuhiro Tanaka

Mariko Hirohashi

Aki Aono

Tatsuo Yamamoto

Hidetoshi Komatsu

Makoto c/o Takeda Pharm Co Ltd Kobayashi

Tadatoshi c/o Takeda Pharm Co Ltd Hashimoto

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 GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

Receptor function regulator

By using FPRL1 ligand, which comprises the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, SEQ ID NO: 17 or SEQ ID NO: 21, and FPRL1, an efficient screening for FPRL1 agonist or FPRL1 antagonist can be performed.

FPRL1 ligands and use thereof

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 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 present invention relates to novel peptide derivatives, which are recognized as ligands to G-coupled protein receptor proteins. The peptide of the present invention can be used in (1) development of a receptor binding assay system using the expression system of the recombinant receptor protein and screening of candidates for pharmaceutical compounds, and (2) development of pharmaceutical preparations such as a neutral nerve function regulator, a circulatory function regulator, a cardiac function regulator, an immune function regulator, a digestive organ function regulator, a metabolic function regulator, a generative organ regulator or the like.

Peptides having ligand activities on APJ that is an orphan G protein-coupled receptor, and use thereof

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 anti-19P2 ligand monoclonal antibodies of the invention (in particular P2L-1Ca) have very high binding ability and can neutralize the arachidonic acid metabolite releasing activity of the 19P2 ligand. Therefore, they can be used, among others, as diagnostic, prophylactic and/or therapeutic agents for various diseases caused by some or other abnormality in the pituitary function modulating activity (e.g. prolactin secretion promoting activity), central nervous system modulating activity and pancreatic function modulating activity, among others, supposedly possessed by the 19P2 ligand.

Antibody and use thereof

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

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

The RFRP-3 peptide of the present invention which is an agent for promoting prolactin secretion is useful as a prophylactic and/or therapeutic agent for various diseases associated with prolactin secretion, such as hypoovarianism, seminal vesicle hypoplasia, menopausal syndrome and hypothyroidism.

RFRP-3 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.

Screening method

Growing community of inventors

Tsukuba, Japan

Shuji Hinuma