Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limited

Takeda Chemical Ind., Ltd.

Chieko Kitada

Shuji Hinuma

Tetsuya Ohtaki

Masaki Hosoya

Hirokazu Matsumoto

Yugo Habata

Takuya Watanabe

Ryo Fujii

Masahiko Fujino

Taiji Asami

Shoji Fukusumi

Yoshihiro Ishibashi

Masaaki Mori

Nobuhiro Suzuki

Yasushi Shintani

Haruo Onda

Kazuhiro Ogi

Yukio Shimomura

Yasuko Terao

Naoki Nishizawa

Tsukasa Sugo

Yuji Kawamata

Yasushi Masuda

Yasuko Horikoshi

Kazuhiko Tatemoto

Mitsuhiro Wakimasu

Toshifumi Watanabe

Chiharu Kimura

Akira Arimura

Norio Shimamoto

Mika Goto

Hiromi Yoshida

Kimiko Kanehashi

Hideki Matsui

Mioko Harada

Yasunori Miyamoto

Yoshio Matsumoto

Yuka Adachi

Michiko Abe

Kuniko Kikuchi

Asano Odaka

Osamu Nishimura

Shuichi Furuya

Koichi Kato

Tsunehiko Fukuda

Kazunori Nishi

Naoki Tarui

Shiro Takekawa

Masataka Harada

Yasuaki Itoh

Masao Tsuda

Shuji Sato

Toshimi Nagi

Hidetoshi Komatsu

Naoko Nishizawa

Eri Hashimoto

Kozo Hayashi

Hisanori Matsui

Hiroyuki Miya

Yuko Noguchi

The invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, etc.). By modifying the constituent amino acids of metastin with specific modifying groups, metastin derivatives having more improved blood stability, etc. than native metastin and showing excellent cancer metastasis suppressing activity or cancer growth suppressing activity have been found. Furthermore, it has been found that these metastin derivatives exhibit effects of suppressing gonadotropic hormone secretion, suppressing sex hormone secretion, etc., which are wholly different from the effects heretofore known.

Metastin derivatives and use thereof

The present invention provides a metastin derivative in which the amino acids comprising metastin were modified by alternative chemical substituents resulting in metastin derivitives, having excellent blood stability and exhibiting cancer metastasis inhibiting action or cancer growth inhibiting action.

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

Metastin, compounds that promote the activity of metastin or its receptors and the like are excellent gonadal function improving agents, ovulation inducers or promoters, gonadotropic hormone secretion promoters, gonadotropic hormone secretion inhibitors, sex hormone secretion promoters, sex hormone secretion inhibitors, etc., and can be used as agents for preventing/treating sterility, hormone-sensitive cancers, endometriosis, etc. Metastin and its receptors are useful for screening for these pharmaceuticals.

Methods of inhibiting secretion of follicle-stimulating hormone and testosterone

The present invention aims at providing an antibody, by which metastin or its derivative can be quantified specifically with a high sensitivity, a method of detecting/quantifying metastin or its derivative using the antibody, and a diagnostic agent (e.g., a diagnostic for pregnancy) the same. Specifically, an antibody capable of specifically reacting with a partial peptide at the N-terminus or C-terminus of a polypeptide having the amino acid sequence represented by SEQ ID NO: 1 or its derivative, and a method of detecting/quantifying metastin or its derivative using the antibody as well as a diagnostic agent using the same.

Anti-metastin antibody and its use

The present invention provides a ligand to GPR8, in particular polypeptides capable of binding to GPR8 or its amides or esters, or salts thereof, as well as the DNA encoding for such polypeptides. The ligand to GPR8 of the present invention is useful in developing receptor-binding assay systems with the use of a GPR8 expression system, for screening candidate compounds for drugs such as preventive/therapeutic agents for obesity, appetite stimulants, and prolactin production inhibitors.

Ligand to GPR8

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

The present invention relates to rat cerebellum-derived and human brain-derived G protein coupled receptor proteins or salts thereof, their partial peptides, amides, esters or salts thereof, ligands to the same, a method/kit for screening compounds that alter the binding property between the ligands and the G protein coupled receptor proteins, compounds obtained by the screening or salts thereof, and antibodies to the G protein coupled receptor proteins.

Screening assay using G-protein coupled receptor protein OT7T175

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 present invention relates to a peptide comprising an amino acid sequence identical to or substantially identical to an amino acid sequence represented by SEQ ID NO: 35 and having an ability of binding to a receptor protein comprising an amino acid sequence identical to or substantially identical to an amino acid sequence represented by SEQ ID NO: 1, SEQ ID NO: 2 or SEQ ID NO: 3, or a precursor thereof, its amide or ester, or a salt thereof. An inventive peptide-encoding DNA or equivalent can be employed in (1) a development of a receptor binding assay system using an expression system of a recombinant receptor protein and a screening for a pharmaceutical candidate compound, and (2) a development of a pharmaceutical having a reduced side effect such as a memory function improving agent, an appetite improving agent, an uterine, renal, prostatic, testicular or skeletal muscle function regulating agent.

DNA encoding galanin receptor activating peptide

The antibody of the present invention, which specifically reacts with the N-terminal or C-terminal partial peptide of TGR23-2 ligand, is useful in detecting and quantifying the TGR23-2 ligand. Moreover, it is useful as a preventing/treating agent and a diagnostic agent for cancer, etc.

The present invention aims at providing a novel polypeptide, a receptor, a DNA thereof, and the like. Specifically, the present invention provides a polypeptide having a binding ability to the protein represented by SEQ ID NO: 1 or SEQ ID NO: 3, or its amide, its ester or its salt, a polynucleotide encoding the polypeptide, an antisense polynucleotide or an antibody to the polypeptide, a screening of agent for prevention and/or treatment of cancer, obesity, etc., which comprises using the above, and the like. The polypeptide, receptor, polynucleotide, antisense polynucleotide, antibody and the like are useful for an agent of prevention and/or treatment of cancer, obesity and the like. Further, they are useful for a screening of an agent for prevention and/or treatment of cancer, obesity and the like.

Polypeptide DNA thereof and use of the same

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Osaka, Japan

Chieko Kitada