Japan Science and Technology Corporation

J-pharma Co., Ltd.

Human Cell Systems, Inc.

Other

Japan Science and Technology Agency

Dowa Mining Co., Ltd.

Nippon Zoki Pharmaceutical Co., Ltd.

Nippon Chemiphar Co., Ltd.

Dethree Res. Lab. Inc.

Torli Pharmaceutical Co., Ltd.

Fuji Bio Medix Co., Ltd.

Endou, Hitoshi

Hitoshi Endou

Koji Yamashita

Yoshikatsu Kanai

Takashi Sekine

Atsushi Enomoto

Michael Fitzpatrick Wempe

Naohiko Anzai

Seok Ho Cha

Daisuke Saito

Kazuharu Ienaga

Kunio Kobayashi

Toshihiro Oikawa

Masahiro Furo

Tsuyoshi Endo

Masuharu Hirano

Hiroto Tanaka

Tomotaka Yanagita

Richard J Johnson

Isao Okayasu

Jean-Francois Peyron

Karen L Price

Hiroyuki Kusuhara

Promsuk Jutabha

Kenji Tsujihara

Kunio Saito

Makoto Hosoyamada

Tadao Hishinuma

Hirano Masuharu

A method for treating cancer includes administering to a subject in need of the treatment an anticancer agent composition that includes the following agents as active ingredients; a LAT1 inhibitor, and one or more agents selected from the group consisting of an alkylating agent, a platinum-based antineoplastic agent, an anti-metabolite, a topoisomerase inhibitor, an anti-microtubule polymerizing agent, a hormonal agent, an anti-microtubule depolymerizing agent, an anticancer antibiotic, and a molecular targeted agent.

Anticancer agent composition

Provided are a compound represented by the following Formula (III), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt or solvate thereof used as a therapeutic agent for gout or hyperuricemia. (In the Formula (III), R, R, R, and Rrepresent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or a cyano group, Rand Rform a benzene ring or a 5-membered heteroaryl ring containing 1 to 3 heteroatoms, as a ring constituent element, selected from nitrogen atoms, oxygen atoms, and sulfur atoms together with two carbon atoms to which Rand Rare bonded, Rand Rform a benzene ring together with two carbon atoms to which Rand Rare bonded or represent any of the groups represented by Rdescribed above, Wrepresents CRor N, and where, Rrepresents any of the groups represented by R, Xrepresents an oxygen atom or a sulfur atom, Yrepresents an alkylene chain having 1 to 8 carbon atoms, and where, the alkylene chain may be substituted with an alkyl group having 1 to 8 carbon atoms and the alkylene chain may be a linear or branched alkylene chain, the branched alkylene chain may have a 3- to 7-membered ring formed by side chains bonded to carbon atoms which are the same as or different from each other, together with the carbon atoms to which the side chains are bonded and may have a double bond in the middle thereof, and Zrepresents COH). 

URAT1 inhibitor

A compound represented by the general Formula I: 

Developing potent urate transporter inhibitors: compounds designed for their uricosuric action

A method for the diagnosis of breast cancer using an anti-LAT1 monoclonal antibody. Among intraductal breast neoplastic lesions, duct carcinoma in situ, which is malignant, expresses LAT1 at a significantly high level, as compared to intraductal breast papilloma, which is benign. An anti-LAT1 monoclonal antibody is useful for the discrimination between these two lesions. Further, LAT1 is expressed at a high level in most of triple negative infiltrating carcinomas, which are negative for all of ER, PgR, and HER2 that are conventional molecular targeting markers for breast cancer. Therefore, LAT1 can be used as a novel molecular targeting marker for the triple negative breast cancer.

Biomarker for breast cancer

It is intended to clarify a transportation system participating in the uric acid uptake in vascular smooth muscle cells (VSMCs) and provide a novel remedy, a preventive or a treating agent for vascular disorders, hypertension and renal disorders with the use of a drug participating in this transportation system. It is also intended to provide a novel screening system for a remedy, a preventive or a treating agent for vascular disorders, hypertension and renal disorders with the use of such a transportation system. Namely, a medicinal composition for healing, preventing or treating vascular disorders, hypertension and renal disorders which comprises a drug having an effect of inhibiting the uric acid uptake by a uric acid transporter URAT1 and a pharmaceutically acceptable carrier; and a method of screening a substance efficacious for healing, preventing or treating vascular disorders, hypertension and renal disorders which comprises using a cell line expressing URAT1 in the presence or absence of a test compound and assaying the uric acid uptake level, cell proliferation ability or the amount of a monocyte chemotactic factor produced by the cells.

Method of screening for therapeutic compounds for vascular disorders and hypertension based on URAT1 activity modulation

A cerebral organic anion transporter OAT3 which is useful as a protein regulating the uptake/excretion of organic anionic substances in the brain; a nucleic acid having a base sequence encoding the same; and an antibody against the same. The amino acid sequence and the base sequence of the above OAT3 are shown in Sequence Listing in the description.

Cerebral organic anion transporter and its gene

A novel amino acid transporter molecule mediating transportation of amino acids, which are nutrients essentially required in the survival and proliferation of various normal cells constituting a living body and various pathology-associated abnormal cells such as tumor cells, into cells and being expressed specifically in tumor cells compared with normal cells; and drugs for treating various pathogenic conditions such as tumor (cancer) which are obtained by identifying and isolating the above amino acid transporter molecule and identifying a substance capable of inhibiting the biological activity and/or expression of this molecule. Intensive studies were made to identify a tumor cell membrane surface molecule associating or interacting with a cell membrane surface 4F2hc molecule seemingly playing an important role in the activation of an unknown amino acid transporter. As a result, a gene encoding the novel amino acid transporter molecule, which mediates the incorporation of various neutral amino acids, various drugs or physiological substances into cells, has been found out and a substance capable of inhibiting the incorporation of amino acids via this molecule and thus inhibiting the proliferation of tumor cells has been also found out.

Neutral amino acid transporter and gene thereof

It is intended to identify and provide a novel carnitine transporter gene participating in carnitine transport in the testis and epididymis and carnitine transporter which is a protein encoded by the gene. A protein comprising the amino acid sequence represented by SEQ ID NO: 2 or an amino acid sequence derived therefrom by deletion, substitution or addition of one to several amino acids and being capable of transporting carnitine or its analog; and a gene encoding this protein.

DNA encoding a testicular carnitine transporter

It is intended to provide amino acid transporters which act as a single molecule and transport neutral amino acids typified by branched amino acids, and genes thereof. A protein consisting of an amino acid sequence represented by SEQ ID NO:2, 4, 6 or 8 or an amino acid sequence derived from an amino acid sequence represented by SEQ ID NO:2, 4, 6 or 8 by deletion, substitution or addition of one to several amino acids, and being capable of sodium-independently transporting neutral amino acids typified by branched amino acids and analogs thereof as a single molecule. A gene which is a DNA consisting of a base sequence represented by SEQ ID NO:1, 3, 5 or 7 or a DNA hybridizable with it and encodes a protein capable of sodium-independently transporting branched amino acids as a single molecule.

Branched neutral amino acid transporters acting as single molecule

To provide highly safe therapeutic or preventive agents for hyperuricemia, more specifically uricosuric agents, which have potent uricosuric effect and do not cause grave hepatic disorder. Medicinal compositions for the treatment or prevention of hyperuricemia or diseases caused by hyperuricemia, which contain 6-hydroxybenzbromarone or salts thereof, and pharmaceutically acceptable carriers; uricosuric agents, xanthine oxidase inhibitors, and inhibitors against the uptake of uric acid in kidney, which contain 6-hydroxybenzbromarone or salts thereof; and a process for the production of 6-hydroxybenzbromarone.

Medicinal compositions containing 6-hydroxybenzbromarone or salts thereof

It is intended to identify and provide a novel urate transporter gene participating in the urate transport in the kidney and a urate transporter which is a polypeptide encoded by the above gene. Namely, a protein comprising the amino acid sequence represented by SEQ ID NO:1 or an amino acid sequence derived therefrom by deletion, substitution or addition of one to several amino acids and being capable of transporting uric acid and its analogs; and a gene encoding this protein.

Kidney-specific urate transporter and gene thereof

It is intended to provide a sodium-independent transporter carrying an acidic amino acid and its gene. A protein having the amino acid sequence represented by SEQ ID NO: 1 and being capable of sodium-independently transporting an acidic amino acid and its analogs; a gene encoding this protein; a fused protein of the above protein with an auxiliary factor enabling the expression of its function; a gene encoding the same; a method of analyzing the function of a transporter using the same: and utilization thereof.

Sodium-independent transporter carrying acidic amino acid and its gene

DNA encoding neutral amino acid transporter

A novel organic anion transporter gene participating in organic anion transport in the placenta; and an organic anion transporter which is a polypeptide encoded by the gene. A placental organic anion transporter OAT4, more particularly, a placental organic anion transporter OAT4 having the amino acid sequence represented by SEQ ID NO:2 or an amino acid sequence derived therefrom by deletion, substitution or addition of a part of the amino acids thereof. A nucleic acid (preferably DNA) having a base sequence encoding the placental organic anion transporter OAT4 or a base sequence hybridizable therewith under stringent conditions.

Placental organic anion transporter and gene thereof

1. An aromatic amino acid derivative represented by the formula (I) or its pharmacologically acceptable salt: wherein,

Growing community of inventors

Kanagawa, Japan

Hitoshi Endou