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    • 1. 发明申请
    • G protein coupled receptor protein, production and use thereof
    • G蛋白偶联受体蛋白,其生产和使用
    • US20030113909A1
    • 2003-06-19
    • US09929752
    • 2001-08-14
    • Takeda Chemical Industries, Ltd.
    • Shuji HinumaRyo FujiiYuji Kawamata
    • C12Q001/68G01N033/53G01N033/567C12P021/06C12N015/00C12N015/09C12N015/63C12N015/70C12N015/74C07K005/00C07K007/00C07K016/00C07K017/00A61K038/00C12N005/00C12N005/02C12P021/08
    • C07K14/705
    • Rabbit gastropyrolic part smooth muscle-derived G protein coupled receptor proteins, partial peptides thereof; and DNAs containing said protein or partial peptide-encoding DNA are provided. The receptor protein and the DNA coding for said protein can be used for {circle over (1)} determination of ligands; {circle over (2)} acquisition of antibody and antiserum; {circle over (3)} construction of expression system for of a recombinant type receptor protein; {circle over (4)} development of the receptor binding assay system using said expression system and screening of the candidate compounds for pharmaceuticals; {circle over (5)}conducting a drug design based upon a comparison with structurally analogous ligands and receptors; {circle over (6)} preparation of probes and PCR primers for a gene diagnosis; {circle over (7)} preparation of transgenic animals; and {circle over (8)}preparation of model patient animals deficient in the receptor protein DNA. Elucidation of the structure and property of the G protein coupled receptor is particularly related to the development of unique pharmaceuticals which act on such a system.
    • 兔子胃部分平滑肌衍生的G蛋白偶联受体蛋白,其部分肽; 并提供含有所述蛋白质或部分肽编码DNA的DNA。 受体蛋白和编码所述蛋白质的DNA可以用于(循环(1个配体的测定; {循环(2次获得抗体和抗血清; {circle over(3构建重组型受体蛋白质的表达系统 ;(循环(使用所述表达系统的受体结合测定系统的4个开发和用于药物的候选化合物的筛选); {循环(基于与结构上类似的配体和受体的比较来设计药物设计; {循环(6 制备用于基因诊断的探针和PCR引物;(循环(7个转基因动物的制备;和循环(8个制备缺陷受体蛋白DNA的模型患者动物),阐明G蛋白偶联受体的结构和性质 特别是与这种系统的独特药物的开发有关。
    • 2. 发明申请
    • G protein coupled receptor proteins, their production and use
    • G蛋白偶联受体蛋白,其生产和使用
    • US20020168720A1
    • 2002-11-14
    • US10067477
    • 2002-02-04
    • Takeda Chemical Industries Ltd.
    • Shuji HinumaJunichi SakamotoMasaki Hosoya
    • C07K014/705C07H021/04C12N005/06C12P021/02
    • C07K14/705C07K14/723
    • This invention relates to a human amygdaloid nucleus-derived G protein coupled receptor protein or a salt thereof, a partial peptide of the G protein coupled receptor protein, DNA encoding the G protein coupled receptor protein, a method of producing the G protein coupled receptor protein, a method of identifying a ligand to the G protein coupled receptor protein, a method or kit for screening out compounds capable of changing the binding activity of a ligand to the G protein coupled receptor protein, a compound or a salt thereof obtained by the screening method or by using the screening kit, a pharmaceutical composition comprising the compound or a salt thereof, and an antibody against the G protein coupled receptor protein or a partial peptide. The G protein coupled receptor protein and DNA encoding the protein can be used (1) identifying a ligand to the G protein coupled receptor protein of the present invention, (2) acquiring antibodies and antisera, (3) constructing the expression system for the recombinant receptor protein, (4) developing receptor binding assay systems using the expression system, and screening out candidate drug substances, (5) drug designing based on comparison with structurally similar ligands and receptors, (6) construction of probes and PCR primers for gene diagnosis, and (7) gene therapy, among others. In particular, elucidation of the structure and properties of the G protein coupled receptor will result in development of a unique drug acting on these systems.
    • 本发明涉及人杏仁核衍生的G蛋白偶联受体蛋白或其盐,G蛋白偶联受体蛋白的部分肽,编码G蛋白偶联受体蛋白的DNA,产生G蛋白偶联受体蛋白的方法 鉴定G蛋白偶联受体蛋白质的配体的方法,用于筛选能够改变配体与G蛋白偶联受体蛋白质的结合活性的化合物的方法或试剂盒,通过筛选获得的化合物或其盐 方法或通过使用筛选试剂盒,包含该化合物或其盐以及针对G蛋白偶联受体蛋白或部分肽的抗体的药物组合物。 可以使用G蛋白偶联受体蛋白和编码蛋白的DNA(1)鉴定本发明的G蛋白偶联受体蛋白质的配体,(2)获得抗体和抗血清,(3)构建重组体的表达系统 受体蛋白,(4)使用表达系统开发受体结合测定系统,筛选候选药物,(5)基于与结构相似的配体和受体的比较的药物设计,(6)构建探针和用于基因诊断的PCR引物 ,(7)基因治疗等。 特别地,解释G蛋白偶联受体的结构和性质将导致发挥作用于这些系统的独特药物。
    • 3. 发明申请
    • G protein coupled receptor protein, production, and use thereof
    • G蛋白偶联受体蛋白,其生产和使用
    • US20030138817A1
    • 2003-07-24
    • US10278087
    • 2002-10-22
    • Takeda Chemical Industries, Ltd.
    • Shuji HinumaYasuaki ItoRyo Fujii
    • C12Q001/68C07H021/04C12P021/02C12N005/06C07K014/705
    • C12Q1/6876C07K14/705C07K14/70571C07K14/723C12Q1/6809C12Q1/6883
    • DNA primers effective in screening G protein coupled receptor protein-encoding DNA fragments are provided. The primers which are complementary to nucleotide sequences that are in community with (homologous to) the nucleotide sequences encoding amino acid sequences corresponding to or near the first membrane-spanning domain or the sixth membrane-spanning domain each of known various G protein coupled receptor proteins were designed and synthesized. Methods of amplifying G protein coupled receptor protein-encoding DNAs using the above DNA primers, and novel target G protein coupled receptor protein-encoding DNAs are also provided. Screening of DNA libraries can be efficiently carried out. Human pituitary gland or amygdala-derived and mouse pancreas-derived G protein coupled receptor proteins, etc. or salts thereof, partial peptides thereof, DNAs coding for the above G protein coupled receptor proteins, processes for producing the above G protein coupled receptor proteins, methods of determining ligands for the above G protein coupled receptor proteins, methods of screening compounds that inhibit the binding between the ligand and the G protein coupled receptor proteins or screening kits therefor, compounds or salts thereof obtained by the above screening method or the screening kit, pharmaceutical compositions containing the above compounds or salts thereof, and antibodies against the above protein coupled receptor proteins or partial peptides thereof are provided.
    • 提供了有效筛选编码G蛋白偶联受体蛋白的DNA片段的DNA引物。 与与编码对应于或接近第一跨膜结构域或第六跨膜结构域的氨基酸序列的核苷酸序列(同源的)的核苷酸序列互补的引物,每个已知的各种G蛋白偶联受体蛋白 被设计和合成。 还提供了使用上述DNA引物扩增G蛋白偶联受体蛋白质编码DNA的方法,以及新的靶向G蛋白偶联受体蛋白质编码DNA。 可以有效地进行DNA文库的筛选。 人类垂体腺或来自扁桃体的小鼠胰腺衍生的G蛋白偶联受体蛋白等,或其盐,其部分肽,编码上述G蛋白偶联受体蛋白质的DNA,用于产生上述G蛋白偶联受体蛋白质的方法, 确定上述G蛋白偶联受体蛋白质的配体的方法,筛选抑制配体和G蛋白偶联受体蛋白质或其筛选试剂盒之间的结合的化合物的方法,通过上述筛选方法获得的化合物或其盐或筛选试剂盒 提供含有上述化合物或其盐的药物组合物和针对上述蛋白质偶联受体蛋白质或其部分肽的抗体。
    • 5. 发明申请
    • Galanin receptor protein, production and use thereof
    • 格拉宁受体蛋白,其生产和使用
    • US20030008329A1
    • 2003-01-09
    • US10090569
    • 2002-03-04
    • Takeda Chemical Industries, Ltd.
    • Shuji HinumaRyo FujiiShoji FukusumiTetsuya OhtakiMasaki HosoyaKazuhiro OhgiHaruo Onda
    • G01N033/567C07H021/04C12P021/02C12N005/06C07K014/705
    • C07K14/723
    • Galanin receptor proteins, production and use thereof including screening of galanin receptor agonists and antagonists are provided. Galanin receptor proteins, etc. or salts thereof, partial peptides thereof, DNAs coding for the above galanin receptor protein, processes for producing the above receptor protein, methods of screening for a galanin receptor agonist and/or antagonist or screening kits therefor, agonist and/or antagonist compounds or salts thereof obtained by the above screening method or the screening kit, pharmaceutical compositions containing the above compound or its salt, and antibodies against the above receptor protein are provided. It is allowable to efficiently screen a galanin receptor agonist or antagonist by using the galanin receptor protein, the partial peptide thereof, the galanin receptor protein-encoding DNA, the receptor protein-containing cell or its membrane fraction. The pharmaceuticals thus screened or characterized permits various applications including prophylactic and/or therapeutic treatments against a variety of diseases, e.g., stomach ulcer, diabetes, Alzheimer's disease, dementia, etc. and a sedative.
    • 提供了Galanin受体蛋白质,其生产和使用,包括甘露糖素受体激动剂和拮抗剂的筛选。 加兰林素受体蛋白等或其盐,其部分肽,编码上述甘丙肽受体蛋白质的DNA,产生上述受体蛋白质的方法,筛选甘丙肽受体激动剂和/或拮抗剂的方法或其筛选试剂盒,激动剂和 /或通过上述筛选方法获得的拮抗剂化合物或其盐或筛选试剂盒,含有上述化合物或其盐的药物组合物和抗上述受体蛋白的抗体。 可以通过使用甘丙肽受体蛋白,其部分肽,编码甘露糖素受体蛋白的DNA,含受体蛋白的细胞或其膜部分来有效筛选甘丙肽受体激动剂或拮抗剂。 如此筛选或表征的药物允许各种应用,包括针对各种疾病(例如胃溃疡,糖尿病,阿尔茨海默病,痴呆等)和镇静剂的预防和/或治疗性治疗。