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    • 5. 发明申请
    • NEW G-PROTEIN COUPLED RECEPTOR LUSTR2 AND USES THEREOF
    • 新型G蛋白偶联受体LUSTR2及其用途
    • WO2003046179A2
    • 2003-06-05
    • PCT/EP2002/012820
    • 2002-11-15
    • BAYER AKTIENGESELLSCHAFTGOLZ, StefanBRÜGGEMEIER, UlfGEERTS, Andreas
    • GOLZ, StefanBRÜGGEMEIER, UlfGEERTS, Andreas
    • C12N15/12
    • C07K14/705
    • Polynucleotide sequence for novel G-protein coupled receptor LUSTR2 and uses thereof. The present invention is directed to a polynucleotide sequence of a novel G-Protein Coupled Receptor LUSTR2. More particularly, the present invention provides a polynucleotide sequence comprising the nucleic acid sequence SEQ ID NO: 1 or nucleic acid sequences that hybridize to SEQ ID NO: 1 or its complimentary strand having at least 40% sequence identity. Preferably, the hybridizing nucleic acid sequence should hybridize under stringent conditions and in particular have 85% sequence identity, more preferably 90% sequence identity, and most preferably 95% sequence identity. The invention also provides the human LUSTR2 associated with the haemaotological, peripheral and central nervous system, COPD, asthma, genito-urological, metabolic diseases and pancreas and heart disorders as a result of relative quantification of the mRNA distribution in different human tissues by expression profiling. The invention also provides assays for the identification of compounds useful for the modulation of hematological, peripheral and central nervous system, COPD, asthma, genito-urological, metabolic diseases and pancreas and heart disorders for treating or preventing hematological, peripheral and central nervous system, COPD, asthma, genito-urological, metabolic diseases and pancreas and heart disorders associated with expression of the LUSTR2. The methods of the invention involve cell-free and cell-based assays that identify compounds which bind to and/or activate or inhibit the activity of LUSTR2, a G protein coupled receptor, followed by an in vivo assay of the effect of the compound on hematological, peripheral and central nervous system, COPD, asthma, genito-urological, metabolic diseases and pancreas and heart disorders. The invention also features compounds which bind to and/or activate or inhibit the activity of LUSTR2 as well as pharmaceutical compositions comprising such compounds.
    • 新型G蛋白偶联受体LUSTR2的多核苷酸序列及其用途。 本发明涉及新型G-蛋白偶联受体LUSTR2的多核苷酸序列。 更具体地,本发明提供了包含核酸序列SEQ ID NO:1或与SEQ ID NO:1杂交的核酸序列或其具有至少40%序列同一性的互补链的多核苷酸序列。 优选地,杂交核酸序列应在严格条件下杂交,特别是具有85%序列同一性,更优选90%序列同一性,最优选95%序列同一性。 本发明还提供了与通过表达谱分析在不同人体组织中mRNA分布的相对定量相结合的血液学,外周和中枢神经系统COPD,哮喘,生殖泌尿,代谢疾病和胰腺和心脏病的人LUSTR2 。 本发明还提供了用于鉴定可用于调节血液系统,外周和中枢神经系统,COPD,哮喘,泌尿系统,代谢疾病和胰腺以及用于治疗或预防血液学,外周和中枢神经系统的心脏病的化合物的测定, COPD,哮喘,生殖泌尿,代谢疾病,与LUSTR2表达相关的胰腺和心脏病。 本发明的方法包括无细胞和基于细胞的测定,其鉴定结合和/或激活或抑制LUSTR2,G蛋白偶联受体的活性的化合物,随后在体内测定化合物对 血液学,外周和中枢神经系统,COPD,哮喘,泌尿系统,代谢疾病和胰腺和心脏病。 本发明还涉及结合和/或活化或抑制LUSTR2的活性的化合物以及包含这些化合物的药物组合物。