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1. 发明申请

WO1998008100A1 AGONIST-DEPENDENT INTERNALIZATION OF HUMAN SOMATOSTATIN RECEPTORS TYPES 1-5 审中-公开
标题翻译：人类SOMATOSTATIN受体的激素依赖性内分泌类型1-5
公开(公告)号：WO1998008100A1
公开(公告)日：1998-02-26
申请号：PCT/CA1997000592
申请日：1997-08-20
申请人： PATEL, CELL & RECEPTOR TECHNOLOGIES INC. , PATEL, Yogesh, C. , HUKOVIC, Nedim , PANETTA, Rosemarie , KUMAR, Ujendra
发明人： PATEL, CELL & RECEPTOR TECHNOLOGIES INC.
IPC分类号： G01N33/74
CPC分类号： A61K51/08 , G01N33/574 , G01N33/57415 , G01N33/6893 , G01N2333/726
摘要： The present invention relates to the uses of human somatostatin receptors types 1-5 in the diagnosis and/or treatment of diseases and more particularly to tumor cells, e.g. breast cancer and in cases of Alzheimer's. The present invention relates to (i) recombinant host cells (CHO-Kl cells) individually expressing the 5 hSSTR subtypes; (ii) the use of these cells as tools for testing the ability of synthetic SST agonists or antagonists to induce receptor internalization or upregulation; (iii) the use of the internalization property of hSSTR subtypes to target tumors for selective targeted destruction. For instance, subtypes such as hSSTR3 and 5 which are extensively internalized could be targeted with selective alpha or beta -emitting SST radioligands for radiotherapy of, for example, breast cancers which display a rich concentration of these receptors; (iv) the use of the ability of hSSTR1 (in particular) and hSSTR2 and 4 (to a lesser extent) to be upregulated at the cell surface upon prolonged treatment with agonist as a test for increasing the sensitivity of receptor scans for detection and diagnosis of tumors and inflammatory conditions; (v) the use of the differential ability of the hSSTR subtypes to be upregulated or internalized as a means for producing enhanced images in receptor scans by subtraction analysis to recruit, for example, SSTR1 selective to the membrane whilst internalizing others such as hSSTR3, hSSTR4, and hSSTR5.
摘要翻译：本发明涉及1-5型人生长抑素受体在诊断和/或治疗疾病中的用途，更具体地涉及肿瘤细胞，例如，乳腺癌和阿尔茨海默病。本发明涉及（i）分别表达5个hSSTR亚型的重组宿主细胞（CHO-K1细胞）; （ii）使用这些细胞作为测试合成SST激动剂或拮抗剂诱导受体内化或上调的能力的工具; （iii）使用hSSTR亚型的内在特性来靶向肿瘤以进行选择性靶向破坏。例如，广泛内化的hSSTR3和5型亚型可以用选择性α或β发射的SST放射性配体靶向用于放射治疗，例如显示这些受体浓度较高的乳腺癌; （iv）长时间用激动剂治疗时，使用hSSTR1（特别是）和hSSTR2和4（在较小程度上）的能力在细胞表面上调节作为增加受体扫描检测和诊断灵敏度的试验的肿瘤和炎症病症; （v）使用hSSTR亚型的差异能力作为在受体扫描中通过减法分析产生增强图像的手段进行上调或内化，以招募例如对膜选择性的SSTR1，同时内化其他如hSSTR3，hSSTR4 ，和hSSTR5。

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