发明授权
- 专利标题: Receptor(SSTR4)-selective somatostatin analogs
- 专利标题(中): 受体(SSTR4) - 选择性生长抑素类似物
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申请号: US11041676申请日: 2005-01-24
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公开(公告)号: US07238775B2公开(公告)日: 2007-07-03
- 发明人: Jean E. F. Rivier , Jean Claude Reubi , Judit Erchegyi , Roland Riek
- 申请人: Jean E. F. Rivier , Jean Claude Reubi , Judit Erchegyi , Roland Riek
- 申请人地址: US CA San Diego
- 专利权人: The Salk Institute for Biological Studies
- 当前专利权人: The Salk Institute for Biological Studies
- 当前专利权人地址: US CA San Diego
- 代理机构: Fitch, Even, Tabin & Flannery
- 主分类号: A61K38/00
- IPC分类号: A61K38/00
摘要:
Analogs of SRIF which are selective for SSTR4 in contrast to the other cloned SRIF receptors are useful in determining tissue and cellular expression of the receptor SSTR4 and its biological role in regulating tumor growth. SRIF analog peptides, such as des-AA1,2,4,5,12,13[Ala7]-SRIF; des-AA1,2,4,5,12,13[Aph7]-SRIF, des-AA1,2,4,5,12,13[Aph7]Cbm-SRIF; des-AA1,2,4,5,12,13[Tyr2,Ala7]-Cbm-SRIF, and des-AA1,2,4,5,12,13[Tyr7,CβMe-L-2Nal8]-SRIF, and counterparts incorporating D-Cys3 and/or D-Trp8 and/or Ala11, bind with high affinity to the cloned human receptor SSTR4 and activate the receptor, but they do not bind with significant affinity to human SSTR1, SSTR2, SSTR3 or SSTR5. By incorporating an iodinated tyrosine in position-2 in these SSTR4-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, cytotoxins or highly radioactive elements can be N-terminally coupled or complexed thereto.
公开/授权文献
- US20050245438A1 Receptor(SSTR4)-selective somatostatin analogs 公开/授权日:2005-11-03
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