发明授权
- 专利标题: Cystine knot peptides that bind alpha-V-beta-6 integrin
- 专利标题(中): 结合α-V-β-6整联蛋白的胱氨酸结结肽
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申请号: US14283830申请日: 2014-05-21
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公开(公告)号: US09206237B2公开(公告)日: 2015-12-08
- 发明人: Richard H. Kimura , Sanjiv S. Gambhir , Benjamin J. Hackel , Robert Teed , Bin Shen , Frederick T Chin , Zhen Cheng
- 申请人: The Board of Trustees of the Leland Stanford Junior University
- 申请人地址: US CA Stanford
- 专利权人: The Board of Trustees of the Leland Stanford Junior University
- 当前专利权人: The Board of Trustees of the Leland Stanford Junior University
- 当前专利权人地址: US CA Stanford
- 代理机构: Bozicevic, Field & Francis LLP
- 代理商 David J. Aston
- 主分类号: C07K14/00
- IPC分类号: C07K14/00 ; A61K51/08 ; G01N33/574 ; G01N33/68
摘要:
Disclosed are peptides comprising a molecular scaffold portion and a loop portion that binds to integrin αvβ6. This integrin is expressed on pancreatic tumors, making the peptides useful as imaging agents, among other uses. The peptides showed single-digit nanomolar dissociation constants similar to antibodies used clinically for imaging and therapy. The peptides rapidly accumulated in αvβ6-positive tumors, which led to excellent tumor-to-normal contrast. The peptides are specific for the targeted integrin αvβ6 receptors expressed on orthotopic pancreatic tumors and various xenografts used. Additionally, pharmacokinetic-stabilization strategies endowed knots with rapid renal clearance, which significantly reduced off-target dosing.
公开/授权文献
- US20140271469A1 CYSTINE KNOT PEPTIDES THAT BIND ALPHA-V-BETA-6 INTEGRIN 公开/授权日:2014-09-18
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