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    Cystine knot peptides that bind alpha-V-beta-6 integrin
    1.
    发明授权
    Cystine knot peptides that bind alpha-V-beta-6 integrin 有权
    结合α-V-β-6整联蛋白的胱氨酸结结肽

    公开(公告)号：US09206237B2

    公开(公告)日：2015-12-08

    申请号：US14283830

    申请日：2014-05-21

    申请人： The Board of Trustees of the Leland Stanford Junior University

    发明人： Richard H. Kimura ,  Sanjiv S. Gambhir ,  Benjamin J. Hackel ,  Robert Teed ,  Bin Shen ,  Frederick T Chin ,  Zhen Cheng

    IPC分类号： C07K14/00 ,  A61K51/08 ,  G01N33/574 ,  G01N33/68

    CPC分类号： C07K14/001 ,  A61K51/088 ,  G01N33/574 ,  G01N33/57492 ,  G01N33/6863 ,  G01N2333/70546

    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.

    摘要翻译： 公开了包含分子支架部分和结合整联蛋白αv＆bgr的环部分的肽6。 这种整合素在胰腺肿瘤中表达，使得肽可用作成像剂，以及其他用途。 这些肽显示出与临床上用于成像和治疗的抗体相似的单位纳摩尔解离常数。 肽在6个阳性的肿瘤中迅速积累，导致肿瘤与正常的对比。 这些肽对于在原位胰腺肿瘤和各种​​异种移植物上表达的靶向整合素αv和bgr 6受体是特异性的。 此外，药代动力学稳定化策略赋予了快速肾清除的结，这显着降低了靶外给药。

    CASPASE-TRIGGERED NANO-AGGREGATION PROBES AND METHODS OF USE
    4.
    发明申请
    CASPASE-TRIGGERED NANO-AGGREGATION PROBES AND METHODS OF USE 有权
    CASPASE-TRIGGERED NANO-AgGREGATION PROBES AND METHODS OF USE

    公开(公告)号：US20150056137A1

    公开(公告)日：2015-02-26

    申请号：US14464111

    申请日：2014-08-20

    申请人： The Board of Trustees of the Leland Stanford Junior University

    发明人： Jianghong Rao ,  Deju Ye ,  Adam Shuhendler ,  Frederick Te-Ning Chin ,  Jongho Jeon ,  Bin Shen

    IPC分类号： A61K51/08 ,  A61K49/08 ,  G01N33/52 ,  A61K49/00

    CPC分类号： A61K49/0002 ,  A61K49/0021 ,  A61K49/0032 ,  A61K49/0041 ,  A61K49/0052 ,  A61K49/085 ,  A61K49/101 ,  A61K51/0455 ,  G01N33/5005 ,  G01N2333/96469 ,  G01N2510/00

    摘要： Provided is an activatable probe that undergoes intramolecular cyclization and subsequent aggregation in apoptotic tumor cells upon peptidase-initiated, and most advantageously caspase-3, activation. These caspase-sensitive nano-aggregation probes (C-SNAFs) are generally biocompatible, possess NIR spectral properties or may serve as PET or MRI imaging agents, and have a mechanism of target-mediated nanostructure self-assembly amenable to in vivo use. The probes encompass biocompatible condensation chemistry products that comprise D-cysteine and 2-cyano-6-hydroxyquinoline (CHQ) moieties linked to an amino-luciferin scaffold, and which can be activated by a two-step reaction requiring caspase-3/7-mediated cleavage of an aspartate-glutamate-valine-aspartate (L-DEVD) capping peptide and the free intracellular thiol-mediated reduction of the disulfide bond.

    摘要翻译： 提供了一种可激活的探针，其在肽酶引发，最有利的是胱天蛋白酶-3激活时，经历分子内环化和随后在凋亡性肿瘤细胞中的聚集。 这些胱天蛋白酶敏感的纳米聚集探针（C-SNAF）通常是生物相容性的，具有NIR光谱性质或可以用作PET或MRI成像剂，并且具有适于体内使用的靶向介导的纳米结构自组装的机制。 探针包括与氨基荧光素支架连接的D-半胱氨酸和2-氰基-6-羟基喹啉（CHQ）部分的生物相容性缩合化学产物，其可以通过需要半胱天冬酶-3 / 7- 介导的天冬氨酸 - 谷氨酸 - 缬氨酸 - 天冬氨酸（L-DEVD）封端肽的切割和游离的细胞内硫醇介导的二硫键的还原。

    CYSTINE KNOT PEPTIDES THAT BIND ALPHA-V-BETA-6 INTEGRIN
    5.
    发明申请
    CYSTINE KNOT PEPTIDES THAT BIND ALPHA-V-BETA-6 INTEGRIN 有权
    氨基酸-β-6整合的CYSTINE KNOT PEPTIDES

    公开(公告)号：US20140271469A1

    公开(公告)日：2014-09-18

    申请号：US14283830

    申请日：2014-05-21

    申请人： The Board of Trustees of the Leland Stanford Junior University

    发明人： Richard H. Kimura ,  Sanjiv S. Gambhir ,  Benjamin J. Hackel ,  Robert Teed ,  Bin Shen ,  Frederick T Chin ,  Zhen Cheng

    IPC分类号： C07K14/00 ,  G01N33/574 ,  A61K51/08

    CPC分类号： C07K14/001 ,  A61K51/088 ,  G01N33/574 ,  G01N33/57492 ,  G01N33/6863 ,  G01N2333/70546

    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.

    摘要翻译： 公开了包含分子支架部分和结合整联蛋白αv＆bgr的环部分的肽6。 这种整合素在胰腺肿瘤中表达，使得肽可用作成像剂，以及其他用途。 这些肽显示出与临床上用于成像和治疗的抗体相似的单位纳摩尔解离常数。 肽在6个阳性的肿瘤中迅速积累，导致肿瘤与正常的对比。 这些肽对于在原位胰腺肿瘤和各种​​异种移植物上表达的靶向整合素αv和bgr 6受体是特异性的。 此外，药代动力学稳定化策略赋予了快速肾清除的结，这显着降低了靶外给药。