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    CRFR1 SELECTIVE LIGANDS
    1.
    发明申请
    CRFR1 SELECTIVE LIGANDS 有权
    CRFR1选择性配偶

    公开(公告)号：US20090149629A1

    公开(公告)日：2009-06-11

    申请号：US12366816

    申请日：2009-02-06

    申请人： Jean E.F. Rivier ,  Wylie W. Vale, JR. ,  Marilyn H. Perrin ,  Jozsef Gulyas

    发明人： Jean E.F. Rivier ,  Wylie W. Vale, JR. ,  Marilyn H. Perrin ,  Jozsef Gulyas

    IPC分类号： C07K14/47

    CPC分类号： C07K14/47 ,  A61K38/00 ,  C07K14/57509

    摘要： CRF peptide analogs that bind to CRFR1 with an affinity far greater than they bind to CRFR2. Some of these analogs exhibit CRF agonist activity. One exemplary analog that may be made by solid-phase synthesis is:(cyclo 31-34)[Ac-Pro4, D-Phe12, Nle18,21, Glu31, Lys34]-sucker urotensin(4-41).

    摘要翻译： 结合CRFR1的CRF肽类似物的亲和力远远大于它们与CRFR2结合的亲和力。 这些类似物中的一些表现出CRF激动剂活性。 可以通过固相合成制备的一个示例性类似物是：（环31-34）[Ac-Pro4，D-Phe12，Nle18,21，Glu31，Lys34]刺激性尿素转运蛋白（4-41）。

    UROCORTIN-III AND USES THEREOF
    2.
    发明申请
    UROCORTIN-III AND USES THEREOF 有权
    胭脂红III及其用途

    公开(公告)号：US20120270792A1

    公开(公告)日：2012-10-25

    申请号：US13328821

    申请日：2011-12-16

    申请人： Wylie W. Vale, JR. ,  Kathy A. Lewis ,  Marilyn H. Perrin ,  Koichi S. Kunitake ,  Jean E. Rivier ,  Jozsef Gulyas

    发明人： Wylie W. Vale, JR. ,  Kathy A. Lewis ,  Marilyn H. Perrin ,  Koichi S. Kunitake ,  Jean E. Rivier ,  Jozsef Gulyas

    IPC分类号： A61K38/02 ,  A61P9/00

    CPC分类号： A61K38/2228 ,  A61K38/00 ,  C07K14/57509 ,  C07K14/695

    摘要： A search of the public human genome database identified a human EST, GenBank accession number AW293249, which has high homology to known pufferfish urocortin sequences. The full length sequence was amplified from human genomic DNA and sequenced. Sequence homology comparisons of the novel sequence with human urocortin I and urocortin II revealed that the sequence encoded a novel human urocortin, which was designated urocortin III (UcnIII). While urocortin III does not have high affinity for either CRF-R1 or CRF-R2, the affinity for CRF-R2 is greater than the affinity for CRF-R1. Urocortin III is capable stimulating cyclic AMP production in cells expressing CRF-R2α or β. Thus, the affinity is high enough that urocortin III could act as a native agonist of CRF-R2. However, it is also likely that urocortin III is a stronger agonist of a yet to be identified receptor.

    摘要翻译： 公众人类基因组数据库的搜索确定了人类EST，GenBank登录号AW293249，其与已知的河豚urocortin序列具有高同源性。 从人类基因组DNA扩增全长序列并进行测序。 新序列与人尿皮质素I和尿皮质素II的序列同源性比较显示，该序列编码了一种新的人类urocortin，其命名为urocortin III（UcnIII）。 虽然urocortin III对CRF-R1或CRF-R2没有高亲和力，但CRF-R2的亲和力大于对CRF-R1的亲和力。 Urocortin III能够刺激表达CRF-R2α或bgr的细胞中的环AMP产生。 因此，亲和力足够高，使得尿皮质素III可以作为CRF-R2的天然激动剂。 然而，urocortin III也可能是未被鉴定的受体的更强的激动剂。

    CRFR1 selective ligands
    3.
    发明授权
    CRFR1 selective ligands 有权
    CRFR1选择性配体

    公开(公告)号：US07851588B2

    公开(公告)日：2010-12-14

    申请号：US12366816

    申请日：2009-02-06

    申请人： Jean E. F. Rivier ,  Wylie W. Vale, Jr. ,  Marilyn H. Perrin ,  Jozsef Gulyas

    发明人： Jean E. F. Rivier ,  Wylie W. Vale, Jr. ,  Marilyn H. Perrin ,  Jozsef Gulyas

    IPC分类号： A61K38/12

    CPC分类号： C07K14/47 ,  A61K38/00 ,  C07K14/57509

    摘要： CRF peptide analogs that bind to CRFR1 with an affinity far greater than they bind to CRFR2. Some of these analogs exhibit CRF agonist activity. One exemplary analog that may be made by solid-phase synthesis is:(cyclo 31-34)[Ac-Pro4,D-Phe12,Nle18,21,Glu31,Lys34]-sucker urotensin(4-41).

    摘要翻译： 结合CRFR1的CRF肽类似物的亲和力远远大于它们与CRFR2结合的亲和力。 这些类似物中的一些表现出CRF激动剂活性。 可以通过固相合成制备的一个示例性类似物是：（环31-34）[Ac-Pro4，D-Phe12，Nle18,21，Glu31，Lys34]刺激性尿素转运蛋白（4-41）。

    Urocortin-III and uses thereof
    4.
    发明授权
    Urocortin-III and uses thereof 有权
    Urocortin-III及其用途

    公开(公告)号：US08084413B2

    公开(公告)日：2011-12-27

    申请号：US12266430

    申请日：2008-11-06

    申请人： Wylie W. Vale, Jr. ,  Kathy A. Lewis ,  Marilyn H. Perrin ,  Koichi S. Kunitake ,  Jean E. Rivier ,  Jozsef Gulyas

    发明人： Wylie W. Vale, Jr. ,  Kathy A. Lewis ,  Marilyn H. Perrin ,  Koichi S. Kunitake ,  Jean E. Rivier ,  Jozsef Gulyas

    IPC分类号： C07K14/00

    CPC分类号： A61K38/2228 ,  A61K38/00 ,  C07K14/57509 ,  C07K14/695

    摘要： A search of the public human genome database identified a human EST, GenBank accession number AW293249, which has high homology to known pufferfish urocortin sequences. The full length sequence was amplified from human genomic DNA and sequenced. Sequence homology comparisons of the novel sequence with human urocortin I and urocortin II revealed that the sequence encoded a novel human urocortin, which was designated urocortin III (UcnIII). While urocortin III does not have high affinity for either CRF-R1 or CRF-R2, the affinity for CRF-R2 is greater than the affinity for CRF-R1. Urocortin III is capable stimulating cyclic AMP production in cells expressing CRF-R2α or β. Thus, the affinity is high enough that urocortin III could act as a native agonist of CRF-R2. However, it is also likely that urocortin III is a stronger agonist of a yet to be identified receptor.

    摘要翻译： 公众人类基因组数据库的搜索确定了人类EST，GenBank登录号AW293249，其与已知的河豚urocortin序列具有高同源性。 从人类基因组DNA扩增全长序列并进行测序。 新序列与人尿皮质素I和尿皮质素II的序列同源性比较显示，该序列编码了一种新的人类urocortin，其命名为urocortin III（UcnIII）。 虽然urocortin III对CRF-R1或CRF-R2没有高亲和力，但CRF-R2的亲和力大于对CRF-R1的亲和力。 Urocortin III能够刺激表达CRF-R2α或bgr的细胞中的环AMP产生。 因此，亲和力足够高，使得尿皮质素III可以作为CRF-R2的天然激动剂。 然而，urocortin III也可能是未被鉴定的受体的更强的激动剂。

    UROCORTIN-III AND USES THEREOF
    6.
    发明申请
    UROCORTIN-III AND USES THEREOF 有权
    胭脂红III及其用途

    公开(公告)号：US20090156493A1

    公开(公告)日：2009-06-18

    申请号：US12266430

    申请日：2008-11-06

    申请人： Wylie W. Vale, JR. ,  Kathy A. Lewis ,  Marilyn H. Perrin ,  Koichi S. Kunitake ,  Jean E. Rivier ,  Jozsef Gulyas

    发明人： Wylie W. Vale, JR. ,  Kathy A. Lewis ,  Marilyn H. Perrin ,  Koichi S. Kunitake ,  Jean E. Rivier ,  Jozsef Gulyas

    IPC分类号： A61K38/17 ,  C07K14/47

    CPC分类号： A61K38/2228 ,  A61K38/00 ,  C07K14/57509 ,  C07K14/695

    摘要： A search of the public human genome database identified a human EST, GenBank accession number AW293249, which has high homology to known pufferfish urocortin sequences. The full length sequence was amplified from human genomic DNA and sequenced. Sequence homology comparisons of the novel sequence with human urocortin I and urocortin II revealed that the sequence encoded a novel human urocortin, which was designated urocortin III (UcnIII). While urocortin III does not have high affinity for either CRF-R1 or CRF-R2, the affinity for CRF-R2 is greater than the affinity for CRF-R1. Urocortin III is capable stimulating cyclic AMP production in cells expressing CRF-R2α or β. Thus, the affinity is high enough that urocortin III could act as a native agonist of CRF-R2. However, it is also likely that urocortin III is a stronger agonist of a yet to be identified receptor.

    摘要翻译： 公众人类基因组数据库的搜索确定了人类EST，GenBank登录号AW293249，其与已知的河豚urocortin序列具有高同源性。 从人类基因组DNA扩增全长序列并进行测序。 新序列与人尿皮质素I和尿皮质素II的序列同源性比较显示，该序列编码了一种新的人类urocortin，其命名为urocortin III（UcnIII）。 虽然urocortin III对CRF-R1或CRF-R2没有高亲和力，但CRF-R2的亲和力大于对CRF-R1的亲和力。 Urocortin III能够刺激表达CRF-R2alpha或β的细胞中的环AMP产生。 因此，亲和力足够高，使得尿皮质素III可以作为CRF-R2的天然激动剂。 然而，urocortin III也可能是未被鉴定的受体的更强的激动剂。

    Urocortin-III and uses thereof
    7.
    发明授权
    Urocortin-III and uses thereof 有权
    Urocortin-III及其用途

    公开(公告)号：US07459427B2

    公开(公告)日：2008-12-02

    申请号：US11214371

    申请日：2005-08-29

    申请人： Wylie W. Vale, Jr. ,  Kathy A. Lewis ,  Marilyn H. Perrin ,  Koichi S. Kunitake ,  Jean E. Rivier ,  Jozsef Gulyas

    发明人： Wylie W. Vale, Jr. ,  Kathy A. Lewis ,  Marilyn H. Perrin ,  Koichi S. Kunitake ,  Jean E. Rivier ,  Jozsef Gulyas

    IPC分类号： C07K14/00

    CPC分类号： A61K38/2228 ,  A61K38/00 ,  C07K14/57509 ,  C07K14/695

    摘要： A search of the public human genome database identified a human EST, GenBank accession number AW293249, which has high homology to known pufferfish urocortin sequences. The full length sequence was amplified from human genomic DNA and sequenced. Sequence homology comparisons of the novel sequence with human urocortin I and urocortin II revealed that the sequence encoded a novel human urocortin, which was designated urocortin III (UcnIII). While urocortin III does not have high affinity for either CRF-R1 or CRF-R2, the affinity for CRF-R2 is greater than the affinity for CRF-R1. Urocortin III is capable stimulating cyclic AMP production in cells expressing CRF-R2α or β. Thus, the affinity is high enough that urocortin III could act as a native agonist of CRF-R2. However, it is also likely that urocortin III is a stronger agonist of a yet to be identified receptor.

    摘要翻译： 公众人类基因组数据库的搜索确定了人类EST，GenBank登录号AW293249，其与已知的河豚urocortin序列具有高同源性。 从人类基因组DNA扩增全长序列并进行测序。 新序列与人尿皮质素I和尿皮质素II的序列同源性比较显示，该序列编码了一种新的人类urocortin，其命名为urocortin III（UcnIII）。 虽然urocortin III对CRF-R1或CRF-R2没有高亲和力，但CRF-R2的亲和力大于对CRF-R1的亲和力。 Urocortin III能够刺激表达CRF-R2alpha或β的细胞中的环AMP产生。 因此，亲和力足够高，使得尿皮质素III可以作为CRF-R2的天然激动剂。 然而，urocortin III也可能是未被鉴定的受体的更强的激动剂。