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    ENDOTHELIAL NITRIC OXIDE SYNTHASE
    3.
    发明申请
    ENDOTHELIAL NITRIC OXIDE SYNTHASE 审中-公开
    内氧化氮氧化物合成酶

    公开(公告)号：US20150232576A1

    公开(公告)日：2015-08-20

    申请号：US14672642

    申请日：2015-03-30

    申请人： John C. Salerno ,  Carol A. Chrestensen

    发明人： John C. Salerno ,  Carol A. Chrestensen

    IPC分类号： C07K16/40 ,  G01N33/573

    CPC分类号： C07K16/40 ,  C07K2317/24 ,  C07K2317/54 ,  C07K2317/55 ,  C07K2317/622 ,  C12N9/0075 ,  C12N9/99 ,  C12Y114/13039 ,  G01N33/573 ,  G01N2333/90254 ,  G01N2440/14

    摘要： Endothelial nitric oxide synthase (eNOS) activity was modulated by contact with an effective amount of a mitogen-activated protein (MAP) kinase, resulting in phosphorylation of S602, T46, and/or S58. Kinetics and stoichiometry are disclosed. The contact strongly reduced nitric oxide (NO) synthesis, and inhibited the cytochrome c reductase activity of eNOS reductase domains. Three sites of phosphorylation were determined that matched the serine-proline (SP) and threonine-proline (TP) motifs of typical MAP kinase phosphorylation sites.

    摘要翻译： 通过与有效量的丝裂原活化蛋白（MAP）激酶接触调节内皮一氧化氮合酶（eNOS）活性，导致S602，T46和/或S58的磷酸化。 公开了动力学和化学计量。 接触强烈地减少一氧化氮（NO）合成，并抑制eNOS还原酶结构域的细胞色素c还原酶活性。 测定三个磷酸化位点，其与典型的MAP激酶磷酸化位点的丝氨酸 - 脯氨酸（SP）和苏氨酸 - 脯氨酸（TP）基序相匹配。

    ANTI-INFLAMMATORY FOOD PRODUCT
    4.
    发明申请
    ANTI-INFLAMMATORY FOOD PRODUCT 审中-公开
    抗炎食品

    公开(公告)号：US20140193369A1

    公开(公告)日：2014-07-10

    申请号：US13735547

    申请日：2013-01-07

    申请人： WHITEWAVE SERVICES, INC.

    发明人： Neal Allan Bringe

    IPC分类号： C12Q1/02 ,  G01N33/68 ,  G01N33/573

    CPC分类号： C12Q1/025 ,  G01N33/573 ,  G01N33/6863 ,  G01N33/6869 ,  G01N33/88 ,  G01N2333/525 ,  G01N2333/5412 ,  G01N2333/545 ,  G01N2333/90254 ,  G01N2800/7095

    摘要： According to some embodiments, a method selects one or more inflammatory markers to evaluate. The one or more inflammatory markers selected from the group consisting of iNOS, COX-2, TNF-alpha, NO, PGE2, IL-6, and IL-1β. The method determines a first expression level and a second expression level of the one or more inflammatory markers. The first expression level is associated with a positive control sample comprising a type of human macrophages. The second expression level is associated with a test sample obtained by exposing a food product to a digest, the type of human macrophages, and a pro-inflammatory compound. The method performs a comparison between the first expression level and the second expression level and designates the food product according to an anti-inflammatory standard based on the comparison.

    摘要翻译： 根据一些实施方案，一种方法选择一种或多种炎性标志物进行评估。 选自iNOS，COX-2，TNF-α，NO，PGE2，IL-6和IL-1和bgr的一种或多种炎性标志物。 该方法确定一种或多种炎性标志物的第一表达水平和第二表达水平。 第一表达水平与包含一种人类巨噬细胞的阳性对照样品相关。 第二表达水平与通过将食物暴露于消化物，人类巨噬细胞的类型和促炎症化合物而获得的测试样品相关联。 该方法在第一表达水平和第二表达水平之间进行比较，并且基于比较来指定根据抗炎标准的食品。

    Method for sustaining enos activity
    6.
    发明申请
    Method for sustaining enos activity 审中-公开
    维持enos活动的方法

    公开(公告)号：US20060127385A1

    公开(公告)日：2006-06-15

    申请号：US10537599

    申请日：2003-12-04

    申请人： Sibaji Sarkar ,  Jane Freedman ,  Sonia Varghese

    发明人： Sibaji Sarkar ,  Jane Freedman ,  Sonia Varghese

    IPC分类号： A61K38/54

    CPC分类号： G01N33/86 ,  A61K31/05 ,  A61K31/27 ,  C12Q1/26 ,  G01N2333/90254

    摘要： The present invention is directed to methods for sustaining eNOS activity to inhibit platelet aggregation, clot retraction, and enhance fibrinolysis. One embodiment of the invention provides methods of treating thrombosis by inhibiting the activity of the syk kinase. Another embodiment provides assays for the discovery of improved compounds to treat thrombosis, by screening for compounds which sustain eNOS activity. Yet another embodiment provides assays for the discovery of improved compounds to treat thrombosis, by identifying inhibitors of calpain and IIbIIIa by screening for compounds which act through calpain or IIbIIIa to sustain eNOS activity. Yet another embodiment provides for enhancing fibrinolysis, by inhibiting the activity of the syk kinase or calpain.

    摘要翻译： 本发明涉及维持eNOS活性以抑制血小板聚集，凝块缩回和增强纤维蛋白溶解的方法。 本发明的一个实施方案提供了通过抑制syk激酶的活性来治疗血栓形成的方法。 另一个实施方案提供了通过筛选维持eNOS活性的化合物来发现用于治疗血栓形成的改进化合物的测定。 另一个实施方案提供了通过筛选通过钙蛋白酶或IIbIIIa作用以维持eNOS活性的化合物来鉴定钙蛋白酶和IIbIIIa的抑制剂来发现治疗血栓形成的改进化合物的测定。 另一个实施方案通过抑制syk激酶或钙蛋白酶的活性来提供增强纤维蛋白溶解。

    Inhibitors of bacterial nitric oxide synthase, and related screening methods
    10.
    发明授权
    Inhibitors of bacterial nitric oxide synthase, and related screening methods 有权
    细菌一氧化氮合酶抑制剂及相关筛选方法

    公开(公告)号：US08709743B2

    公开(公告)日：2014-04-29

    申请号：US12808889

    申请日：2008-12-17

    申请人： Stephen J. Lippard ,  Lindsey E. McQuade ,  Evgeny A. Nudler

    发明人： Stephen J. Lippard ,  Lindsey E. McQuade ,  Evgeny A. Nudler

    IPC分类号： C12Q1/02

    CPC分类号： C12Q1/26 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C12Q1/025 ,  G01N2333/90254 ,  G01N2500/10

    摘要： The invention relates in part to compounds that act as highly nitric oxide (NO)-specific turn-on fluorescent probes. The present invention also relates to the use of these fluorescein-based sensors to screen selectively for inhibitors of bacterial nitric oxide synthase (bNOS). Compounds of the present invention readily detect nitric oxide produced in vivo. Therefore they can be used in an assay that measures NO production by bNOS. Using a sensor of the invention one can screen libraries of small molecules for inhibitors of bNOS.

    摘要翻译： 本发明部分地涉及作为高度一氧化氮（NO）特异性开启荧光探针的化合物。 本发明还涉及这些基于荧光素的传感器选择性筛选细菌一氧化氮合酶（bNOS）抑制剂的用途。 本发明的化合物容易检测体内产生的一氧化氮。 因此，它们可用于通过bNOS测量NO产生的测定。 使用本发明的传感器，可以筛选用于bNOS抑制剂的小分子的文库。