Screening method for GPCR ligands
    11.
    发明授权
    Screening method for GPCR ligands 失效
    GPCR配体的筛选方法

    公开(公告)号:US08623606B2

    公开(公告)日:2014-01-07

    申请号:US12310296

    申请日:2007-08-09

    IPC分类号: G01N33/53 C07K14/705

    摘要: This invention relates to a method of identifying a compound capable of binding to a target domain of a G-protein coupled receptor comprising the steps of: (a) providing a receptor comprising said target domain and a first group linked to said target domain; (b) bringing into contact said receptor of (a) with a test molecule comprising a second group and said compound linked to each other, wherein said first group binds said second group; and (c) determining, subsequent to the binding of said first group to said second group, whether said compound binds to said target domain.

    摘要翻译: 本发明涉及鉴定能够结合G蛋白偶联受体的靶结构域的化合物的方法,包括以下步骤:(a)提供包含所述靶结构域和与所述靶结构域连接的第一基团的受体; (b)使(a)的所述受体与包含第二组的测试分子和彼此连接的所述化合物接触,其中所述第一组结合所述第二组; 和(c)在所述第一组与所述第二组的结合之后确定所述化合物是否结合所述靶结构域。

    RNA SEQUENCE-SPECIFIC MEDIATORS OF RNA INTERFERENCE
    12.
    发明申请
    RNA SEQUENCE-SPECIFIC MEDIATORS OF RNA INTERFERENCE 审中-公开
    RNA干扰RNA序列特异性介质

    公开(公告)号:US20130198875A1

    公开(公告)日:2013-08-01

    申请号:US13830751

    申请日:2013-03-14

    IPC分类号: C07H21/02

    摘要: The present invention relates to a Drosophila in vitro system which was used to demonstrate that dsRNA is processed to RNA segments 21-23 nucleotides (nt) in length. Furthermore, when these 21-23 nt fragments are purified and added back to Drosophila extracts, they mediate RNA interference in the absence of long dsRNA. Thus, these 21-23 nt fragments are the sequence-specific mediators of RNA degradation. A molecular signal, which may be their specific length, must he present in these 21-23 nt fragments to recruit cellular factors involved in RNAi. This present invention encompasses these 21-23 nt fragments and their use for specifically inactivating gene function. The use of these fragments (or chemically synthesized oligonucleotides of the same or similar nature) enables the targeting of specific mRNAs for degradation in mammalian cells, where the use of long dsRNAs to elicit RNAi is usually not practical, presumably because of the deleterious effects of the interferon response. This specific targeting of a particular gene function is useful in functional genomic and therapeutic applications.

    摘要翻译: 本发明涉及果蝇体外系统,其用于证明dsRNA被加工成长度为21-23个核苷酸(nt)的RNA片段。 此外,当这些21-23个片段被纯化并加回到果蝇提取物时,它们在不存在长dsRNA的情况下介导RNA干扰。 因此,这些21-23个片段是RNA降解的序列特异性介质。 必须在这21-23个nt片段中存在可能是其特异性长度的分子信号来招募涉及RNAi的细胞因子。 本发明包括这些21-23个片段及其用于特异性失活基因功能的用途。 使用这些片段(或具有相同或相似性质的化学合成的寡核苷酸)使得能够靶向用于哺乳动物细胞降解的特异性mRNA,其中使用长dsRNA引发RNAi通常是不实际的,可能是因为有害影响 干扰素反应。 特定基因功能的特异性靶向在功能基因组和治疗应用中是有用的。

    ENZYME-CONTAINING MINI-EMULSIONS
    13.
    发明申请
    ENZYME-CONTAINING MINI-EMULSIONS 有权
    含酶的微乳液

    公开(公告)号:US20130196395A1

    公开(公告)日:2013-08-01

    申请号:US13802862

    申请日:2013-03-14

    IPC分类号: C12P7/62

    摘要: The present invention relates to a mini-emulsion which comprises at least one hydrolase, where the continuous phase of the mini-emulsion contains at least one oxidant, while the dispersed phase comprises at least one C6-60 carboxylic acid and optionally at least one reactant. Furthermore, the present invention relates to a method of preparing the mini-emulsion and to a process for the preparation of C6-60 percarboxylic acids and to a process for the preparation of an oxidized reactant, in each case using the abovementioned mini-emulsions.

    摘要翻译: 本发明涉及一种微乳液,其包含至少一种水解酶,其中微乳液的连续相含有至少一种氧化剂,而分散相包含至少一种C6-60羧酸和任选的至少一种反应物 。 此外,本发明涉及制备微乳液的方法和制备C6-60过羧酸的方法以及制备氧化反应物的方法,每种情况都使用上述微型乳液。

    MZB1, A NOVEL B CELL FACTOR, AND USES THEREOF
    14.
    发明申请
    MZB1, A NOVEL B CELL FACTOR, AND USES THEREOF 审中-公开
    MZB1,新型B细胞因子及其用途

    公开(公告)号:US20130189266A1

    公开(公告)日:2013-07-25

    申请号:US13740772

    申请日:2013-01-14

    IPC分类号: C07K16/18

    摘要: The marginal zone (MZ) and B1 subsets of B cells, which differ from conventional follicular (FO) B cells both developmentally and functionally, are involved in early responses to infectious pathogens and the production of self-reactive antibodies. A novel gene, mzb1, is expressed at high levels in MZ and B1 B cells but at low level, if at all, in FO B cells. MZB1 is involved in the regulation of proliferation, BCR-mediated signal transduction, and antibody production in B cells. Inhibitors, activators and enhancers of MZB1 expression or activity can be used as immune modulators for research and therapeutic purposes.

    摘要翻译: 与发育和功能上的常规卵泡(FO)B细胞不同的B细胞的边缘区(MZ)和B1亚群参与对感染性病原体的早期应答和自身反应性抗体的产生。 一种新型基因mzb1在MZ和B1B细胞中以高水平表达,但在FO B细胞中表达较低水平(如果有的话)。 MZB1参与B细胞增殖,BCR介导的信号转导和抗体产生的调控。 MZB1表达或活性的抑制剂,活化剂和增强剂可用作研究和治疗目的的免疫调节剂。

    Method for Separation of Racemic Compound-Forming Chiral Substances by a Cyclic-Crystallization Process and a Crystallization Device
    15.
    发明申请
    Method for Separation of Racemic Compound-Forming Chiral Substances by a Cyclic-Crystallization Process and a Crystallization Device 有权
    通过循环结晶法和结晶装置分离外消旋化合物形成的手性物质的方法

    公开(公告)号:US20130184489A2

    公开(公告)日:2013-07-18

    申请号:US13368638

    申请日:2012-02-08

    IPC分类号: C07B57/00 B01D9/04

    摘要: The invention concerns a method for separating a racemic compound-forming chiral substance by a cyclic crystallization process which is conducted in at least one first crystallization unit (10) and in at least one second crystallization unit (18), wherein in a first process cycle an enantiomer is crystallized in the first crystallization unit (10) and a racemic compound is crystallized in the second crystallization unit (18), wherein in a second process cycle the enantiomer is crystallized in the second crystallization unit (18) and the racemic compound is crystallized in the first crystallization unit (10), wherein during each process cycle in at least one process sub-step (B→C, F→G) a mother liquor (12) being contained in the first crystallization unit (10) is mutually exchanged with a mother liquor (20) being contained in the second crystallization unit (18). An auto-seeding process sub-step is applied at the beginning of a process cycle.

    摘要翻译: 本发明涉及通过在至少一个第一结晶单元(10)和至少一个第二结晶单元(18)中进行的循环结晶过程分离外消旋化合物形成手性物质的方法,其中在第一工艺循环 第一结晶单元(10)中的对映异构体结晶,外消旋化合物在第二结晶单元(18)中结晶,其中在第二工艺循环中,对映异构体在第二结晶单元(18)中结晶,外消旋化合物为 在第一结晶单元(10)中结晶的第一结晶单元(10)中的母液(12)在每个工艺循环期间在至少一个工艺子步骤(B-> C,F→G) 与包含在第二结晶单元(18)中的母液(20)相互交换。 自动播种过程子步骤在过程周期开始时被应用。

    COMPOSITIONS AND METHODS FOR MODULATING CIRCADIAN SYNCHRONIZATION
    19.
    发明申请
    COMPOSITIONS AND METHODS FOR MODULATING CIRCADIAN SYNCHRONIZATION 有权
    用于调制CIRCADIAN同步的组合物和方法

    公开(公告)号:US20120230978A1

    公开(公告)日:2012-09-13

    申请号:US13413907

    申请日:2012-03-07

    摘要: The present invention relates to a modulator of glucocorticoid biosynthesis, degradation and/or receptor activation for use in preventing or treating symptoms and/or diseases associated with jet lag. The compositions of the invention may be used as a lead compound for developing a drug for preventing or treating symptoms and/or diseases associated with jet lag. The invention relates to the discovery that administration of the modulator(s) to a subject results in a directional change of the time point of maximum amounts of glucocorticoids in the subject as compared to the time point of maximum amounts of glucocorticoids in a subject not treated with the modulator(s).

    摘要翻译: 本发明涉及用于预防或治疗与时差相关的症状和/或疾病的糖皮质激素生物合成,降解和/或受体活化的调节剂。 本发明的组合物可用作开发用于预防或治疗与时差相关的症状和/或疾病的药物的铅化合物。 本发明涉及以下发现:相对于未经治疗的受试者中最大量的糖皮质激素的时间点,向受试者施用调节剂导致受试者中最大量糖皮质激素的时间点的定向改变 与调制器。

    Method of treating depression
    20.
    发明授权
    Method of treating depression 有权
    治疗抑郁症的方法

    公开(公告)号:US08153127B2

    公开(公告)日:2012-04-10

    申请号:US12278023

    申请日:2007-02-07

    摘要: The present invention relates to a method for identifying a TMEFF2 modulator, comprising (a) contacting a cell which expresses TMEFF2 with a candidate compound to be tested; (b) measuring whether said compound to be tested decreases or increases the level of a constituent of the cAMP signalling pathway, preferably the CRH signalling pathway, in said cell when compared to a corresponding cell which does not express TMEFF2; (b′) optionally determining whether said compound is capable of reduncing the binding between Activin and TMEFF2; and (c) identifying said modulator compound. Furthermore, a method for identifying a TMEFF2 modulator comprising determining whether said TMEFF2 modulator is capable of reducing the binding between Activin and TMEFF2 is contemplated. It also relates to uses and methods applying a TMEFF2 agonist for the treatment of Cushing's Syndromes and a TMEFF2 modulator for the treatment of affective disorders. Furthermore, methods of diagnosing affective disorders or Cushing's Syndromes are provided.

    摘要翻译: 本发明涉及鉴定TMEFF2调节剂的方法,其包括(a)使表达TMEFF2的细胞与待测试的候选化合物接触; (b)当与不表达TMEFF2的相应细胞相比时,测量所述待测化合物是否降低或增加所述细胞中cAMP信号传导途径(优选CRH信号传导途径)的成分的水平; (b')任选地确定所述化合物是否能够重新激活激活素和TMEFF2之间的结合; 和(c)鉴定所述调节剂化合物。 此外,考虑了用于鉴定TMEFF2调节剂的方法,其包括确定所述TMEFF2调节剂是否能够降低活化素和TMEFF2之间的结合。 它还涉及应用TMEFF2激动剂治疗库兴综合征和用于治疗情感障碍的TMEFF2调节剂的用途和方法。 此外,提供了诊断情感障碍或库兴氏综合征的方法。