COMPOSITIONS AND METHODS FOR ENHANCING ODORANT RECEPTOR ACTIVITY
    3.
    发明申请
    COMPOSITIONS AND METHODS FOR ENHANCING ODORANT RECEPTOR ACTIVITY 审中-公开
    用于增强气味受体活性的组合物和方法

    公开(公告)号:WO2011069156A3

    公开(公告)日:2011-08-11

    申请号:PCT/US2010059093

    申请日:2010-12-06

    CPC classification number: C12Q1/6881 C07K14/70571 C12Q2600/136 C12Q2600/156

    Abstract: The present invention relates to polypeptides capable of modulating odorant receptor activation. In particular, the present invention provides polypeptides (e.g., type 3 muscarinic actetylcholine receptor M3) capable of enhancing odorant receptor activation. The present invention further provides assays for the detection of ligands specific for various odorant receptors. Additionally, the present invention provides methods of screening for polypeptide polymorphisms and mutations associated with odorant receptor activation (e.g., polymorphisms and mutations associated with muscarinic actetylcholine receptor polypeptides (e.g., M1, M2, M3, M4, M5)), as well as methods of screening for therapeutic agents, ligands, and modulators of such proteins.

    Abstract translation: 本发明涉及能够调节气味受体活化的多肽。 特别地,本发明提供能够增强加味剂受体活化的多肽(例如,3型毒蕈碱性乙酰胆碱受体M3)。 本发明还提供了检测各种加臭剂受体特异性配体的测定法。 此外,本发明提供了筛选多肽多态性和与气味受体激活相关的突变的方法(例如,与毒蕈碱性乙酰胆碱受体多肽(例如,M1,M2,M3,M4,M5)相关的多态性和突变)以及方法 筛选这些蛋白质的治疗剂,配体和调节剂。

    NOVEL STEROID 5 α -REDUCTASE
    7.
    发明申请
    NOVEL STEROID 5 α -REDUCTASE 审中-公开
    NOVEL STEROID 5 a -REDUCTASE

    公开(公告)号:WO2006122214A2

    公开(公告)日:2006-11-16

    申请号:PCT/US2006/018147

    申请日:2006-05-10

    Abstract: The invention provides an isolated, novel steroid 5α-reductase enzyme termed SRD5AIIL The protein has an estimated molecular weight of 37 kDa and is capable of converting testosterone to dihydrotestosterone at a pH of about 7.0. Also provided is a method for identifying inhibitors of SRD5 AIII by contacting SRD5 AIII with a test compound and measuring the activity of the enzyme. A reduced activity relative to a control indicates that the test compound is an inhibitor of SRD5AIII. A method is also provided for detecting androgen stimulated prostate cancer or recurrent prostate cancer in an individual. The method comprises obtaining a prostate biopsy from an individual and determining the level of expression of SRD5ADI gene or protein relative to a normal control. An increased expression of SRD5AIII relative to the control is indicative of androgen stimulated prostate cancer or recurrent prostate cancer.

    Abstract translation: 本发明提供了一种称为SRD5AIIL的分离的新型类固醇5a-还原酶。该蛋白质具有37kDa的估计分子量,并且能够在约7.0的pH下将睾酮转化为二氢睾酮。 还提供了通过将SRD5AIII与测试化合物接触并测量酶的活性来鉴定SRD5AIII的抑制剂的方法。 相对于对照的降低的活性表明测试化合物是SRD5AIII的抑制剂。 还提供了用于检测个体中激素刺激的前列腺癌或复发性前列腺癌的方法。 该方法包括从个体获得前列腺活检,并确定SRD5ADI基因或蛋白质相对于正常对照的表达水平。 SRD5AIII相对于对照的增加的表达指示雄激素刺激的前列腺癌或复发性前列腺癌。

    FUSED PYRROLE DERIVATIVES AS PI3K INHIBITORS
    9.
    发明申请
    FUSED PYRROLE DERIVATIVES AS PI3K INHIBITORS 审中-公开
    作为PI3K抑制剂的FUSED PYRORO衍生物

    公开(公告)号:WO2011163195A1

    公开(公告)日:2011-12-29

    申请号:PCT/US2011/041202

    申请日:2011-06-21

    CPC classification number: C07D473/34 A61K31/52 C07D519/00

    Abstract: The present invention provides fused pyrrole derivatives of Formula (I) wherein V, W, X, Y, L, Q, Ar, Z, R 1 and R 6 are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.

    Abstract translation: 本发明提供式(I)的稠合吡咯衍生物,其中V,W,X,Y,L,Q,Ar,Z,R 1和R 6在本文中定义,其调节磷酸肌醇3-激酶(PI3K)的活性, 可用于治疗与PI3Ks的活性相关的疾病,包括例如炎性疾病,基于免疫的疾病,癌症和其它疾病。

    COMPOSITIONS AND METHODS FOR ENHANCING ODORANT RECEPTOR ACTIVITY
    10.
    发明申请
    COMPOSITIONS AND METHODS FOR ENHANCING ODORANT RECEPTOR ACTIVITY 审中-公开
    增强气味受体活性的组合物和方法

    公开(公告)号:WO2011069156A2

    公开(公告)日:2011-06-09

    申请号:PCT/US2010/059093

    申请日:2010-12-06

    CPC classification number: C12Q1/6881 C07K14/70571 C12Q2600/136 C12Q2600/156

    Abstract: The present invention relates to polypeptides capable of modulating odorant receptor activation. In particular, the present invention provides polypeptides (e.g., type 3 muscarinic actetylcholine receptor M3) capable of enhancing odorant receptor activation. The present invention further provides assays for the detection of ligands specific for various odorant receptors. Additionally, the present invention provides methods of screening for polypeptide polymorphisms and mutations associated with odorant receptor activation (e.g., polymorphisms and mutations associated with muscarinic actetylcholine receptor polypeptides (e.g., M1, M2, M3, M4, M5)), as well as methods of screening for therapeutic agents, ligands, and modulators of such proteins.

    Abstract translation: 本发明涉及能够调节气味受体活化的多肽。 特别地,本发明提供能够增强气味受体活化的多肽(例如,3型毒蕈碱乙酰胆碱受体M3)。 本发明进一步提供了用于检测对各种气味受体特异性的配体的测定。 另外,本发明提供了筛选与气味受体激活相关的多肽多态性和突变(例如,与毒蕈碱性乙酰胆碱受体多肽(例如M1,M2,M3,M4,M5)相关的多态性和突变)的方法,以及方法 筛选治疗剂,配体和这些蛋白质的调节剂。

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