RATIOMETRIC ASSAY FOR HYDROLYTIC ENZYME QUANTIFICATION
    91.
    发明申请
    RATIOMETRIC ASSAY FOR HYDROLYTIC ENZYME QUANTIFICATION 审中-公开
    水解酶的定量测定

    公开(公告)号:US20160139137A1

    公开(公告)日:2016-05-19

    申请号:US14900133

    申请日:2014-06-23

    Abstract: The invention refers to a nanoparticle comprising (i) a core comprising a first population of quantum dots (QDs) embedded in silica, (ii) a shell comprising a second population of QDs embedded in silica, (iii) at least one biomolecule selected from a peptide, a nucleic acid, a carbohydrate or a lipid which comprises a cleavage site that is susceptible of being cleaved by a hydrolytic enzyme, said biomolecule being bound to the surface of the shell through a moiety, and (iv) a photoluminescent label for each biomolecule, wherein the label is bound to the part of the biomolecule which detaches from the nanoparticle after cleavage of said biomolecule by a hydrolytic enzyme, wherein the first and second QD populations have different maximum photoluminescence emission wavelengths, and only the second QD population is susceptible of producing Forster resonance energy transfer (FRET) with the photoluminescent label.

    Abstract translation: 本发明涉及一种纳米颗粒,其包含(i)包含嵌入二氧化硅中的第一批量子点(QD)的核心,(ii)包含埋在二氧化硅中的第二组质子数量的壳体,(iii)至少一种选自以下的生物分子: 肽,核酸,碳水化合物或脂质,其包含易于被水解酶切割的切割位点,所述生物分子通过部分结合到壳的表面,和(iv)光致发光标记,用于 每个生物分子,其中所述标记与所述生物分子的部分结合,所述部分在通过水解酶切割所述生物分子之后与所述纳米颗粒分离,其中所述第一和第二QD群体具有不同的最大光致发光发射波长,并且仅第二QD群体 容易产生与光致发光标签的福斯特共振能量转移(FRET)。

    Protein structural biomarkers to guide targeted chemotherapies
    92.
    发明授权
    Protein structural biomarkers to guide targeted chemotherapies 有权
    蛋白质结构生物标志物来指导靶向化疗

    公开(公告)号:US09341627B2

    公开(公告)日:2016-05-17

    申请号:US13202131

    申请日:2010-02-19

    Applicant: Sunyoung Kim

    Inventor: Sunyoung Kim

    Abstract: A rapid, infrared spectroscopic method has been developed to assess the efficacy of targeted chemotherapeutics against the structure of the polypeptide target, based on the effect of natural polymorphic sequence variation on the conformation of the protein. This method has an advantage over the current genomics-based screening, as the new method provides a direct readout of the structural, and hence functional, outcome of polymorphisms to the protein region targeted by drugs. It allows rapid measurement of a protein's susceptibility to therapeutic targeted agents, prior to using the drug as treatment in the patient. This method can be used to identify biomarkers for a response for a protein to a drug which can be readily tested, interpreted, and used in a clinical setting.

    Abstract translation: 基于天然多态性序列变异对蛋白质构象的影响,开发了一种快速的红外光谱方法,以评估靶向化学治疗剂对多肽靶结构的功效。 该方法相对于目前基于基因组学的筛选具有优势,因为新方法提供了针对药物的蛋白质区域的多态性的结构,从而功能性的结果的直接读出。 在使用药物作为患者的治疗之前,它可以快速测量蛋白质对治疗性靶向药物的敏感性。 该方法可用于鉴定蛋白质对药物的响应的生物标志物,其可以容易地在临床环境中测试,解释和使用。

    AMINOHETEROARYL COMPOUNDS AS MTH1 INHIBITORS
    94.
    发明申请
    AMINOHETEROARYL COMPOUNDS AS MTH1 INHIBITORS 有权
    AMINOHETEROARYL化合物作为MTH1抑制剂

    公开(公告)号:US20160015702A1

    公开(公告)日:2016-01-21

    申请号:US14424595

    申请日:2013-08-27

    Abstract: The present invention relates to an (S)-enantiomer of an aminoheteroaryl compound for use in treating and/or preventing cancer in a subject. The invention further relates to a pharmaceutical composition comprising said compound. Another aspect of the invention is directed to an in vitro method for determining the effectiveness of said (S)-enantiomer of an aminoheteroaryl compound, or said pharmaceutical composition, the method comprising the steps of: (a) obtaining a cell or tissue sample from a subject; and (b) determining the subject's NUDT1/MTH1-status; wherein a NUDT1/MTH1-positive cell or tissue sample is indicative of an effective treatment and/or prevention of cancer. In addition, provided herein is a screening method for identifying a target of an (S)-enantiomer of an aminoheteroaryl compound. Furthermore, in context of this invention, the herein described compounds inhibit the biological activity of MTH1.

    Abstract translation: 本发明涉及用于治疗和/或预防受试者癌症的氨基杂芳基化合物的(S) - 对映异构体。 本发明还涉及包含所述化合物的药物组合物。 本发明的另一方面涉及用于测定氨基杂芳基化合物或所述药物组合物的所述(S) - 对映异构体的有效性的体外方法,所述方法包括以下步骤:(a)获得细胞或组织样品, 课程; 和(b)确定受试者的NUDT1 / MTH1状态; 其中NUDT1 / MTH1阳性细胞或组织样品指示有效治疗和/或预防癌症。 此外,本文提供了用于鉴定氨基杂芳基化合物的(S) - 对映异构体的靶标的筛选方法。 此外,在本发明的上下文中,本文所述的化合物抑制MTH1的生物活性。

    COMPETITION BASED-DETECTION ASSAYS
    95.
    发明申请
    COMPETITION BASED-DETECTION ASSAYS 有权
    基于竞争的检测测定

    公开(公告)号:US20150338410A1

    公开(公告)日:2015-11-26

    申请号:US14729498

    申请日:2015-06-03

    Abstract: Disclosed herein are methods and kits which are useful for detecting presence of an enzyme and the relative amount of glycan associated with the enzyme in a test sample based upon the enzyme's ability to competitively inhibit the binding of a ligand in such test sample. The present invention provides the ability to evaluate cell culture conditions and optimize the desired glycoform content of recombinantly prepared enzymes.

    Abstract translation: 本文公开了可用于检测酶的存在和测试样品中与酶相关的聚糖的相对量的方法和试剂盒,其基于酶在竞争性抑制配体在该测试样品中结合的能力。 本发明提供了评估细胞培养条件并优化重组制备的酶的所需糖型含量的能力。

    Competition-based detection assays
    97.
    发明授权
    Competition-based detection assays 有权
    基于竞争的检测分析

    公开(公告)号:US09075057B2

    公开(公告)日:2015-07-07

    申请号:US14124979

    申请日:2012-06-08

    Abstract: Disclosed herein are methods and kits which are useful for detecting presence of an enzyme and the relative amount of glycan associated with the enzyme in a test sample based upon the enzyme's ability to competitively inhibit the binding of a ligand in such test sample. The present invention provides the ability to evaluate cell culture conditions and optimize the desired glycoform content of recombinantly prepared enzymes.

    Abstract translation: 本文公开了可用于检测酶的存在和测试样品中与酶相关的聚糖的相对量的方法和试剂盒,其基于酶在竞争性抑制配体在该测试样品中结合的能力。 本发明提供了评估细胞培养条件并优化重组制备的酶的所需糖型含量的能力。

    METHODS OF TREATING A MEIOTIC KINESIN-ASSOCIATED DISEASE
    99.
    发明申请
    METHODS OF TREATING A MEIOTIC KINESIN-ASSOCIATED DISEASE 有权
    治疗一种与生殖细胞相关的疾病的方法

    公开(公告)号:US20150111786A1

    公开(公告)日:2015-04-23

    申请号:US14591678

    申请日:2015-01-07

    Inventor: David Pellman

    Abstract: The invention provides methods of treating a meiotic kinase-associated disease, preferably the meiotic kinase HSET, by administering an inhibitor of the meiotic kinase. Preferably, the disease is associated with the presence of supernumerary centrosomes, such as cancer. Methods of inhibiting the growth of a tumor cell by contacting the cell with an inhibitor of a meiotic kinase, preferably HSET, are also provided. Screening methods for identifying inhibitors of the meiotic Kinase HSET are also provided. Methods of selecting subjects for treatment with an inhibitor of a meiotic kinase, such as HSET, are also provides.

    Abstract translation: 本发明提供了通过施用减数分裂激酶的抑制剂来治疗减数分裂激酶相关疾病,优选减数分裂激酶HSET的方法。 优选地,该疾病与诸如癌症的数量中心体的存在相关。 还提供了通过使细胞与减数分裂激酶抑制剂(优选HSET)接触来抑制肿瘤细胞生长的方法。 还提供了用于鉴定减数分裂激酶HSET的抑制剂的筛选方法。 还提供了选择用减数分裂激酶抑制剂如HSET治疗的受试者的方法。

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