公开(公告)号：US20170037143A1

公开(公告)日：2017-02-09

申请号：US15304394

申请日：2015-04-17

Applicant: The Governors of the University of Alberta

Inventor： Todd MCMULLEN ,  Ana LOPEZ-CAMPISTROUS ,  David WILLIAMS

IPC: C07K16/30 ,  A61K45/06 ,  G01N33/68 ,  C12N15/113 ,  A61K31/7088 ,  A61K39/395 ,  A61K51/00

CPC classification number: C07K16/30 ,  A61K31/7088 ,  A61K39/39558 ,  A61K45/06 ,  A61K51/00 ,  C07K14/71 ,  C07K16/28 ,  C07K2317/76 ,  C12N15/1138 ,  C12N2310/14 ,  C12N2320/31 ,  C12N2320/32 ,  G01N33/6872 ,  G01N2333/4703 ,  G01N2333/71 ,  G01N2800/52

Abstract: The invention includes method, pharmaceutical compositions and uses thereof for treating patients with Papillary Thyroid Carcinoma (PTC) using a Platelet Derived Growth Factor Receptor Alpha (PDGFRA) inhibitor. The PDGFRA inhibitor is preferably an antibody specific to PDGFRA and causes an increase in the sensitivity level of PTC cells to radioiodine treatment. Moreover, the antibody can be used in combination with other PDGFRA inhibitors such as tyrosine kinase inhibitors and RNA interference molecules.

Abstract translation: 本发明包括使用血小板衍生生长因子受体α（PDGFRA）抑制剂治疗患有乳头状甲状腺癌（PTC）的患者的方法，药物组合物及其用途。 PDGFRA抑制剂优选是对PDGFRA特异性的抗体，并且导致PTC细胞对放射性碘治疗的敏感性水平的增加。 此外，抗体可以与其他PDGFRA抑制剂如酪氨酸激酶抑制剂和RNA干扰分子组合使用。

公开(公告)号：US20170023589A1

公开(公告)日：2017-01-26

申请号：US15204749

申请日：2016-07-07

Applicant: President and Fellows of Harvard College

Inventor： Michael CHOREV ,  Jose A. HALPERIN

IPC: G01N33/68

CPC classification number: G01N33/6893 ,  C07K14/70596 ,  C07K16/2896 ,  C07K16/44 ,  G01N33/564 ,  G01N33/6872 ,  G01N2333/70596 ,  G01N2440/00 ,  G01N2440/38 ,  G01N2800/042

Abstract: The present invention provides compounds that are surrogates of post-translationally modified proteins and uses thereof. Numerous diseases are associated with post-translationally modified proteins that are difficult to obtain in homogenous form and in quantities needed for immunization and use as convenient standards, calibrators, and/or reference compounds that facilitate the detection and analysis of endogenous post-translationally modified proteins. The surrogate compounds of the invention typically comprise antigenic epitopes (one of which carries a post-translational modification) that are tethered by a flexible and hydrophilic linker. The resulting compound behaves like a surrogate of the post-translationally modified protein because it preserves the character of the included antigens and allows recognition by specific antibodies targeting the individual antigens. The surrogate compounds may be prepared by covalently joining two or more polypeptide epitopes using one or more linkers, wherein at least one of the epitopes comprises a post-translational modification. In one aspect, the surrogate compounds of the invention comprise a C-terminal epitope and a glycated epitope of human CD59. The inventive methods allow quantification of the levels of glycated CD59 in the serum in human subjects, particularly those with diabetes or pre-diabetes. This technological platform of post-translationally modified protein surrogates can be applied to other diseases associated with post-translationally modified proteins (e.g., autoimmune diseases such as multiple sclerosis, rheumatoid arthritis, and systemic lupus erythematosus). In another aspect, the invention provides antibodies that bind specifically to the compounds of the invention and methods for producing such antibodies.

Abstract translation: 本发明提供了作为翻译后修饰的蛋白质的替代物的化合物及其用途。 许多疾病与翻译后修饰的蛋白质相关，其难以以均匀形式获得，并且以免疫和使用所需的量作为方便的标准品，校准物和/或参考化合物获得，其有助于内源性翻译后修饰的蛋白质的检测和分析 。 本发明的替代化合物通常包含被柔性和亲水接头连接的抗原表位（其中一个携带翻译后修饰）。 所得化合物表现为翻译后修饰的蛋白质的替代物，因为其保留所包含的抗原的特征，并允许通过针对各个抗原的特异性抗体进行识别。 替代化合物可以通过使用一种或多种接头共价连接两个或多个多肽表位来制备，其中至少一个表位包含翻译后修饰。 一方面，本发明的替代化合物包含人CD59的C-末端表位和糖基化表位。 本发明的方法允许定量人受试者，特别是糖尿病或前期糖尿病患者血清中糖基化CD59的水平。 翻译后修饰的蛋白质替代物的这种技术平台可以应用于与翻译后修饰的蛋白质（例如自身免疫性疾病如多发性硬化症，类风湿性关节炎和系统性红斑狼疮）相关的其它疾病。 另一方面，本发明提供了与本发明化合物特异性结合的抗体以及用于产生此类抗体的方法。

公开(公告)号：US20170016881A1

公开(公告)日：2017-01-19

申请号：US15104830

申请日：2013-12-16

Applicant: ATROGI AB

Inventor： Tore Bengtsson

IPC: G01N33/50 ,  G01N33/74 ,  A61K31/196

CPC classification number: G01N33/5023 ,  A61K31/196 ,  G01N33/5035 ,  G01N33/5044 ,  G01N33/6872 ,  G01N33/74 ,  G01N2800/042

Abstract: A method to identify a candidate compound for use in the treatment of a condition involving dysregulation of glucose homeostasis or of glucose uptake in a mammal, by identifying a candidate compound that causes an increase in translocation of GLUT without causing an increase in the production of cAMP. A kit for use in such a method. A method of treatment of a condition involving dysregulation of glucose homeostasis or of glucose uptake in a mammal and a compound for use in such a method.

Abstract translation: 通过鉴定导致GLUT易位增加而不引起cAMP生成增加的候选化合物，鉴定用于治疗涉及哺乳动物体内葡萄糖稳态或葡萄糖摄取失调的病症的候选化合物的方法 。 用于这种方法的试剂盒。 一种治疗涉及哺乳动物和用于这种方法的化合物的葡萄糖稳态或葡萄糖摄取失调的病症的方法。

公开(公告)号：US09545442B2

公开(公告)日：2017-01-17

申请号：US14815111

申请日：2015-07-31

Applicant: CytomX Therapeutics, Inc.

Inventor： Henry Bernard Lowman ,  Luc Roland Desnoyers ,  Shouchun Liu ,  James William West ,  Jason Gary Sagert ,  Olga Vasiljeva ,  Elizabeth-Edna Mary Menendez

IPC: C07K16/00 ,  C12P21/08 ,  A61K39/395 ,  C07K16/28 ,  A61K47/48 ,  A61K49/00 ,  C07K16/30 ,  G01N33/574 ,  A61K39/00

CPC classification number: A61K49/0058 ,  A61K39/3955 ,  A61K47/6803 ,  A61K47/6849 ,  A61K2039/505 ,  C07K16/2863 ,  C07K16/2866 ,  C07K16/30 ,  C07K2317/14 ,  C07K2317/24 ,  C07K2317/56 ,  C07K2317/90 ,  C07K2317/92 ,  C07K2317/94 ,  G01N33/57492 ,  G01N33/58 ,  G01N33/6872 ,  G01N2333/71

Abstract: The invention relates generally to activatable antibodies that include a masking moiety (MM), a cleavable moiety (CM), and an antibody (AB) that specifically binds to epidermal growth factor receptor (EGFR), and to methods of making and using these anti-EGFR activatable antibodies in a variety of therapeutic, diagnostic and prophylactic indications.

Abstract translation: 本发明一般涉及可激活的抗体，其包括特异性结合表皮生长因子受体（EGFR）的掩蔽部分（MM），可切割部分（CM）和抗体（AB），以及制备和使用这些抗体 -EGFR可激活的抗体在各种治疗，诊断和预防指征。

公开(公告)号：US20170010255A1

公开(公告)日：2017-01-12

申请号：US15276088

申请日：2016-09-26

Applicant: Alagu P. THIRUVENGADAM

Inventor： Alagu P. THIRUVENGADAM

IPC: G01N33/50

CPC classification number: G01N33/5041 ,  G01N33/5008 ,  G01N33/502 ,  G01N33/6872 ,  G01N2333/912 ,  G01N2333/91215 ,  G01N2800/304 ,  G01N2800/305

Abstract: The present invention provides methods to modulate key elements along the DAG signaling pathway as well as a diagnostic assay, device and methods of using the same to diagnose bipolar disorder (BD) and attention deficit hyperactivity disorder (ADHD). Methods to identify diagnostic markers and drug targets for BD and ADHD. Methods of identifying effective compounds responsible for membrane potentials and excitabilities influencing bipolar disorder (BD) and attention deficit hyperactivity disorder (ADHD). Methods of identifying an effective compound that modulates the activity of Ca2+/CaM enzyme and compounds involved in changing the K+ gradient across the plasma membrane thereby increasing or decreasing the membrane potential ratio (MPR™) values. The invention provides methods of identifying a compound that modulates the activity of PKC which is an important protein of the DAG signaling pathway. Methods of identifying a compound that modulates DAG and its related enzymes along the DAG signaling pathway are provided. These compounds decrease or increase the membrane potential ratio (MPR™) in BD and ADHD patients.

Abstract translation: 本发明提供了调节沿着DAG信号通路的关键元件的方法以及使用该方法诊断双相情感障碍（BD）和注意缺陷多动障碍（ADHD）的诊断测定，装置和方法。 识别BD和ADHD的诊断标志物和药物靶标的方法。 鉴定负责影响双相情感障碍（BD）和注意缺陷多动障碍（ADHD）的膜电位和兴奋性的有效化合物的方法。 鉴定调节Ca2 + / CaM酶的活性的有效化合物的方法和涉及改变跨越质膜的K +梯度的化合物，从而增加或降低膜电位比（MPR TM）值。 本发明提供了鉴定调节作为DAG信号通路的重要蛋白质的PKC的活性的化合物的方法。 提供了鉴定沿着DAG信号通路调节DAG及其相关酶的化合物的方法。 这些化合物降低或增加BD和ADHD患者的膜电位比（MPR™）。

公开(公告)号：US09540422B2

公开(公告)日：2017-01-10

申请号：US14993952

申请日：2016-01-12

Applicant: University of Washington ,  The UAB Research Foundation

Inventor： Jens H. Gundlach ,  Michael Niederweis ,  Thomas Z. Butler ,  Mikhail Pavlenok ,  Mark A. Troll ,  Suja Sukumaran

IPC: A61K39/04 ,  A61K39/02 ,  A61K39/00 ,  C07K14/35 ,  C12N13/00 ,  G01N33/68 ,  C12Q1/68 ,  G01N27/447 ,  G01N33/487

CPC classification number: C12Q1/6869 ,  A61K39/00 ,  A61K39/04 ,  C07K14/35 ,  C12N13/00 ,  G01N24/00 ,  G01N27/44704 ,  G01N27/44791 ,  G01N33/48721 ,  G01N33/6872 ,  C12Q2523/31 ,  C12Q2565/631

Abstract: Provided herein are Mycobacterium smegmatis porin nanopores, systems that comprise these nanopores, and methods of using and making these nanopores. Such nanopores may be wild-type MspA porins, mutant MspA porins, wild-type MspA paralog porins, wild-type MspA homolog porins, mutant MspA paralog porins, mutant MspA homolog porins, or single-chain Msp porins. Also provided are bacterial strains capable of inducible Msp porin expression.

Abstract translation: 本文提供了耻垢分枝杆菌孔蛋白纳米孔，包含这些纳米孔的体系，以及使用和制备这些纳米孔的方法。 这样的纳米孔可以是野生型MspA孔蛋白，突变MspA孔蛋白，野生型MspA旁系同源孔蛋白，野生型MspA同源孔蛋白，突变MspA旁系同源孔蛋白，突变MspA同源孔蛋白或单链Msp孔蛋白。 还提供能够诱导Msp孔蛋白表达的细菌菌株。

公开(公告)号：US20170003279A1

公开(公告)日：2017-01-05

申请号：US15106872

申请日：2014-12-19

Applicant: BASF SE

Inventor： Alexandre Nesterov ,  Ramani Kandasamy ,  Barbara Wedel ,  Vincent L Salgado

IPC: G01N33/50 ,  C07K14/435 ,  G01N33/68

CPC classification number: G01N33/5041 ,  C07K14/43581 ,  C12N2710/10041 ,  G01N33/5085 ,  G01N33/6872 ,  G01N2333/43552 ,  G01N2333/43573 ,  G01N2430/10

Abstract: The present invention relates to a screening method for determining whether or not a candidate compound is a modulator of an insect transient receptor potential V (TRPV) channel. The present invention further provides a method of insect control by applying to an insect-specific TRPV channel modulator determined by the screening method. The present invention further relates to an expression vector that includes a nucleic acid molecule coding for an insect TRPV channel. Also, the present invention relates to cell that includes the expression vector encoding a TRPV channel.

Abstract translation: 本发明涉及一种用于确定候选化合物是否为昆虫瞬态受体电位V（TRPV）通道的调节剂的筛选方法。 本发明还提供了通过应用于通过筛选方法测定的昆虫特异性TRPV通道调节剂的昆虫防治方法。 本发明还涉及包含编码昆虫TRPV通道的核酸分子的表达载体。 此外，本发明涉及包含编码TRPV通道的表达载体的细胞。

公开(公告)号：US09534036B2

公开(公告)日：2017-01-03

申请号：US14391849

申请日：2013-03-15

Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM) ,  Universite Paris Diderot—Paris 7 ,  Universite Paris 13—Paris Nord ,  Assistance Publique—Hopitaux de Paris

Inventor： Giuseppina Caligiuri ,  Antonino Nicoletti

IPC: C07K14/705 ,  G01N33/68 ,  G01N33/86 ,  G01N33/543

CPC classification number: G01N33/6872 ,  C07K14/70503 ,  G01N33/54313 ,  G01N33/6893 ,  G01N33/86 ,  G01N2333/70503 ,  G01N2800/226 ,  G01N2800/24 ,  G01N2800/52

Abstract: The present invention relates to various soluble forms of CD31, including a novel form which is shed by activated platelets and released into the circulation. Methods for detecting said soluble forms of CD31 are disclosed, as are methods of specifically 1 detecting said platelet-derived shed CD31 and the use of such methods as a diagnostic tool.

Abstract translation: 本发明涉及各种可溶形式的CD31，包括被活化的血小板脱落并释放到循环中的新型形式。 公开了用于检测所述可溶形式的CD31的方法，特别是1检测所述血小板衍生的脱落CD31的方法和使用诸如诊断工具的方法。

公开(公告)号：US09511075B2

公开(公告)日：2016-12-06

申请号：US12522444

申请日：2008-01-11

Applicant: J. Marc Simard

Inventor： J. Marc Simard

IPC: A61K31/64 ,  A61K31/57 ,  G01N33/68 ,  A61K31/121 ,  A61K39/395 ,  A61K31/427 ,  A61K31/565 ,  A61K38/00

CPC classification number: A61K31/57 ,  A61K31/427 ,  A61K31/565 ,  A61K38/00 ,  G01N33/6872

Abstract: The present invention concerns protection of an organ or tissue following an ischemic episode In particular aspects, the invention concerns organ preservation for transplantation, angina pectoris, kidney reperfusion injury, and so forth In specific embodiments, the organ is subjected to an inhibitor of an NCCa-ATP channel that is regulated by SUR1 Exemplary inhibitors include sulfonylurea compounds, such as glibenclamide, for example.

Abstract translation: 本发明涉及缺血发作后的器官或组织的保护。在特定方面，本发明涉及用于移植，心绞痛，肾脏再灌注损伤等的器官保存。在具体实施方案中，对器官进行NCCa抑制剂 由SUR1调节的-ATP通道示例性抑制剂包括磺酰脲化合物，例如格列本脲。

公开(公告)号：US09511011B2

公开(公告)日：2016-12-06

申请号：US14725383

申请日：2015-05-29

Applicant: SNU R&DB FOUNDATION

Inventor： Jin Ho Chung ,  So Min Kang ,  Young Mee Lee ,  Yeon Kyung Kim

IPC: A61K38/08 ,  A61K8/64 ,  A61K35/36 ,  A61Q19/02 ,  A61Q19/08 ,  C07K7/06 ,  G01N33/50 ,  G01N33/68

CPC classification number: A61K8/64 ,  A61Q19/02 ,  A61Q19/08 ,  C07K7/06 ,  G01N33/5008 ,  G01N33/502 ,  G01N33/6872 ,  G01N2333/705

Abstract: TRPV1 inhibitory peptides and a composition for skin-aging prevention and wrinkle improvement comprising the same as an active ingredient are described. The TRPV1 inhibitory peptide of the present subject matter inhibits the expressions of MMP and proinflammatory cytokines induced by UV exposure and reduces skinfold thickness and intracellular Ca2+ influx, so that it can be effectively used as an active ingredient of the composition for skin-aging prevention, wrinkle improvement, skin-whitening, or alleviating inflammation, irritation, or pain.

Abstract translation: 描述了TRPV1抑制肽和包含其作为活性成分的防止皮肤衰老和皱纹改善的组合物。 本发明的TRPV1抑制肽抑制由UV暴露诱导的MMP和促炎细胞因子的表达，并减少皮肤厚度和细胞内Ca 2+流入，从而可有效地用作预防皮肤衰老的组合物的活性成分， 皱纹改善，皮肤美白或减轻炎症，刺激或疼痛。