公开(公告)号：US20150182581A1

公开(公告)日：2015-07-02

申请号：US14382428

申请日：2013-03-01

Applicant: Council of Scientific & Industrial Research

Inventor： Raj Kamal Tripathi ,  Balawant Kumar ,  Ravishankar Ramachandran ,  Jitendra Kumar Tripathi ,  Smriti Bhadauria ,  Jimut Kanti Ghosh

IPC: A61K38/04 ,  C12Q1/18 ,  C07K2/00

CPC classification number: A61K38/04 ,  A61K38/00 ,  C07K2/00 ,  C07K14/005 ,  C12N2740/16322 ,  C12Q1/18 ,  G01N33/5041 ,  G01N33/56988 ,  G01N2500/10

Abstract: The present invention relates to synthetic peptide inhibitors (Seq ID No. 67-71) useful as anti-HIV therapeutics. The invention also relates to a novel screening method for screening anti-HIV molecules. The present invention relates to a synthetic peptide useful as anti-HIV therapeutic. The invention also relates to a novel screening method for screening of anti-HIV therapeutics. In particular, the present invention relates to reporter gene constructs for the detection of the HIV Nef and host ASK1 protein interaction. Furthermore, the invention relates to a functional interaction for Nef-ASK1 proteins prepared in a recombinant manner, a method for identifying of Nef-ASK1 interaction which causes activation of pathway to activate apoptosis presumably causing immune evasion for HIV in infected cells. The reporter gene construct according to the present invention, after it had been introduced into cells, in the presence of HIV Nef and host ASK1 proteins result in the expression of reporter luciferase protein which may be used for quantitative/qualitative interaction of HIV Nef and host ASK1 protein. The both interacting construct cloned in fluorescence expression vector when transfected in eukaryotic cells inhibits ASK1 mediated apoptosis and were reversed by the inhibitors. Furthermore, the invention was used to identify the inhibitor for the interaction of Nef-ASK1 in the cell.

Abstract translation: 本发明涉及可用作抗HIV治疗剂的合成肽抑制剂（Seq ID No.67-71）。 本发明还涉及用于筛选抗HIV分子的新型筛选方法。 本发明涉及可用作抗HIV治疗剂的合成肽。 本发明还涉及用于筛选抗HIV治疗剂的新型筛选方法。 特别地，本发明涉及用于检测HIV Nef和宿主ASK1蛋白相互作用的报道基因构建体。 此外，本发明涉及以重组方式制备的Nef-ASK1蛋白质的功能相互作用，用于鉴定Nef-ASK1相互作用的方法，其引起途径激活以诱导感染细胞中可能引起HIV免疫逃避的凋亡的凋亡的方法。 根据本发明的报告基因构建体在HIV Nef和宿主ASK1蛋白存在下被引入细胞后，导致报告荧光素酶蛋白的表达，其可用于HIV Nef和宿主的定量/定性相互作用 ASK1蛋白。 当在真核细胞中转染时，克隆在荧光表达载体中的两个相互作用构建体都抑制ASK1介导的细胞凋亡并被抑制剂逆转。 此外，本发明用于鉴定细胞内Nef-ASK1相互作用的抑制剂。

公开(公告)号：US09068973B2

公开(公告)日：2015-06-30

申请号：US14026145

申请日：2013-09-13

Applicant: Biocrine AB

Inventor： Per Olof Berggren ,  Shao-Nian Yang

IPC: A01N1/02 ,  C12N5/00 ,  G01N33/50

CPC classification number: A61K39/395 ,  A61K31/472 ,  A61K31/496 ,  A61K31/7076 ,  A61K31/713 ,  C07K16/2842 ,  C12N15/113 ,  C12N15/1138 ,  C12N15/115 ,  C12N2310/14 ,  C12N2320/30 ,  G01N33/5041 ,  G01N33/507

Abstract: The present invention provides methods for identifying candidate compounds for limiting development of and/or treating diabetes, and methods for limiting development of and/or treating diabetes.

公开(公告)号：US20150158921A1

公开(公告)日：2015-06-11

申请号：US14407770

申请日：2013-06-08

Applicant: HAINAN UNIVERSITY

Inventor： Sulan Luo ,  Dongting Zhangsun ,  Yong Wu ,  Xiaopeng Zhu ,  Yuanyan Hu ,  J.Michael Mcintosh

IPC: C07K14/435 ,  G01N33/50 ,  C07K1/00

CPC classification number: C07K14/43504 ,  A61K38/00 ,  C07K1/00 ,  C07K14/00 ,  C07K2319/00 ,  C07K2319/55 ,  G01N33/5041 ,  G01N33/6872 ,  G01N33/944 ,  G01N2500/04 ,  G01N2500/10

Abstract: The present invention pertains to fields of biochemistry and molecular biology, relates to an αO-superfamily conotoxin peptide, pharmaceutical composition thereof, preparation method and use thereof. The present invention further relates to a propeptide of the conotoxin peptide, nucleic acid construct thereof, expression vector and transformed cell thereof, and fusion protein thereof. The present invention further relates to a method for blocking acetylcholine receptors as well as a use of the conotoxin peptide in the manufacture of a medicament. The new αO-superfamily conotoxin peptide of the present invention is capable of specifically blocking acetylcholine receptor (nAChRs) (e.g., α9α10 nAChR), and NMDA receptor (e.g., NR2C NMDAR), and has activity for treatment of neuralgia, addiction, and activity for treatment of chemotherapy of cancers, breast cancer, lung cancer, wound healing, epilepsia, ischemia, and thus is promising in the manufacture of analgesic, a medicament for treatment of addiction, and a tool drug for neuroscience.

Abstract translation: 本发明涉及生物化学和分子生物学领域，涉及αO超家族荚果毒素肽，其药物组合物，其制备方法和用途。 本发明还涉及荚蛋毒素肽的前肽，其核酸构建体，表达载体及其转化细胞及其融合蛋白。 本发明还涉及一种阻断乙酰胆碱受体的方法，以及在制造药物中使用芋头毒素肽。 本发明的新型αO超家族荚果毒素肽能够特异性阻断乙酰胆碱受体（nAChRs）（例如α9α10nAChR）和NMDA受体（如NR2C NMDAR），具有治疗神经痛，成瘾和活动的活性 用于治疗癌症，乳腺癌，肺癌，伤口愈合，癫痫，局部缺血的化疗，因此在制造镇痛药中是有希望的，用于治疗成瘾的药物和用于神经科学的工具药物。

公开(公告)号：US20150141470A1

公开(公告)日：2015-05-21

申请号：US14399085

申请日：2013-05-08

Applicant: The Broad Institute, Inc. ,  Dana-Farber Cancer Institute, Inc.

Inventor： Levi A. Garraway ,  Cory M. Johannessen

IPC: G01N33/50 ,  A61K45/06 ,  A61K31/435 ,  A61K31/404 ,  A61K31/16

CPC classification number: G01N33/5008 ,  A61K31/16 ,  A61K31/404 ,  A61K31/435 ,  A61K31/44 ,  A61K31/485 ,  A61K31/506 ,  A61K31/519 ,  A61K45/06 ,  C12Q1/6827 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158 ,  G01N33/5041 ,  G01N33/57484 ,  G01N2333/726 ,  G01N2800/52 ,  G01N2800/60 ,  C12Q2537/16 ,  A61K2300/00

Abstract: A method of identifying a subject having cancer who is likely to benefit from treatment with a combination therapy with a MAPK pathway inhibitor, such as a RAF inhibitor, MEK inhibitor, or ERK inhibitor, and a GEF or HDAC inhibitor is provided. A method of treating cancer in a subject in need thereof is also provided and includes administering to the subject an effective amount of a MAPK inhibitor, such as a RAF inhibitor, MEK inhibitor, or ERK inhibitor, and an effective amount of a GEF or HDAC inhibitor. A method of identifying targets that confers resistance to a MAPK pathway inhibitor is also provided.

Abstract translation: 提供了鉴定具有可能受益于通过与MAPK途径抑制剂如RAF抑制剂，例如RAK抑制剂或ERK抑制剂，GEF或HDAC抑制剂的MAPK途径抑制剂联合治疗的癌症的患者的方法。 还提供了在有需要的受试者中治疗癌症的方法，包括向受试者施用有效量的MAPK抑制剂如RAF抑制剂，MEK抑制剂或ERK抑制剂和有效量的GEF或HDAC 抑制剂。 还提供了鉴定赋予对MAPK通路抑制剂抗性的靶标的方法。

公开(公告)号：US20150133441A1

公开(公告)日：2015-05-14

申请号：US14297863

申请日：2014-06-06

Applicant: HMI Medical Innovations, LLC.

Inventor： Gerard M. Housey

IPC: A61K31/5377 ,  A61K31/47 ,  G01N33/50 ,  A61K31/505 ,  A61K31/53 ,  A61K31/506 ,  A61K31/4709

CPC classification number: A61K31/5377 ,  A61K31/166 ,  A61K31/175 ,  A61K31/195 ,  A61K31/27 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/53 ,  C07C243/38 ,  C07D213/77 ,  C07D213/81 ,  C07D213/86 ,  C07D213/87 ,  C07D215/38 ,  C07D215/50 ,  C07D231/14 ,  C07D239/42 ,  C07D239/48 ,  C07D239/84 ,  C07D253/065 ,  C07D253/075 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  G01N33/5011 ,  G01N33/502 ,  G01N33/5041 ,  G01N33/573 ,  G01N33/574 ,  G01N2500/00 ,  G01N2500/10

Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

Abstract translation: 本发明涉及作为内源性蛋白质的变体形式的抑制剂或活化剂的试剂，以及鉴定这些变体的新方法。 特别令人感兴趣的是内源性蛋白质变体的抑制剂和活化剂，其由具有突变的基因编码，所述变体经常出现或至少首先被鉴定为在暴露于化学试剂之后产生，已知其是相应的抑制剂或活化剂 未突变的内源蛋白

公开(公告)号：US09005909B2

公开(公告)日：2015-04-14

申请号：US13333817

申请日：2011-12-21

Applicant: Vadim Markovtsov ,  Yasumichi Hitoshi

Inventor： Vadim Markovtsov ,  Yasumichi Hitoshi

IPC: G01N33/573 ,  G01N33/49 ,  G01N33/53

CPC classification number: G01N33/573 ,  G01N33/49 ,  G01N33/4915 ,  G01N33/5041 ,  G01N33/53 ,  G01N2333/912 ,  G01N2333/91205 ,  G01N2800/02

Abstract: A method of sample analysis is provided. In certain embodiments, the method comprises: a) labeling cells of a blood sample using an antibody that specifically binds to phospho-AMPK or a phosphorylated target thereof, to produce a labeled sample; and b) measuring antibody binding by a population of blood cells of the labeled sample using flow cytometry. In particular embodiments, the method may further comprise, prior to the labeling step: contacting blood with a test agent ex vivo or in vivo; and comparing the evaluation to results obtained from a reference sample of blood cells.

Abstract translation: 提供了样品分析的方法。 在某些实施方案中，所述方法包括：a）使用特异性结合磷酸化AMPK或其磷酸化靶标的抗体标记血液样品的细胞，以产生标记的样品; 和b）使用流式细胞术测量标记样品的血细胞群体的抗体结合。 在具体实施方案中，该方法还可以包括在标记步骤之前：离体或体内使血液与测试试剂接触; 并将评估与从血细胞的参考样品获得的结果进行比较。

公开(公告)号：US08986687B2

公开(公告)日：2015-03-24

申请号：US13509592

申请日：2010-11-15

Applicant: Ana Martin-Vilalba ,  Peter Herhaus ,  Ignacio Sancho-Martinez ,  Susanne Kleber ,  Thilo Welsch

Inventor： Ana Martin-Vilalba ,  Peter Herhaus ,  Ignacio Sancho-Martinez ,  Susanne Kleber ,  Thilo Welsch

IPC: A61K39/395 ,  G01N33/50 ,  A61K31/7105

CPC classification number: G01N33/5041 ,  A61K31/7105 ,  G01N33/5011 ,  G01N2333/70578

Abstract: The present invention is concerned with compounds inhibiting CD95 signaling in pancreatic cancer cells. Furthermore, contemplated by the current invention are medicaments comprising such a compound for the prevention and/or treatment of pancreatic cancer as well as the use of such a compound for the manufacture of a medicament for the prevention and/or treatment of pancreatic cancer, the prevention of migration of cancer cells, and/or the prevention and/or treatment of an inflammatory reaction. The present invention also refers to a method for the identification of a compound inhibiting CD95 signaling, as we to a method for the manufacture of a medicament comprising the steps of the method for the identification of a compound inhibiting CD95 signaling and the further step of formulating the inhibiting compound as a medicament.

Abstract translation: 本发明涉及抑制胰腺癌细胞中CD95信号传导的化合物。 此外，本发明考虑的是包含这种用于预防和/或治疗胰腺癌的化合物的药物以及这种化合物在制备用于预防和/或治疗胰腺癌的药物中的用途， 预防癌细胞的迁移，和/或预防和/或治疗炎性反应。 本发明还涉及一种用于鉴定抑制CD95信号的化合物的方法，如我们关于制备药物的方法，包括以下步骤：鉴定抑制CD95信号的化合物的方法和进一步的配制步骤 作为药物的抑制化合物。

公开(公告)号：US08962263B2

公开(公告)日：2015-02-24

申请号：US13094735

申请日：2011-04-26

Applicant: Omar D. Perez ,  Garry P. Nolan

Inventor： Omar D. Perez ,  Garry P. Nolan

IPC: G01N33/574 ,  G01N33/557 ,  G01N33/53 ,  C12Q1/48 ,  G01N33/50 ,  G01N33/543 ,  G01N33/573 ,  G01N33/58

CPC classification number: G01N33/6845 ,  C12Q1/485 ,  G01N21/6428 ,  G01N33/5008 ,  G01N33/5041 ,  G01N33/5091 ,  G01N33/5094 ,  G01N33/5302 ,  G01N33/54313 ,  G01N33/573 ,  G01N33/582 ,  G01N2021/6441 ,  G01N2333/91205 ,  G01N2333/96466 ,  G01N2405/00 ,  G01N2440/14 ,  Y10S435/973 ,  Y10T436/101666 ,  Y10T436/25

Abstract: The invention provides methods and compositions for simultaneously detecting the activation state of a plurality of proteins in single cells using flow cytometry. The invention further provides methods and compositions of screening for bioactive agents capable of coordinately modulating the activity of a plurality of proteins in single cells. The methods and compositions can be used to determine the protein activation profile of a cell for predicting or diagnosing a disease state, and for monitoring treatment of a disease state.

公开(公告)号：US20150024407A1

公开(公告)日：2015-01-22

申请号：US14338003

申请日：2014-07-22

Applicant: SENOMYX, INC.

Inventor： Jon E. ADLER ,  Xiaodong LI ,  Lena STASZEWSKI ,  Hong XU ,  Fernando ECHEVERRI

IPC: G01N33/50

CPC classification number: G01N33/5041 ,  C07K14/723 ,  G01N33/5008 ,  G01N33/5023 ,  G01N33/74 ,  G01N2333/705 ,  G01N2333/726 ,  G01N2500/00

Abstract: Newly identified mammalian taste-cell-specific G protein-coupled receptors which function as hetero-oligomeric complexes in the sweet taste transduction pathway, and the genes and cDNA encoding said receptors are described. Specifically, T1R G protein-coupled receptors active in sweet taste signaling as hetero-oligomeric complexes, and the genes and cDNA encoding the same, are described, along with methods for isolating such genes and for isolating and expressing such receptors. Methods for identifying putative taste modulating compounds using such hetero-oligomeric complexes also described, as is a novel surface expression facilitating peptide useful for targeting integral plasma membrane proteins to the surface of a cell.

Abstract translation: 描述了在甜味转导途径中作为异寡聚复合物起作用的新鉴定的哺乳动物味细胞特异性G蛋白偶联受体，以及编码所述受体的基因和cDNA。 具体来说，描述了作为异寡聚复合物的甜味信号传导中起作用的T1R G蛋白偶联受体，以及编码相同基因和cDNA的方法，以及用于分离这些基因并分离和表达此类受体的方法。 还描述了使用这种异寡​​聚复合物鉴定推定的味觉调节化合物的方法，以及用于靶向细胞表面的整合质膜蛋白的新颖的表达表达促进肽。

公开(公告)号：US08937050B2

公开(公告)日：2015-01-20

申请号：US13665679

申请日：2012-10-31

Applicant: Paul Talalay ,  Andrew W. Zimmerman ,  Kirby D. Smith

Inventor： Paul Talalay ,  Andrew W. Zimmerman ,  Kirby D. Smith

IPC: A61K31/145 ,  A61K31/17 ,  A61K31/70 ,  A61K31/165 ,  A61K31/18 ,  A61K31/19 ,  A61K31/192 ,  A61K31/26 ,  A61K31/343 ,  A61K31/4045 ,  A61K31/4184 ,  A61K31/506 ,  A61K31/517 ,  A61K31/167

CPC classification number: A61K31/17 ,  A61K31/145 ,  A61K31/165 ,  A61K31/167 ,  A61K31/18 ,  A61K31/19 ,  A61K31/192 ,  A61K31/26 ,  A61K31/343 ,  A61K31/4045 ,  A61K31/4184 ,  A61K31/506 ,  A61K31/517 ,  A61K31/70 ,  G01N33/5023 ,  G01N33/5041 ,  G01N33/5044 ,  G01N2500/10 ,  G01N2800/2814 ,  G01N2800/52

Abstract: Disclosed herein are methods and compositions for treating autism. Disclosed herein are methods and compositions for treating an autism spectrum disorder.

Abstract translation: 本文公开了治疗自闭症的方法和组合物。 本文公开了治疗自闭症谱系障碍的方法和组合物。