HARNESSING NETWORK BIOLOGY TO IMPROVE DRUG DISCOVERY
    1.
    发明公开
    HARNESSING NETWORK BIOLOGY TO IMPROVE DRUG DISCOVERY 审中-公开
    网络生物学用于改进药物发现

    公开(公告)号:EP1836631A2

    公开(公告)日:2007-09-26

    申请号:EP05824951.7

    申请日:2005-11-22

    IPC分类号: G06F19/00

    摘要: This invention provides principles, methods and compositions for ascertaining the mechanism of action of pharmacologically important compounds in the context of network biology, across the entire scope of the complex pathways of living cells. Importantly, the principles, methods and compositions provided allow a rapid assessment of the on-pathway and off-pathway effects of lead compounds and drug candidates in living cells, and comparisons of lead compounds with well-characterized drugs and toxicants to identify patterns associated with efficacy and toxicity. The invention will be useful in improving the drug discovery process, in particular by identifying drug leads with desired safety and efficacy and in effecting early attrition of compounds with potential adverse effects in man.

    KINASE INHIBITORS FOR THE TREATMENT OF DIABETES AND OBESITY
    4.
    发明公开
    KINASE INHIBITORS FOR THE TREATMENT OF DIABETES AND OBESITY 审中-公开
    激酶抑制剂来治疗糖尿病和肥胖症

    公开(公告)号:EP1812078A2

    公开(公告)日:2007-08-01

    申请号:EP05851268.2

    申请日:2005-10-29

    摘要: The present invention discloses a method of treating an individual or animal with diabetes and/or obesity. The method comprises administering to the individual or animal a therapeutically effective amount of a protein tyrosine kinase inhibitor. Preferably, the preventative and therapeutic methods of the present invention involve administering - to a mammal in need thereof - a therapeutically effective amount of an inhibitor of a c-Src-family protein tyrosine kinase. The invention pertains to pharmaceutical compositions containing an inhibitor of a c-Src-family protein tyrosine kinase or an analog or metabolite thereof, or an inhibitor of another protein tyrosine kinase, and a pharmaceutically acceptable carrier. Purines and pyrimidines and other molecules useful in the treatment of diabetes and obesity are provided herein, in particular, pyrazolopyrimidines, cyanoquinolines, phenylaminopyrimidines, anilinoquinazolines and related compounds. The invention also provides cellular targets and assay compositions useful for the identification of additional novel therapeutic agents for the treatment of these disorders.

    PHARMACOLOGICAL PROFILING OF DRUGS WITH CELL-BASED ASSAYS
    5.
    发明公开
    PHARMACOLOGICAL PROFILING OF DRUGS WITH CELL-BASED ASSAYS 审中-公开
    CREATING原料药的药理特性文件通过试验对蜂窝基站的方式

    公开(公告)号:EP1784642A2

    公开(公告)日:2007-05-16

    申请号:EP05788134.4

    申请日:2005-08-18

    IPC分类号: G01N33/53

    摘要: The instant invention provides a method for establishing safety profiles for chemical compounds, as well as pharmacological profiling said method comprising (A) testing the effects of said chemical compounds on the amount and/or post-translational modifications of two or more macromolecules in intact cells; (B) constructing a pharmacological profile based on the results of said tests; and (C) comparing said profile to the profile(s) of drugs with established safety characteristics. Additionally, the invention is also directed to a composition comprising an assay panel, said panel comprising at least one high-content assay for the amount and/or post-­translational modification of a protein and at least one high-content assay for the amount and/or subcellular location of a protein-protein interaction.

    FRAGMENT COMPLEMENTATION ASSAYS FOR G-PROTEIN-COUPLED RECEPTORS AND THEIR SIGNALING PATHWAYS
    6.
    发明公开
    FRAGMENT COMPLEMENTATION ASSAYS FOR G-PROTEIN-COUPLED RECEPTORS AND THEIR SIGNALING PATHWAYS 有权
    FRAGMENTKOMPLEMENTATIONSTESTS对于G蛋白偶联受体,和信号通路

    公开(公告)号:EP1668161A2

    公开(公告)日:2006-06-14

    申请号:EP04785127.4

    申请日:2004-09-24

    IPC分类号: C12Q1/68 G01N33/53 C12P21/02

    摘要: This invention relates generally to the fields of biology, molecular biology, chemistry and biochemistry. The invention is directed to a large number of novel assays for G-protein-coupled receptors (GPCRs) and their signaling pathways. Methods are described for constructing such assays for one or more steps in a GPCR pathway. The invention can be used for functional characterization of GPCRs, target validation, de-orphanization of receptors, high-throughput screening, high-content screening, pharmacological profiling, and other drug discovery applications. The assays can be used directly to assess whether a compound library or a biological extract contains an agonist or antagonist of a receptor. Assay compositions are also provided. The development of such assays is shown to be straightforward, providing for a broad, flexible and biologically relevant platform for the discovery of novel drugs and natural ligands that act on GPCRs or their cognate pathways.

    FRAGMENTS OF FLUORESCENT PROTEINS FOR PROTEIN FRAGMENT COMPLEMENTATION ASSAYS
    7.
    发明公开
    FRAGMENTS OF FLUORESCENT PROTEINS FOR PROTEIN FRAGMENT COMPLEMENTATION ASSAYS 审中-公开
    荧光蛋白碎片作蛋白片段,互补

    公开(公告)号:EP1616186A2

    公开(公告)日:2006-01-18

    申请号:EP04759337.1

    申请日:2004-04-09

    IPC分类号: G01N33/53 C07K14/00

    摘要: The present invention is directed to Protein-fragment Complementation Assays (PCAs) and assay compositions based on fluorescent proteins. The invention provides methods for fragmenting fluorescent proteins and generating mutant fragments with desir4 spectral characteristics for PCA. The invention encompasses assays and compositions based on fluorescent proteins from the species Aequorea, Anemonia and Anthozoa. In particular, the invention is directed to fragments of mutant fluorescent proteins having improved spectral properties over the wild-type proteins. The invention encompasses fragments of mutant versions of A. Victoria green fluorescent protein (GFP), in particular yellow fluorescent proteins (EYFP and super-EYFP), 'Venus', cyan, 'citrine', blue, cyan-green, and photoactivatable variants of GFP. The invention also encompasses red fluorescent PCAs based on Discosoma red fluorescent protein (RFP PCA)and a kindling fluorescent protein PCA (KFP 1 PCA) derived from Anemonia sulcata. Any useful mutation of a fluorescent protein can be engineered into a fragment, generating a wide range of assays useful for drug discovery, target validation, high-throughput screening, high-content screening, pathway mapping, drug mechanism-of-action studies, blosensors, and diagnostics.