Patent application number | Description | Published |
20090221530 | Relaxase Modulators and Methods of Using Same - Methods of treating a microbial infection in a subject by administering to the subject an effective amount of a compound that modulates an enzymatic activity of a relaxase polypeptide is provided. Methods of inhibiting bacterial conjugation by modulating activity of a relaxase polypeptide in a bacterium are also provided. Novel compounds that modulate relaxase enzymes and assays for measuring kinetics of relaxase enzymes and selecting for modulators of relaxase enzyme activity are further provided. | 09-03-2009 |
20110165141 | Compositions for treating bacterial infections - Polynucleotides encoding a mutant human carboxylesterase enzyme and polypeptides encoded by the polynucleotides which are capable of metabolizing a prodrug and inactive metabolites thereof to active drug are provided. Compositions and methods for sensitizing cells to a prodrug agent, inhibiting cell growth, treating drug addiction, and facilitating the metabolism of an organophosphate with this enzyme are also provided. In addition, a screening assay for identification of drugs activated by this enzyme is described. | 07-07-2011 |
20120142108 | Compositions For Treating Bacterial Infections - Polynucleotides encoding a mutant human carboxylesterase enzyme and polypeptides encoded by the polynucleotides which are capable of metabolizing a prodrug and inactive metabolites thereof to active drug are provided. Compositions and methods for sensitizing cells to a prodrug agent, inhibiting cell growth, treating drug addiction, and facilitating the metabolism of an organophosphate with this enzyme are also provided. In addition, a screening assay for identification of drugs activated by this enzyme is described. | 06-07-2012 |
Patent application number | Description | Published |
20120309037 | Methods and Compositions for Detection and Identification of Organophosphorus Nerve Agents, Pesticides and Other Toxins - The present invention provides methods and devices for detecting and identifying toxins, including but not limited to organophosphorus nerve agents and/or organophosphorus pesticides, in a sample. One embodiment of the present invention comprises a method for identifying an organophosphorus nerve agent and/or an organophosphorus pesticide, comprising: exposing a group of enzymes comprising human carboxylesterase 1, at least one mutant of human carboxylesterase 1, and acetylcholinesterase to a sample, wherein the enzymes are separate from each other and each enzyme binds at least one organophosphorus nerve agent or at least one organophosphorus pesticide; contacting the exposed enzymes with a fluid comprising an oxime and a substrate; and detecting a signal produced upon reaction of the substrate and the exposed enzymes, whereby detection of the signal identifies the organophosphorus nerve agent and/or the organophosphorus pesticide. | 12-06-2012 |
20130345196 | PHENOXY THIOPHENE SULFONAMIDES AND OTHER COMPOUNDS FOR USE AS INHIBITORS OF BACTERIAL GLUCURONIDASE - This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial β-glucuronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy. | 12-26-2013 |
20130345235 | PHENOXY THIOPHENE SULFONAMIDES AND THEIR USE AS INHIBITORS OF GLUCURONIDASE - This invention relates generally to compounds that are glucuronidase inhibitors. Glucuronidase inhibitors described include phenoxy thiophene sulfonamides. Other compounds, for instance pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls, are also contemplated. Also contemplated are compositions including one or more of such compounds for use inhibiting glucuronidase and methods of using one or more of such compounds as a co-drug to be used in combination with the anticancer drug CPT-11. | 12-26-2013 |