专利号:US-6624144-B1 优先权日:1998-03-18 标 题:Matrix metalloproteinase inhibitors and down-regulators 发明人:KOIVUNEN ERKKI; SORSA TIMO; SALO TUULA 权利人:CTT CANCER TARGETING TECH OY 摘要:The present invention relates to novel matrix metalloproteinase (MMP) inhibitors and down-regulators, to a process for the preparation of these inhibitors, to pharmaceutical compositions comprising these inhibitors/down-regulators, to the use of the novel MMP inhibitors for the manufacture of pharmaceutical and research preparations, to a method for inhibiting and down-regulating MMP-dependent conditions either in vivo or in vitro, to a method for inhibiting formation, synthesis, expression activations, and/or functions as well as actions of matrix metalloproteinases, and to the use of the novel MMP inhibitors and down-regulators in biochemical isolation and purification procedures of matrix metalloproteinases.
专利号:US-6911318-B2 优先权日:1999-03-03 标 题:Bacterial transglycosylases: assays for monitoring the activity using Lipid II substrate analogs and methods for discovering new antibiotics 发明人:KAHNE SUZANNE WALKER 权利人:UNIV PRINCETON 摘要:This invention provides a direct method for monitoring bacterial transglycosylase activity using labeled substrates produced by chemo-enzymatic synthesis wherein the labels are selected to permit the detection of both polymeric and non-polymeric products simultaneously, either directly or following the separation of product from starting material. The invention promotes the discovery of new antibiotics with activity against bacterial transglycosylases by a) laying the groundwork for structural analysis of purified, active transglycosylase (which permits structure-based design); and b) providing an assay that can be used to screen for inhibitors.
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合成参考文献
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