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公开(公告)号：US07294496B1
公开(公告)日：2007-11-13
申请号：US09493601
申请日：2000-01-28
申请人： Edward A. Dennis , Aijun Wang
发明人： Edward A. Dennis , Aijun Wang
CPC分类号： C12N9/20 , A61K38/00 , A61K48/00 , C12Q1/34 , G01N2333/918
摘要： A cloned of a human brain lysophospholipid-specific lysophospholipase enzyme molecule, its potential use for treatment of a host of diseases and method of inactivation are disclosed. Also disclosed are its distribution in tissue sand detailed kinetic analysis. hLysoPLA has a single substrate binding site and a surface recognition site. In contrast to many nonspecific lipolytic enzymes that exhibit lysophospholipase activity, hLysoPLA hydrolyzes only lysophospholipids and has no other significant enzymatic activity.
摘要翻译： 公开了人脑溶血磷脂特异性溶血磷脂酶分子的克隆，其用于治疗一系列疾病的潜在用途和灭活方法。 还披露了其在组织砂中的分布详细的动力学分析。 hLysoPLA具有单个底物结合位点和表面识别位点。 与许多显示溶血磷脂酶活性的非特异性脂肪分解酶相反，hLysoPLA仅水解溶血磷脂并且没有其他显着的酶活性。
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公开(公告)号：US5464754A
公开(公告)日：1995-11-07
申请号：US107378
申请日：1993-08-17
申请人： Edward A. Dennis , Laure J. Reynolds , Lin Yu
发明人： Edward A. Dennis , Laure J. Reynolds , Lin Yu
CPC分类号： C07F9/10 , C12Q1/44 , G01N2333/918
摘要： A non-radioactive, spectrophotometric, microtiter plate assay for human cystolic phospholipase A.sub.2 (cPLA.sub.2) is described. The assay utilizes a novel synthetic thiol-phospholipid analog as a substrate. In one embodiment, the substrate is a phosphatidylcholine derivative with an arachidonoylthioester in the sn-2 position and an alkenyl-ether or alkenyl-ether in the sn-1 position. The alkyl-ether and the alkenyl-ether in the sn-1 position of the substrate ensures that the assay will only measure cPLA.sub.2 activity and will not be complicated by metabolism of the lysophospholipid product by the enzyme's and lysophospholypase activity.
摘要翻译： 描述了人类收缩磷脂酶A2（cPLA2）的非放射性，分光光度法，微量滴定板测定法。 该测定法利用新的合成硫醇 - 磷脂类似物作为底物。 在一个实施方案中，底物是具有sn-2位置的花生四烯酰硫代酯和sn-1位置的烯基醚或链烯基醚的磷脂酰胆碱衍生物。 底物sn-1位置中的烷基醚和链烯基醚确保了该测定将仅测量cPLA2活性，并且不会因酶和溶血磷脂酶活性而使溶血磷脂产物的代谢变得复杂。
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公开(公告)号：US5352673A
公开(公告)日：1994-10-04
申请号：US712968
申请日：1991-06-10
申请人： Edward A. Dennis
发明人： Edward A. Dennis
IPC分类号： A61K31/00 , C07F9/10 , C12Q1/34 , A61K31/685
CPC分类号： A61K31/685 , A61K31/00 , C07F9/10 , C12Q1/34 , C12Q2334/10 , G01N2333/918 , G01N2405/04
摘要： The present invention provides prodrugs that serve as useful therapeutics for various disease states and conditions mediated by underlying specific hydrolytic enzyme activity. The prodrugs hereof (additionally) impart a physiologically bioactive component thus providing prodrug compounds that are capable of imparting dual effect systemically.
摘要翻译： 本发明提供了用作各种疾病状态和由潜在的特异性水解酶活性介导的病症的有用治疗剂的前药。 本发明的前药（另外）赋予生理活性成分，从而提供能够全身赋予双重效果的前药化合物。
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