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1. 发明申请

US20080118933A1 Methods of screening for inhibitors of antiplasmin cleaving enzyme 审中-公开
标题翻译：筛选抗肿瘤酶切割酶抑制剂的方法
公开(公告)号：US20080118933A1
公开(公告)日：2008-05-22
申请号：US11986058
申请日：2007-11-20
申请人： Patrick McKee , Kyung Lee , Kenneth Jackson , Victoria Christiansen
发明人： Patrick McKee , Kyung Lee , Kenneth Jackson , Victoria Christiansen
IPC分类号： G01N33/53 , C12N9/68
CPC分类号： C12Q1/37 , A61K38/00 , C07K14/745 , C07K14/8121 , C12N9/6421 , C12P21/06 , G01N2500/00
摘要： Human α2-antiplasmin (α2AP) is the major inhibitor of the proteolytic enzyme plasmin that digests fibrin. Two forms of α2AP circulate in human plasma: a 464-residue protein, which we have termed “pro”-form, or α2APpro and an N-terminally-shortened 452-residue “activated”-form, or α2APact. The latter becomes crosslinked to fibrin by activated factor XIII about 5-fold more rapidly than α2APpro and makes fibrin resistant to digestion by plasmin. A new human plasma proteinase has been identified herein that cleaves the Pro12-Asn13 bond of α2APpro to yield α2APact. This enzyme is identified herein as Antiplasmin Cleaving Enzyme (APCE). Novel inhibitors of circulating APCE can diminish α2AP inhibitory capacity within forming fibrin or blood clots thereby making fibrin deposits or blood clots more susceptible to removal by plasmin. Patients who are susceptible to atherosclerotic plaque formation or are susceptible to developing thrombi that compromise organ function will benefit by therapies providing such inhibitors on a long term basis.
摘要翻译：人α2 - 对映体蛋白（α2 AP）是消化纤维蛋白的蛋白水解酶纤溶酶的主要抑制剂。两种形式的α2 AP在人血浆中循环：464残基的蛋白质，我们称之为“亲”型或α2亚基 / SUB>和N-末端缩短的452残基“活化”形式或α2亚类作用。后者通过活化因子XIII与α2 P肽相比快速交联5倍，并使纤维蛋白对纤溶酶消化具有抗性。本文已经鉴定了一种新的人血浆蛋白酶，其切割了α2 -ATP pro pro的Pro12-Asn13键，以产生α2亚基。该酶在本文中被鉴定为抗血小板裂解酶（APCE）。循环APCE的新型抑制剂可以降低形成纤维蛋白或血凝块中的α2 AP抑制能力，从而使纤维蛋白沉积物或血块更容易被纤溶酶去除。易受动脉粥样硬化斑块形成或容易发生危及器官功能的血栓的患者将通过长期提供这种抑制剂的疗法而受益。

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