Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors

Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors
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DOI:
10.1021/ja0277226
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发表时间:
2002-10-09
影响因子:
15
通讯作者:
Patane, MA
Patane, MA
中科院分区:
化学1区
文献类型:
--
作者:
Dales, NA;Gould, AE;Patane, MA

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血管紧张素转换酶相关羧肽酶(ACE2)是最近利用我们的基因组学平台鉴定的一种具有羧肽酶活性的锌金属蛋白酶。我们实施了一种合理的设计方法来确定有效和选择性的ACE2抑制剂。为此,我们设计合成了血管紧张素转换酶2的皮摩尔抑制剂。
Angiotensin-converting enzyme-related carboxypeptidase (ACE2) is a recently identified zinc metalloprotease with carboxypeptidase activity that was identified using our genomics platform. We implemented a rational design approach to identify potent and selective ACE2 inhibitors. To this end, picomolar inhibitors of ACE2 were designed and synthesized.