N-(4-Aminobutyl)-N'-(2-methoxyethyl)guanidine (8a) is a potent inhibitor targeting the hDDAH-1 active site (Ki = 18 μM) and derived from a series of guanidine- and amidine-based inhibitors. Its nonamino acid nature leads to high selectivities toward other enzymes of the nitric oxide-modulating system. Crystallographic data of 8a-bound hDDAH-1 illuminated a unique binding mode. Together with its developed N-hydroxyguanidine prodrug 11, 8a will serve as a most widely applicable, pharmacological tool to target DDAH-1-associated diseases.

中文翻译：

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N-（4-氨基丁基）-N'-（2-甲氧基乙基）胍作为人类二甲基精氨酸二甲基氨基水解酶-1（hDDAH-1）的第一种选择性，非氨基酸催化位点抑制剂的发现。

N-（4-氨基丁基）-N'-（2-甲氧基乙基）胍（8a）是靶向hDDAH-1活性位点（Ki = 18μM）的有效抑制剂，衍生自一系列基于胍和am的抑制剂。它的非氨基酸性质导致对一氧化氮调节系统的其他酶具有很高的选择性。结合8a的hDDAH-1的晶体学数据阐明了一种独特的结合模式。连同其开发的N-羟基胍前药11、8a一起，将成为针对DDAH-1相关疾病的最广泛应用的药理学工具。