I. Lunk, Felix-A. Litty, S. Hennig
Dec 16, 2019
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0
Influential Citations
1
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Journal
Journal of medicinal chemistry
Abstract
N-(4-aminobutyl)-N'-(2-methoxyethyl)guanidine (8a) is as a potent inhibitor targeting the hDDAH-1 active site (Ki = 18 µM) and derived from a series of guanidine- and amidine-based inhibitors. Its non-amino acid nature leads to high selectivities towards 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, currently available pharmacological tool to target DDAH-1-associated diseases.