Selective substrate-based inhibitors of mammalian dimethylarginine dimethylaminohydrolase

S. Rossiter, C.L. Smith, M. Malaki, M. Nandi, H. Gill, J.M. Leiper, P. Vallance, D.L. Selwood

Research output: Contribution to journalArticlepeer-review

50 Citations (Scopus)


The enzyme DDAH metabolizes methylarginines that are inhibitors of nitric oxide synthase (NOS). Substrate-based inhibitors of mammalian DDAH have been synthesized, with optimization to give selective inhibition of DDAH with no significant direct effect on NOSs. These are the first examples of reversible DDAH inhibitors with significant activity and selectivity. In vivo administration increases plasma ADMA levels, giving proof of concept that these inhibitors can be used to probe the physiological effects of DDAH inhibition, with potential for pharmaceutical use of DDAH inhibitors in diseases where excess NO production is implicated.
Original languageEnglish
Pages (from-to)4670-4678
JournalJournal of Medicinal Chemistry
Issue number14
Publication statusPublished - 2005


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