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Selective substrate-based inhibitors of mammalian dimethylarginine dimethylaminohydrolase

Rossiter, Sharon and Smith, Caroline L. and Malaki, Mohammed and Nandi, Manasi and Gill, Herpreet and Leiper, James M. and Vallance, Patrick and Selwood, David L. (2005) Selective substrate-based inhibitors of mammalian dimethylarginine dimethylaminohydrolase. Journal of Medicinal Chemistry, 48 (14). pp. 1670-1678. ISSN 0022-2623

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Official URL: http://pubs.acs.org/cgi-bin/article.cgi/jmcmar/200...

Abstract

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.

Item Type:Article
Additional Information:Online ISSN 1520-4804
Research Community:University of Westminster > Life Sciences, School of
ID Code:1680
Deposited On:30 May 2006
Last Modified:07 Apr 2008 14:26

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