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Isoform-selective substrates of nitric oxide synthase
Journal article   Peer reviewed

Isoform-selective substrates of nitric oxide synthase

Qiang Jia, Tingwei Cai, Mingchuan Huang, Huiying Li, Ming Xian, Thomas L Poulos and Peng G Wang
Journal of medicinal chemistry, Vol.46(12), pp.2271-2274
06/05/2003
DOI: https://doi.org/10.1021/jm0340703
Handle:
https://hdl.handle.net/2376/112895
PMID: 12773030

Abstract

Guanidines - chemistry Hemoglobins - chemistry Nitric Oxide Synthase - chemistry Nitric Oxide Synthase Type I Guanidines - chemical synthesis Substrate Specificity Isoenzymes - chemistry Structure-Activity Relationship Nitric Oxide Synthase Type II
Because of the double-edged nature of NO, the development of isoform-selective NOS substrates is a highly desirable goal. Given the striking similarity in the heme active sites of the three NOS isoforms, it presents an challenging problem. Several N-aryl-N'-hydroxyguanidines have recently been shown as substrates that are selective for iNOS over nNOS. Here, we report the first success that 3 is a good substrate for nNOS (70% activity of NOHA, K(m) approximately 40 +/- 6 microM) over iNOS.

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