Isoform-selective substrates of nitric oxide synthase.

Abstract:

: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.

journal_name

J Med Chem

authors

Jia Q,Cai T,Huang M,Li H,Xian M,Poulos TL,Wang PG

doi

10.1021/jm0340703

keywords:

subject

Has Abstract

pub_date

2003-06-05 00:00:00

pages

2271-4

issue

12

eissn

0022-2623

issn

1520-4804

journal_volume

46

pub_type

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