title: 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.
authors.affiliation: Department of Chemistry, Wayne State University, Detroit, Michigan 48202, USA.
authors.forename: Qiang
authors.initials: Q
authors.lastname: Jia
authors.forename: Tingwei
authors.initials: T
authors.lastname: Cai
authors.forename: Mingchuan
authors.initials: M
authors.lastname: Huang
authors.forename: Huiying
authors.initials: H
authors.lastname: Li
authors.forename: Ming
authors.initials: M
authors.lastname: Xian
authors.forename: Thomas L
authors.initials: TL
authors.lastname: Poulos
authors.forename: Peng G
authors.initials: PG
authors.lastname: Wang
mesh_terms: D006146:Guanidines / Q000138:chemical synthesis* / Q000737:chemistry; D006454:Hemoglobins / Q000737:chemistry; D007527:Isoenzymes / Q000737:chemistry; D019001:Nitric Oxide Synthase / Q000737:chemistry*; D052248:Nitric Oxide Synthase Type I; D052247:Nitric Oxide Synthase Type II; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D006146:Guanidines; D006454:Hemoglobins; D007527:Isoenzymes; D019001:Nitric Oxide Synthase; D052248:Nitric Oxide Synthase Type I; D052247:Nitric Oxide Synthase Type II