Structural highlights
Function
[NOS2_MOUSE] Produces nitric oxide (NO) which is a messenger molecule with diverse functions throughout the body. In macrophages, NO mediates tumoricidal and bactericidal actions. Also has nitrosylase activity and mediates cysteine S-nitrosylation of cytoplasmic target proteins such COX2.[1]
Publication Abstract from PubMed
Inducible arginine oxidation and subsequent NO production by correspondent synthase (iNOS) are important cellular answers to proinflammatory signals. Prolonged NO production has been proved in higher organisms to cause stroke or septic shock. Several classes of potent NOS inhibitors have been reported, most of them targeting the arginine binding site of the oxygenase domain. Here we disclose the SAR and the rational design of potent and selective iNOS inhibitors which may be useful as anti-inflammatory drugs.
Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights.,Gradler U, Fuchss T, Ulrich WR, Boer R, Strub A, Hesslinger C, Anezo C, Diederichs K, Zaliani A Bioorg Med Chem Lett. 2011 Jul 15;21(14):4228-32. Epub 2011 May 30. PMID:21684157[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Kim SF, Huri DA, Snyder SH. Inducible nitric oxide synthase binds, S-nitrosylates, and activates cyclooxygenase-2. Science. 2005 Dec 23;310(5756):1966-70. PMID:16373578 doi:http://dx.doi.org/10.1126/science.1119407
- ↑ Gradler U, Fuchss T, Ulrich WR, Boer R, Strub A, Hesslinger C, Anezo C, Diederichs K, Zaliani A. Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4228-32. Epub 2011 May 30. PMID:21684157 doi:10.1016/j.bmcl.2011.05.073
