2y37
The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS)The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS)
Structural highlights
FunctionNOS2_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 PubMedBy careful analysis of experimental X-ray ligand crystallographic protein data across several inhibitor series we have discovered a novel, potent and selective series of iNOS inhibitors exemplified by compound 8. The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS).,Cheshire DR, Berg A, Andersson GM, Andrews G, Beaton HG, Birkinshaw TN, Boughton-Smith N, Connolly S, Cook TR, Cooper A, Cooper SL, Cox D, Dixon J, Gensmantel N, Hamley PJ, Harrison R, Hartopp P, Kack H, Leeson PD, Luker T, Mete A, Millichip I, Nicholls DJ, Pimm AD, St-Gallay SA, Wallace AV Bioorg Med Chem Lett. 2011 Apr 15;21(8):2468-71. Epub 2011 Feb 18. PMID:21398123[2] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
|
|