5g6c
Structure of Bacillus subtilis Nitric Oxide Synthase I218V in complex with 7-((3-Fluorophenethylamino)ethyl)quinolin-2-amineStructure of Bacillus subtilis Nitric Oxide Synthase I218V in complex with 7-((3-Fluorophenethylamino)ethyl)quinolin-2-amine
Structural highlights
FunctionNOSO_BACSU Catalyzes the production of nitric oxide. Publication Abstract from PubMedNitric oxide (NO) is produced in Gram-positive pathogens Bacillus anthracis and Staphylococcus aureus by the bacterial isoform of nitric oxide synthase (NOS). Inhibition of bacterial nitric oxide synthase (bNOS) has been identified as a promising antibacterial strategy for targeting methicillin-resistant Staphylocoocus aureus1. One class of NOS inhibitors that demonstrates antimicrobial efficacy utilizes an aminoquinoline scaffold. Here we report on a variety of aminoquinolines that target the bacterial NOS active site, in part, by binding to a hydrophobic patch that is unique to bNOS. Through mutagenesis and crystallographic studies, our findings demonstrate that aminoquinolines are an excellent scaffold to further aid in the development of bNOS-specific inhibitors. Targeting Bacterial Nitric Oxide Synthase with Aminoquinoline-based Inhibitors.,Holden JK, Lewis MC, Cinelli MA, Abdullatif Z, Pensa AV, Silverman RB, Poulos TL Biochemistry. 2016 Sep 8. PMID:27607918[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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