Abstract:
:Development of potent and isoform selective nitric oxide synthase (NOS) inhibitors is challenging because of the structural similarity in the heme active sites. One amino acid difference between NOS isoforms, Asp597 in rat neuronal NOS (nNOS) versus Asn368 in bovine endothelial NOS (eNOS), has been identified as the structural basis for why some dipeptide amide inhibitors bind more tightly to nNOS than to eNOS. We now have found that the same amino acid variation is responsible for substantially different binding modes and affinity for a new class of aminopyridine-based inhibitors.
journal_name
Biochemistryjournal_title
Biochemistryauthors
Li H,Wang HY,Kang S,Silverman RB,Poulos TLdoi
10.1021/acs.biochem.6b00261subject
Has Abstractpub_date
2016-07-05 00:00:00pages
3702-7issue
26eissn
0006-2960issn
1520-4995journal_volume
55pub_type
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